Ligand source activities (1 row/activity)



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377 2756 53 None -3 10 Human 9.9 pEC50 = 9.9 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acsmedchemlett.2c00052
425 2756 53 None -3 10 Human 9.9 pEC50 = 9.9 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acsmedchemlett.2c00052
448222 2756 53 None -3 10 Human 9.9 pEC50 = 9.9 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acsmedchemlett.2c00052
CHEMBL464859 2756 53 None -3 10 Human 9.9 pEC50 = 9.9 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acsmedchemlett.2c00052
3035850 950 73 None 14 2 Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/jm4007966
457 950 73 None 14 2 Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/jm4007966
CHEMBL431733 950 73 None 14 2 Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/jm4007966
DB12885 950 73 None 14 2 Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/jm4007966
118730350 118136 0 None 1 2 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 424 3 4 9 0.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4cccs4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
CHEMBL3407783 118136 0 None 1 2 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 424 3 4 9 0.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4cccs4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
154730931 171521 1 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 462 4 3 8 1.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N(C)c4cccc(Cl)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL4464176 171521 1 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 462 4 3 8 1.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N(C)c4cccc(Cl)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
168278076 190250 0 None 3 2 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 295 2 0 6 1.9 Cn1nc(-c2ccccc2)c2cnnc(N3CCOCC3)c21 10.1021/acsmedchemlett.2c00052
CHEMBL5175347 190250 0 None 3 2 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 295 2 0 6 1.9 Cn1nc(-c2ccccc2)c2cnnc(N3CCOCC3)c21 10.1021/acsmedchemlett.2c00052
91799687 118126 0 None 4 2 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 420 3 4 10 -0.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4cnccn4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
CHEMBL3407774 118126 0 None 4 2 Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 420 3 4 10 -0.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4cnccn4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
123683 3119 63 None 67 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.8b00435
422 3119 63 None 67 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.8b00435
CHEMBL119709 3119 63 None 67 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.8b00435
DB05511 3119 63 None 67 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.8b00435
118730350 118136 0 None -1 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at human recombinant A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 424 3 4 9 0.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4cccs4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
CHEMBL3407783 118136 0 None -1 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at human recombinant A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 424 3 4 9 0.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4cccs4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
3035850 950 73 None 14 2 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassayAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.5b01998
457 950 73 None 14 2 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassayAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.5b01998
CHEMBL431733 950 73 None 14 2 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassayAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.5b01998
DB12885 950 73 None 14 2 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassayAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.5b01998
168285237 191750 0 None 3 2 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 315 4 1 5 3.6 Cn1nc2c(NCc3ccccc3)nncc2c1-c1ccccc1 10.1021/acsmedchemlett.2c00052
CHEMBL5197567 191750 0 None 3 2 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 315 4 1 5 3.6 Cn1nc2c(NCc3ccccc3)nncc2c1-c1ccccc1 10.1021/acsmedchemlett.2c00052
123683 3119 63 None 67 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
422 3119 63 None 67 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
CHEMBL119709 3119 63 None 67 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
DB05511 3119 63 None 67 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
168281259 190762 0 None 2 2 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 295 2 0 6 1.9 Cn1nc2c(N3CCOCC3)nncc2c1-c1ccccc1 10.1021/acsmedchemlett.2c00052
CHEMBL5183118 190762 0 None 2 2 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 295 2 0 6 1.9 Cn1nc2c(N3CCOCC3)nncc2c1-c1ccccc1 10.1021/acsmedchemlett.2c00052
118730351 118137 2 None 57 2 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 458 3 4 9 1.0 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
CHEMBL3407784 118137 2 None 57 2 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 458 3 4 9 1.0 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
76336527 106061 0 None 501 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 433 5 5 10 0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(Cl)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133161 106061 0 None 501 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 433 5 5 10 0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(Cl)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
9893136 98757 0 None 208 3 Human 9.2 pEC50 = 9.2 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 527 5 4 8 2.0 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/jm9905965
CHEMBL27809 98757 0 None 208 3 Human 9.2 pEC50 = 9.2 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 527 5 4 8 2.0 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/jm9905965
9805713 162844 0 None 309 3 Human 9.2 pEC50 = 9.2 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 493 5 4 8 1.3 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)ncnc31)[C@H](O)[C@@H]2O 10.1021/jm9905965
CHEMBL417292 162844 0 None 309 3 Human 9.2 pEC50 = 9.2 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 493 5 4 8 1.3 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)ncnc31)[C@H](O)[C@@H]2O 10.1021/jm9905965
57523714 76691 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 528 5 4 8 2.5 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL2064653 76691 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 528 5 4 8 2.5 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
168281767 190921 0 None 7 2 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 281 4 1 5 3.1 CC(C)c1nn(C)c2c(NCc3ccccc3)nncc12 10.1021/acsmedchemlett.2c00052
CHEMBL5185411 190921 0 None 7 2 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 281 4 1 5 3.1 CC(C)c1nn(C)c2c(NCc3ccccc3)nncc12 10.1021/acsmedchemlett.2c00052
123683 3119 63 None 67 5 Human 9.0 pEC50 = 9 Functional
Inhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptorInhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptor
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm0255724
422 3119 63 None 67 5 Human 9.0 pEC50 = 9 Functional
Inhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptorInhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptor
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm0255724
CHEMBL119709 3119 63 None 67 5 Human 9.0 pEC50 = 9 Functional
Inhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptorInhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptor
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm0255724
DB05511 3119 63 None 67 5 Human 9.0 pEC50 = 9 Functional
Inhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptorInhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptor
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm0255724
168293746 192151 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 281 4 1 5 3.1 CC(C)c1c2cnnc(NCc3ccccc3)c2nn1C 10.1021/acsmedchemlett.2c00052
CHEMBL5203865 192151 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 281 4 1 5 3.1 CC(C)c1c2cnnc(NCc3ccccc3)c2nn1C 10.1021/acsmedchemlett.2c00052
3035850 950 73 None -14 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMPAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1016/j.bmcl.2008.01.070
457 950 73 None -14 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMPAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1016/j.bmcl.2008.01.070
CHEMBL431733 950 73 None -14 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMPAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1016/j.bmcl.2008.01.070
DB12885 950 73 None -14 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMPAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1016/j.bmcl.2008.01.070
57523213 2671 21 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 30 mins prior to forskolin-stimulation measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 30 mins prior to forskolin-stimulation measured after 15 mins by enzyme immunoassay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/jm300396n
8421 2671 21 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 30 mins prior to forskolin-stimulation measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 30 mins prior to forskolin-stimulation measured after 15 mins by enzyme immunoassay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/jm300396n
CHEMBL2064657 2671 21 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 30 mins prior to forskolin-stimulation measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 30 mins prior to forskolin-stimulation measured after 15 mins by enzyme immunoassay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/jm300396n
3035850 950 73 None -14 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP formation incubated for 45 mins followed by forskolin stimulation and measured after 15 mins by liquid scintillation spectrometry analysisAgonist activity at human A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP formation incubated for 45 mins followed by forskolin stimulation and measured after 15 mins by liquid scintillation spectrometry analysis
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.1c00239
457 950 73 None -14 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP formation incubated for 45 mins followed by forskolin stimulation and measured after 15 mins by liquid scintillation spectrometry analysisAgonist activity at human A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP formation incubated for 45 mins followed by forskolin stimulation and measured after 15 mins by liquid scintillation spectrometry analysis
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.1c00239
CHEMBL431733 950 73 None -14 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP formation incubated for 45 mins followed by forskolin stimulation and measured after 15 mins by liquid scintillation spectrometry analysisAgonist activity at human A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP formation incubated for 45 mins followed by forskolin stimulation and measured after 15 mins by liquid scintillation spectrometry analysis
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.1c00239
DB12885 950 73 None -14 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP formation incubated for 45 mins followed by forskolin stimulation and measured after 15 mins by liquid scintillation spectrometry analysisAgonist activity at human A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP formation incubated for 45 mins followed by forskolin stimulation and measured after 15 mins by liquid scintillation spectrometry analysis
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.1c00239
44359213 119450 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 352 3 4 8 -0.5 CNC(=O)C12CC1C(n1cnc3c(NC)nc(Cl)nc31)C(O)C2O 10.1021/jm020211+
CHEMBL345076 119450 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 352 3 4 8 -0.5 CNC(=O)C12CC1C(n1cnc3c(NC)nc(Cl)nc31)C(O)C2O 10.1021/jm020211+
91799687 118126 0 None -4 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at human recombinant A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 420 3 4 10 -0.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4cnccn4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
CHEMBL3407774 118126 0 None -4 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at human recombinant A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 420 3 4 10 -0.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4cnccn4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
122188579 123182 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP productionAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP production
ChEMBL 471 4 4 8 2.0 CCNc1cc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)NC)C[C@H]12 10.1021/acsmedchemlett.5b00150
CHEMBL3612940 123182 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP productionAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP production
ChEMBL 471 4 4 8 2.0 CCNc1cc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)NC)C[C@H]12 10.1021/acsmedchemlett.5b00150
76311194 106044 0 None 100 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 525 5 5 10 -0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133078 106044 0 None 100 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 525 5 5 10 -0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
44387284 132408 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 568 8 6 11 -0.4 CNCC(=O)NC[C@H]1O[C@@H](n2cnc3c(NCc4ccc(N)c(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm020211+
CHEMBL369744 132408 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 568 8 6 11 -0.4 CNCC(=O)NC[C@H]1O[C@@H](n2cnc3c(NCc4ccc(N)c(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm020211+
44436082 147918 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human adenosine A3 receptor after 15 to 30 minsAgonist activity at human adenosine A3 receptor after 15 to 30 mins
ChEMBL 524 6 3 9 1.1 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](OC)[C@@H]1O 10.1016/j.bmc.2007.05.056
CHEMBL393362 147918 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human adenosine A3 receptor after 15 to 30 minsAgonist activity at human adenosine A3 receptor after 15 to 30 mins
ChEMBL 524 6 3 9 1.1 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](OC)[C@@H]1O 10.1016/j.bmc.2007.05.056
3086599 903 45 None -3 6 Human 8.0 pEC50 = 8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
375 903 45 None -3 6 Human 8.0 pEC50 = 8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
424 903 45 None -3 6 Human 8.0 pEC50 = 8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
CHEMBL331372 903 45 None -3 6 Human 8.0 pEC50 = 8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
76336525 106054 0 None 158 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 337 4 5 10 -1.8 CCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
CHEMBL3133154 106054 0 None 158 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 337 4 5 10 -1.8 CCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
76336526 106055 0 None 31 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 351 5 5 10 -1.4 CCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
CHEMBL3133155 106055 0 None 31 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 351 5 5 10 -1.4 CCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
164619608 185663 0 None 2089 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as cAMP level measured after 35 mins by cAMP enzyme immunoassayAgonist activity at human adenosine A3 receptor transfected in CHO cells assessed as cAMP level measured after 35 mins by cAMP enzyme immunoassay
ChEMBL 433 8 4 9 1.5 OC[C@H]1O[C@@H](n2cnc3c(NCCCCc4ccccc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.ejmech.2021.113607
CHEMBL4864883 185663 0 None 2089 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as cAMP level measured after 35 mins by cAMP enzyme immunoassayAgonist activity at human adenosine A3 receptor transfected in CHO cells assessed as cAMP level measured after 35 mins by cAMP enzyme immunoassay
ChEMBL 433 8 4 9 1.5 OC[C@H]1O[C@@H](n2cnc3c(NCCCCc4ccccc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.ejmech.2021.113607
168288912 191626 0 None -812 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5195714 191626 0 None -812 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
76314797 106047 0 None 3 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 391 5 5 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(NC)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133081 106047 0 None 3 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 391 5 5 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(NC)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
118732979 118518 0 None -14 4 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 437 5 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414945 118518 0 None -14 4 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 437 5 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
2844 283 107 None -1 5 Human 6.0 pEC50 = 6.0 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
60961 283 107 None -1 5 Human 6.0 pEC50 = 6.0 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
90 283 107 None -1 5 Human 6.0 pEC50 = 6.0 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
CHEMBL477 283 107 None -1 5 Human 6.0 pEC50 = 6.0 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
DB00640 283 107 None -1 5 Human 6.0 pEC50 = 6.0 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
377 2756 53 None -3 10 Human 5.0 pEC50 = 5.0 Functional
Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
425 2756 53 None -3 10 Human 5.0 pEC50 = 5.0 Functional
Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
448222 2756 53 None -3 10 Human 5.0 pEC50 = 5.0 Functional
Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
CHEMBL464859 2756 53 None -3 10 Human 5.0 pEC50 = 5.0 Functional
Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
67431601 191074 0 None -575 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 471 8 4 11 1.0 COc1cccc(CO[C@@H]2CCC[C@H]2Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c1 10.1021/acs.jmedchem.2c01414
CHEMBL5187478 191074 0 None -575 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 471 8 4 11 1.0 COc1cccc(CO[C@@H]2CCC[C@H]2Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c1 10.1021/acs.jmedchem.2c01414
137661670 159334 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 509 6 3 12 1.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4100130 159334 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 509 6 3 12 1.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
23643558 86067 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation
ChEMBL 498 5 0 6 6.1 COc1ccc(-n2cc3c(n2)c(N(C(=O)c2ccccc2)C(=O)c2ccccc2)nc2ccccc23)cc1 10.1021/jm070123v
CHEMBL230854 86067 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation
ChEMBL 498 5 0 6 6.1 COc1ccc(-n2cc3c(n2)c(N(C(=O)c2ccccc2)C(=O)c2ccccc2)nc2ccccc23)cc1 10.1021/jm070123v
11706 1129 3 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP formation incubated for 45 mins followed by forskolin stimulation and measured after 15 mins by liquid scintillation spectrometry analysisAgonist activity at human A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP formation incubated for 45 mins followed by forskolin stimulation and measured after 15 mins by liquid scintillation spectrometry analysis
ChEMBL 266 2 3 8 -0.2 O[C@H]1[C@@H](SC[C@H]1N)n1cnc2c(ncnc12)NC 10.1021/acs.jmedchem.1c00239
156587569 1129 3 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP formation incubated for 45 mins followed by forskolin stimulation and measured after 15 mins by liquid scintillation spectrometry analysisAgonist activity at human A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP formation incubated for 45 mins followed by forskolin stimulation and measured after 15 mins by liquid scintillation spectrometry analysis
ChEMBL 266 2 3 8 -0.2 O[C@H]1[C@@H](SC[C@H]1N)n1cnc2c(ncnc12)NC 10.1021/acs.jmedchem.1c00239
CHEMBL5075606 1129 3 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP formation incubated for 45 mins followed by forskolin stimulation and measured after 15 mins by liquid scintillation spectrometry analysisAgonist activity at human A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP formation incubated for 45 mins followed by forskolin stimulation and measured after 15 mins by liquid scintillation spectrometry analysis
ChEMBL 266 2 3 8 -0.2 O[C@H]1[C@@H](SC[C@H]1N)n1cnc2c(ncnc12)NC 10.1021/acs.jmedchem.1c00239
71657835 159735 3 None -7 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL4104819 159735 3 None -7 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
44579714 186983 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECAAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECA
ChEMBL 497 4 3 7 2.6 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NCc3cccc(I)c3)nc(Cl)nc21 10.1021/jm900426g
CHEMBL490605 186983 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECAAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECA
ChEMBL 497 4 3 7 2.6 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NCc3cccc(I)c3)nc(Cl)nc21 10.1021/jm900426g
137659441 159097 0 None 1 4 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 441 6 3 12 0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4097468 159097 0 None 1 4 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 441 6 3 12 0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
168287894 191349 0 None -11 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(Cl)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5191989 191349 0 None -11 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(Cl)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
44586227 191452 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Antagonist activity at human adenosine A3 cells expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulationAntagonist activity at human adenosine A3 cells expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation
ChEMBL 433 4 0 9 0.8 CS(=O)(=O)N(c1nc2ccccc2n2c(=O)n(-c3ccccc3)nc12)S(C)(=O)=O 10.1016/j.bmc.2008.04.039
CHEMBL519319 191452 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Antagonist activity at human adenosine A3 cells expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulationAntagonist activity at human adenosine A3 cells expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation
ChEMBL 433 4 0 9 0.8 CS(=O)(=O)N(c1nc2ccccc2n2c(=O)n(-c3ccccc3)nc12)S(C)(=O)=O 10.1016/j.bmc.2008.04.039
137661505 159494 0 None -3 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4101850 159494 0 None -3 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
137650899 157201 0 None -2 4 Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 413 6 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4076003 157201 0 None -2 4 Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 413 6 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
76325694 106059 0 None -1 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 391 4 5 10 -0.5 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133159 106059 0 None -1 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 391 4 5 10 -0.5 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
16109362 137803 0 None -48 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human A3 adenosine receptor expressed in Flp-In-CHO cells assessed as calcium influx by competitive binding assayAgonist activity at human A3 adenosine receptor expressed in Flp-In-CHO cells assessed as calcium influx by competitive binding assay
ChEMBL 883 20 6 14 4.3 O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c02067
CHEMBL375965 137803 0 None -48 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human A3 adenosine receptor expressed in Flp-In-CHO cells assessed as calcium influx by competitive binding assayAgonist activity at human A3 adenosine receptor expressed in Flp-In-CHO cells assessed as calcium influx by competitive binding assay
ChEMBL 883 20 6 14 4.3 O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c02067
57524978 91266 0 None 38 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 608 6 5 10 1.8 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc(S(=O)(=O)O)cc4)nc31)[C@H](O)[C@@H]2O 10.1021/jm4007966
CHEMBL2401954 91266 0 None 38 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 608 6 5 10 1.8 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc(S(=O)(=O)O)cc4)nc31)[C@H](O)[C@@H]2O 10.1021/jm4007966
118732982 118521 0 None -1 4 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 583 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccccc5I)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414948 118521 0 None -1 4 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 583 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccccc5I)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
2844 283 107 None -1 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
60961 283 107 None -1 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
90 283 107 None -1 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
CHEMBL477 283 107 None -1 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
DB00640 283 107 None -1 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
168279634 191030 0 None -20 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(Cl)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5186981 191030 0 None -20 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(Cl)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
168272212 190429 0 None -3 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 518 10 5 10 1.9 O=C(NCCCCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5178142 190429 0 None -3 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 518 10 5 10 1.9 O=C(NCCCCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccccc1 10.1021/acs.jmedchem.2c00320
132991435 180796 0 None -141 4 Human 6.9 pEC50 = 6.9 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 558 8 5 12 0.8 O=C(NCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccc(S(=O)(=O)F)cc1 10.1021/acs.jmedchem.6b01561
CHEMBL4756472 180796 0 None -141 4 Human 6.9 pEC50 = 6.9 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 558 8 5 12 0.8 O=C(NCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccc(S(=O)(=O)F)cc1 10.1021/acs.jmedchem.6b01561
70695812 73282 0 None -208 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human A3A adenosine receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human A3A adenosine receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 375 5 3 7 2.0 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CC3)C3CC3)nc(Cl)nc21 10.1021/acs.jmedchem.8b01662
CHEMBL2012686 73282 0 None -208 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human A3A adenosine receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human A3A adenosine receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 375 5 3 7 2.0 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CC3)C3CC3)nc(Cl)nc21 10.1021/acs.jmedchem.8b01662
10254700 203524 6 None 2 3 Human 7.9 pEC50 = 7.9 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 483 5 4 9 0.7 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm981090+
CHEMBL66393 203524 6 None 2 3 Human 7.9 pEC50 = 7.9 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 483 5 4 9 0.7 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm981090+
118732975 118514 0 None -4 4 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL3414941 118514 0 None -4 4 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
377 2756 53 None -3 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
425 2756 53 None -3 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
448222 2756 53 None -3 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
CHEMBL464859 2756 53 None -3 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
44232535 95613 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 538 8 5 9 1.7 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#CCCCC(=O)O)nc31)[C@H](O)[C@@H]2O 10.1016/j.bmcl.2008.04.001
CHEMBL257833 95613 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 538 8 5 9 1.7 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#CCCCC(=O)O)nc31)[C@H](O)[C@@H]2O 10.1016/j.bmcl.2008.04.001
137657926 159766 0 None -1 4 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 421 6 3 12 0.3 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4105164 159766 0 None -1 4 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 421 6 3 12 0.3 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
377 2756 53 None -3 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
425 2756 53 None -3 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
448222 2756 53 None -3 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
CHEMBL464859 2756 53 None -3 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
137646828 158004 0 None -25 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 856 16 6 13 6.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCCCNC(=O)c4ccc(-c5sc(N)c(C(=O)c6ccccc6)c5-c5cccc(C(F)(F)F)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.8b00047
CHEMBL4085418 158004 0 None -25 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 856 16 6 13 6.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCCCNC(=O)c4ccc(-c5sc(N)c(C(=O)c6ccccc6)c5-c5cccc(C(F)(F)F)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.8b00047
168297905 192429 0 None -660 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 516 8 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5208245 192429 0 None -660 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 516 8 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
168272014 190208 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 594 12 5 11 3.0 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OCCCC4CCCCC4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5174613 190208 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 594 12 5 11 3.0 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OCCCC4CCCCC4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
168283013 190873 0 None -288 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 516 8 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5184828 190873 0 None -288 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 516 8 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
76318139 105684 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 355 5 3 7 1.7 CCCCC#Cc1nc(NCC)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
CHEMBL3125713 105684 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 355 5 3 7 1.7 CCCCC#Cc1nc(NCC)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
76329265 106058 0 None 2 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 377 4 5 10 -0.9 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133158 106058 0 None 2 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 377 4 5 10 -0.9 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
168289948 191620 1 None 4 2 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 315 4 1 5 3.6 Cn1nc(-c2ccccc2)c2cnnc(NCc3ccccc3)c21 10.1021/acsmedchemlett.2c00052
CHEMBL5195631 191620 1 None 4 2 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 315 4 1 5 3.6 Cn1nc(-c2ccccc2)c2cnnc(NCc3ccccc3)c21 10.1021/acsmedchemlett.2c00052
377 2756 53 None -3 10 Human 7.8 pEC50 = 7.8 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
425 2756 53 None -3 10 Human 7.8 pEC50 = 7.8 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
448222 2756 53 None -3 10 Human 7.8 pEC50 = 7.8 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
CHEMBL464859 2756 53 None -3 10 Human 7.8 pEC50 = 7.8 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
168294594 192337 0 None -141 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 560 8 4 10 1.9 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccc(Br)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5206687 192337 0 None -141 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 560 8 4 10 1.9 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccc(Br)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
377 2756 53 None -3 10 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.ejmech.2021.113983
425 2756 53 None -3 10 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.ejmech.2021.113983
448222 2756 53 None -3 10 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.ejmech.2021.113983
CHEMBL464859 2756 53 None -3 10 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.ejmech.2021.113983
168297825 192281 0 None -251 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5205907 192281 0 None -251 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
377 2756 53 None -3 10 Human 6.8 pEC50 = 6.8 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9905965
425 2756 53 None -3 10 Human 6.8 pEC50 = 6.8 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9905965
448222 2756 53 None -3 10 Human 6.8 pEC50 = 6.8 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9905965
CHEMBL464859 2756 53 None -3 10 Human 6.8 pEC50 = 6.8 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9905965
44359420 33210 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 531 13 7 12 -2.2 NC(=O)CCNC1=C2N=CN([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)C2N=CN1NCCc1ccc(CCC(=O)O)cc1 10.1021/jm020211+
CHEMBL141792 33210 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 531 13 7 12 -2.2 NC(=O)CCNC1=C2N=CN([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)C2N=CN1NCCc1ccc(CCC(=O)O)cc1 10.1021/jm020211+
155562467 175218 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 497 6 4 9 2.5 COc1cc(CCNc2nc(C#Cc3ccccc3)nc3c2ncn3[C@H]2[C@H](O)[C@H](O)[C@@H]3C[C@@H]32)ccc1O 10.1021/acs.jmedchem.0c00235
CHEMBL4571380 175218 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 497 6 4 9 2.5 COc1cc(CCNc2nc(C#Cc3ccccc3)nc3c2ncn3[C@H]2[C@H](O)[C@H](O)[C@@H]3C[C@@H]32)ccc1O 10.1021/acs.jmedchem.0c00235
164617060 185407 0 None 1621 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as cAMP level measured after 35 mins by cAMP enzyme immunoassayAgonist activity at human adenosine A3 receptor transfected in CHO cells assessed as cAMP level measured after 35 mins by cAMP enzyme immunoassay
ChEMBL 440 9 4 9 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.ejmech.2021.113607
CHEMBL4861092 185407 0 None 1621 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as cAMP level measured after 35 mins by cAMP enzyme immunoassayAgonist activity at human adenosine A3 receptor transfected in CHO cells assessed as cAMP level measured after 35 mins by cAMP enzyme immunoassay
ChEMBL 440 9 4 9 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.ejmech.2021.113607
168276883 190198 0 None -309 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5174429 190198 0 None -309 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
372 58 103 None -43 5 Human 5.8 pEC50 = 5.8 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10.1021/jm020211+
8974 58 103 None -43 5 Human 5.8 pEC50 = 5.8 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10.1021/jm020211+
CHEMBL285819 58 103 None -43 5 Human 5.8 pEC50 = 5.8 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10.1021/jm020211+
168282699 191016 0 None -1584 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 427 6 4 10 0.9 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5186757 191016 0 None -1584 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 427 6 4 10 0.9 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
162650156 180068 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Antagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation at 10 uM incubated for 2 hrs by fluorescence based assayAntagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation at 10 uM incubated for 2 hrs by fluorescence based assay
ChEMBL 524 5 1 7 6.7 O=C(Nc1nc(-c2ccccc2)c(-c2nc3ccccc3c(=O)n2-c2ccc(Cl)cc2)s1)c1ccco1 10.1016/j.ejmech.2019.111879
CHEMBL4747947 180068 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Antagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation at 10 uM incubated for 2 hrs by fluorescence based assayAntagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation at 10 uM incubated for 2 hrs by fluorescence based assay
ChEMBL 524 5 1 7 6.7 O=C(Nc1nc(-c2ccccc2)c(-c2nc3ccccc3c(=O)n2-c2ccc(Cl)cc2)s1)c1ccco1 10.1016/j.ejmech.2019.111879
377 2756 53 None -3 10 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.ejmech.2021.113983
425 2756 53 None -3 10 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.ejmech.2021.113983
448222 2756 53 None -3 10 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.ejmech.2021.113983
CHEMBL464859 2756 53 None -3 10 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.ejmech.2021.113983
76318140 105690 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 435 6 3 7 3.0 CCCCC#Cc1nc(NCc2cccc(F)c2)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
CHEMBL3125719 105690 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 435 6 3 7 3.0 CCCCC#Cc1nc(NCc2cccc(F)c2)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
11584486 140906 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 525 6 5 9 0.3 NC(=O)N[C@@H]1[C@@H](CO)O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@@H]1O 10.1021/jm050968b
CHEMBL382194 140906 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 525 6 5 9 0.3 NC(=O)N[C@@H]1[C@@H](CO)O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@@H]1O 10.1021/jm050968b
168285984 191740 0 None -199 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5197358 191740 0 None -199 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
377 2756 53 None -54 10 Mouse 6.7 pEC50 = 6.7 Functional
Partial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysisPartial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysis
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c00235
425 2756 53 None -54 10 Mouse 6.7 pEC50 = 6.7 Functional
Partial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysisPartial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysis
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c00235
448222 2756 53 None -54 10 Mouse 6.7 pEC50 = 6.7 Functional
Partial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysisPartial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysis
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c00235
CHEMBL464859 2756 53 None -54 10 Mouse 6.7 pEC50 = 6.7 Functional
Partial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysisPartial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysis
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c00235
76314563 105685 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 367 5 3 7 1.9 CCCCC#Cc1nc(NC2CC2)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
CHEMBL3125714 105685 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 367 5 3 7 1.9 CCCCC#Cc1nc(NC2CC2)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
57523252 76698 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 652 5 4 8 5.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc5ccc6cccc7ccc4c5c67)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL2064661 76698 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 652 5 4 8 5.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc5ccc6cccc7ccc4c5c67)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
137647420 157699 0 None 2 4 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 501 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4081876 157699 0 None 2 4 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 501 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
137638080 156833 0 None 3 4 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 457 6 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4071338 156833 0 None 3 4 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 457 6 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
137648928 157403 0 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 549 6 3 12 1.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(I)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4078479 157403 0 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 549 6 3 12 1.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(I)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
71764235 91267 0 None - 1 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 608 6 5 10 1.8 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4cccc(S(=O)(=O)O)c4)nc31)[C@H](O)[C@@H]2O 10.1021/jm4007966
CHEMBL2401955 91267 0 None - 1 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 608 6 5 10 1.8 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4cccc(S(=O)(=O)O)c4)nc31)[C@H](O)[C@@H]2O 10.1021/jm4007966
16109359 161776 0 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Activity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cellsActivity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells
ChEMBL 924 21 6 14 4.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCNC(=O)CCCCCNC(=O)COc4ccc(/C=C/C5=[N+]6C(=Cc7ccc(-c8cccs8)n7[B-]6(F)F)C=C5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061279i
CHEMBL414055 161776 0 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Activity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cellsActivity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells
ChEMBL 924 21 6 14 4.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCNC(=O)CCCCCNC(=O)COc4ccc(/C=C/C5=[N+]6C(=Cc7ccc(-c8cccs8)n7[B-]6(F)F)C=C5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061279i
16109359 161776 0 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human A3 adenosine receptor expressed in Flp-In-CHO cells assessed as stimulation of cAMP accumulation by competitive binding assayAgonist activity at human A3 adenosine receptor expressed in Flp-In-CHO cells assessed as stimulation of cAMP accumulation by competitive binding assay
ChEMBL 924 21 6 14 4.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCNC(=O)CCCCCNC(=O)COc4ccc(/C=C/C5=[N+]6C(=Cc7ccc(-c8cccs8)n7[B-]6(F)F)C=C5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.0c02067
CHEMBL414055 161776 0 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human A3 adenosine receptor expressed in Flp-In-CHO cells assessed as stimulation of cAMP accumulation by competitive binding assayAgonist activity at human A3 adenosine receptor expressed in Flp-In-CHO cells assessed as stimulation of cAMP accumulation by competitive binding assay
ChEMBL 924 21 6 14 4.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCNC(=O)CCCCCNC(=O)COc4ccc(/C=C/C5=[N+]6C(=Cc7ccc(-c8cccs8)n7[B-]6(F)F)C=C5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.0c02067
132938348 158212 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as decrease in forskolin induced cAMP formation preincubated for 10 mins followed by forskolin challenge measured after 15 mins by AlphaScreen assayAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as decrease in forskolin induced cAMP formation preincubated for 10 mins followed by forskolin challenge measured after 15 mins by AlphaScreen assay
ChEMBL 574 5 4 8 0.5 CNC(=O)[C@H]1[Se][C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.7b00241
CHEMBL4088081 158212 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as decrease in forskolin induced cAMP formation preincubated for 10 mins followed by forskolin challenge measured after 15 mins by AlphaScreen assayAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as decrease in forskolin induced cAMP formation preincubated for 10 mins followed by forskolin challenge measured after 15 mins by AlphaScreen assay
ChEMBL 574 5 4 8 0.5 CNC(=O)[C@H]1[Se][C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.7b00241
45482610 198025 0 None 2 2 Human 8.6 pEC50 = 8.6 Functional
Agonistic effect at human adenosine A3 receptor in CHO cellsAgonistic effect at human adenosine A3 receptor in CHO cells
ChEMBL 406 4 4 8 0.9 CNC(=O)[C@]12C[C@@H]1[C@@H](n1cnc3c(NC4CCCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/jm050726b
CHEMBL573937 198025 0 None 2 2 Human 8.6 pEC50 = 8.6 Functional
Agonistic effect at human adenosine A3 receptor in CHO cellsAgonistic effect at human adenosine A3 receptor in CHO cells
ChEMBL 406 4 4 8 0.9 CNC(=O)[C@]12C[C@@H]1[C@@H](n1cnc3c(NC4CCCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/jm050726b
3035850 950 73 None -14 2 Human 8.6 pEC50 = 8.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/jm020211+
457 950 73 None -14 2 Human 8.6 pEC50 = 8.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/jm020211+
CHEMBL431733 950 73 None -14 2 Human 8.6 pEC50 = 8.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/jm020211+
DB12885 950 73 None -14 2 Human 8.6 pEC50 = 8.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/jm020211+
127047826 140004 0 None - 1 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassayAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
ChEMBL 403 2 3 7 0.6 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(C)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.5b01998
CHEMBL3800048 140004 0 None - 1 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassayAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
ChEMBL 403 2 3 7 0.6 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(C)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.5b01998
415 3649 12 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H](Cc1ccccc1)C 10.1021/jm020211+
5312112 3649 12 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H](Cc1ccccc1)C 10.1021/jm020211+
CHEMBL420705 3649 12 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H](Cc1ccccc1)C 10.1021/jm020211+
168270868 189929 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 578 7 5 11 1.8 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(O)c(OC)c4)nc(C#Cc4ccc(F)s4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5170037 189929 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 578 7 5 11 1.8 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(O)c(OC)c4)nc(C#Cc4ccc(F)s4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
168280775 191155 0 None -15 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 524 7 4 10 2.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(C(C)(C)C)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5188601 191155 0 None -15 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 524 7 4 10 2.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(C(C)(C)C)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
168270868 189929 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 578 7 5 11 1.8 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(O)c(OC)c4)nc(C#Cc4ccc(F)s4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5170037 189929 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 578 7 5 11 1.8 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(O)c(OC)c4)nc(C#Cc4ccc(F)s4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
155537599 172322 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 491 5 3 8 3.5 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NCCc3ccccc3)nc(C#Cc3ccc(Cl)s3)nc21 10.1021/acs.jmedchem.0c00235
CHEMBL4475372 172322 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 491 5 3 8 3.5 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NCCc3ccccc3)nc(C#Cc3ccc(Cl)s3)nc21 10.1021/acs.jmedchem.0c00235
380 1286 54 None -724 5 Human 6.6 pEC50 = 6.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1021/jm020211+
657378 1286 54 None -724 5 Human 6.6 pEC50 = 6.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1021/jm020211+
CHEMBL68738 1286 54 None -724 5 Human 6.6 pEC50 = 6.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1021/jm020211+
137657841 159568 0 None 1 4 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4102750 159568 0 None 1 4 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
168278159 190358 0 None -812 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 839 15 5 15 6.6 Nc1sc(-c2ccc(-c3cn(CCCCCCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)nn3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5177040 190358 0 None -812 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 839 15 5 15 6.6 Nc1sc(-c2ccc(-c3cn(CCCCCCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)nn3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
76332918 106052 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 433 7 4 10 0.4 CCN(CC)c1nc(NC2CCCC2)c2ncn([C@@H]3O[C@H](C(=O)NC)[C@@H](O)[C@H]3O)c2n1 10.1039/C3MD00364G
CHEMBL3133152 106052 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 433 7 4 10 0.4 CCN(CC)c1nc(NC2CCCC2)c2ncn([C@@H]3O[C@H](C(=O)NC)[C@@H](O)[C@H]3O)c2n1 10.1039/C3MD00364G
10450691 99456 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptorAgonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptor
ChEMBL 352 3 4 8 -0.5 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1016/s0960-894x(01)00213-x
CHEMBL283057 99456 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptorAgonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptor
ChEMBL 352 3 4 8 -0.5 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1016/s0960-894x(01)00213-x
377 2756 53 None -3 10 Human 7.6 pEC50 = 7.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm020211+
425 2756 53 None -3 10 Human 7.6 pEC50 = 7.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm020211+
448222 2756 53 None -3 10 Human 7.6 pEC50 = 7.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm020211+
CHEMBL464859 2756 53 None -3 10 Human 7.6 pEC50 = 7.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm020211+
8975 100397 90 None - 1 Human 5.6 pEC50 = 5.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 285 2 4 9 -1.8 Nc1nc(F)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm020211+
CHEMBL290077 100397 90 None - 1 Human 5.6 pEC50 = 5.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 285 2 4 9 -1.8 Nc1nc(F)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm020211+
414 3380 33 None -3 5 Human 7.6 pEC50 = 7.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 10.1021/jm020211+
93205 3380 33 None -3 5 Human 7.6 pEC50 = 7.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 10.1021/jm020211+
CHEMBL139000 3380 33 None -3 5 Human 7.6 pEC50 = 7.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 10.1021/jm020211+
11756182 79223 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 513 6 3 9 2.0 CSC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm981090+
CHEMBL2113427 79223 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 513 6 3 9 2.0 CSC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm981090+
76332686 105686 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 395 5 3 7 2.6 CCCCC#Cc1nc(NC2CCCC2)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
CHEMBL3125715 105686 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 395 5 3 7 2.6 CCCCC#Cc1nc(NC2CCCC2)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
168270204 190061 0 None -19498 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 560 8 4 10 1.9 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(Br)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5172389 190061 0 None -19498 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 560 8 4 10 1.9 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(Br)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
168283120 191059 0 None -20892 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 498 8 4 11 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(OC)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5187330 191059 0 None -20892 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 498 8 4 11 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(OC)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
144852560 170934 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human A3AR expressed in CHO cells assessed as suppression of NECA-induced reduction in cAMP accumulationAntagonist activity at human A3AR expressed in CHO cells assessed as suppression of NECA-induced reduction in cAMP accumulation
ChEMBL 343 2 2 5 3.8 Clc1ccc(C#Cc2nc(NC3CCCC3)c3nc[nH]c3n2)s1 10.1039/C8MD00317C
CHEMBL4455344 170934 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human A3AR expressed in CHO cells assessed as suppression of NECA-induced reduction in cAMP accumulationAntagonist activity at human A3AR expressed in CHO cells assessed as suppression of NECA-induced reduction in cAMP accumulation
ChEMBL 343 2 2 5 3.8 Clc1ccc(C#Cc2nc(NC3CCCC3)c3nc[nH]c3n2)s1 10.1039/C8MD00317C
137639588 156882 0 None 1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccccc2C(=O)NCCCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4072009 156882 0 None 1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccccc2C(=O)NCCCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
137646655 157624 0 None -4 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 711 13 6 12 4.8 Nc1cc(-c2cccc(C(F)(F)F)c2)c(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)s1 10.1021/acs.jmedchem.8b00047
CHEMBL4081224 157624 0 None -4 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 711 13 6 12 4.8 Nc1cc(-c2cccc(C(F)(F)F)c2)c(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)s1 10.1021/acs.jmedchem.8b00047
2844 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cellsAgonist activity at human adenosine A3 receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
60961 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cellsAgonist activity at human adenosine A3 receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
90 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cellsAgonist activity at human adenosine A3 receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
CHEMBL477 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cellsAgonist activity at human adenosine A3 receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
DB00640 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cellsAgonist activity at human adenosine A3 receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
2844 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
60961 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
90 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
CHEMBL477 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
DB00640 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
2844 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
60961 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
90 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
CHEMBL477 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
DB00640 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
2844 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adenosine A3 receptor by cAMP assayAgonist activity at human recombinant adenosine A3 receptor by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
60961 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adenosine A3 receptor by cAMP assayAgonist activity at human recombinant adenosine A3 receptor by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
90 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adenosine A3 receptor by cAMP assayAgonist activity at human recombinant adenosine A3 receptor by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
CHEMBL477 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adenosine A3 receptor by cAMP assayAgonist activity at human recombinant adenosine A3 receptor by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
DB00640 283 107 None -1 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adenosine A3 receptor by cAMP assayAgonist activity at human recombinant adenosine A3 receptor by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
377 2756 53 None -3 10 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
425 2756 53 None -3 10 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
448222 2756 53 None -3 10 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
CHEMBL464859 2756 53 None -3 10 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
44354130 23521 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 554 5 4 8 1.7 CNC(=O)C12CC1C(n1cnc3c(NCc4cccc(I)c4)nc(Cl)nc31)C(O)C2O 10.1021/jm020211+
CHEMBL133387 23521 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 554 5 4 8 1.7 CNC(=O)C12CC1C(n1cnc3c(NCc4cccc(I)c4)nc(Cl)nc31)C(O)C2O 10.1021/jm020211+
CHEMBL5078671 214575 0 None -1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at A3 adenosine receptor (unknown origin)Agonist activity at A3 adenosine receptor (unknown origin)
ChEMBL None None None CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCNC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](C)NC(=O)CCCCCNC(=O)COc4ccc(/C=C/C5=[N+]6C(=Cc7ccc(-c8cccs8)n7[B-]6(F)F)C=C5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.0c02067
71764237 91271 0 None - 1 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 508 6 4 8 1.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccccc4)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/jm4007966
CHEMBL2402024 91271 0 None - 1 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 508 6 4 8 1.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccccc4)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/jm4007966
9828356 10527 11 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptorInhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptor
ChEMBL 528 8 4 12 1.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cc(Cl)ccc4OCc4cc(C)no4)ncnc32)[C@H](O)[C@@H]1N 10.1021/jm0255724
CHEMBL116878 10527 11 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptorInhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptor
ChEMBL 528 8 4 12 1.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cc(Cl)ccc4OCc4cc(C)no4)ncnc32)[C@H](O)[C@@H]1N 10.1021/jm0255724
137642036 158150 0 None 2 4 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 387 6 3 12 -0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4087306 158150 0 None 2 4 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 387 6 3 12 -0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
123683 3119 63 None 67 5 Human 8.4 pEC50 = 8.4 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm020211+
422 3119 63 None 67 5 Human 8.4 pEC50 = 8.4 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm020211+
CHEMBL119709 3119 63 None 67 5 Human 8.4 pEC50 = 8.4 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm020211+
DB05511 3119 63 None 67 5 Human 8.4 pEC50 = 8.4 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm020211+
23643659 92308 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation
ChEMBL 454 5 1 4 6.3 O=C(Nc1nc2ccccc2c2cn(-c3ccccc3)nc12)C(c1ccccc1)c1ccccc1 10.1021/jm070123v
CHEMBL242849 92308 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation
ChEMBL 454 5 1 4 6.3 O=C(Nc1nc2ccccc2c2cn(-c3ccccc3)nc12)C(c1ccccc1)c1ccccc1 10.1021/jm070123v
76329263 106045 0 None 19 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 413 6 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133079 106045 0 None 19 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 413 6 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
168293442 192133 0 None -12589 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 546 7 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Br)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5203632 192133 0 None -12589 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 546 7 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Br)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
44563977 189697 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assayAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assay
ChEMBL 574 6 4 10 1.7 CNC(=O)OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm8014052
CHEMBL515442 189697 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assayAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assay
ChEMBL 574 6 4 10 1.7 CNC(=O)OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm8014052
168274237 190467 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 524 10 5 11 1.0 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OCC4CC4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5178814 190467 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 524 10 5 11 1.0 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OCC4CC4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
137651747 157479 0 None -1 4 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4079433 157479 0 None -1 4 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
76329266 106060 0 None 3 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 399 5 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133160 106060 0 None 3 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 399 5 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
56627882 118510 0 None -8 4 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 367 3 3 12 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414937 118510 0 None -8 4 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 367 3 3 12 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
57523253 76672 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 652 5 4 8 5.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4cc5cccc6ccc7cccc4c7c65)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL2064634 76672 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 652 5 4 8 5.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4cc5cccc6ccc7cccc4c7c65)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
118732980 118519 0 None -4 4 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 461 5 3 12 1.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414946 118519 0 None -4 4 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 461 5 3 12 1.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
137652475 157143 0 None -4 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 829 16 6 13 6.5 Nc1sc(-c2ccc(C(=O)NCCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4075186 157143 0 None -4 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 829 16 6 13 6.5 Nc1sc(-c2ccc(C(=O)NCCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
137641858 158305 0 None -3 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 696 13 5 11 5.3 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccc(-c2sccc2-c2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.8b00047
CHEMBL4089092 158305 0 None -3 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 696 13 5 11 5.3 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccc(-c2sccc2-c2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.8b00047
377 2756 53 None -3 10 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2008.04.001
425 2756 53 None -3 10 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2008.04.001
448222 2756 53 None -3 10 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2008.04.001
CHEMBL464859 2756 53 None -3 10 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2008.04.001
162645916 179494 0 None -4 4 Human 6.5 pEC50 = 6.5 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 414 6 4 11 0.8 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccc(CN=C=S)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.6b01561
CHEMBL4741079 179494 0 None -4 4 Human 6.5 pEC50 = 6.5 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 414 6 4 11 0.8 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccc(CN=C=S)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.6b01561
168288096 191701 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 580 6 5 11 2.3 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4ccc(O)c(OC)c4)nc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5196916 191701 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 580 6 5 11 2.3 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4ccc(O)c(OC)c4)nc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
168288096 191701 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 580 6 5 11 2.3 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4ccc(O)c(OC)c4)nc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5196916 191701 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 580 6 5 11 2.3 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4ccc(O)c(OC)c4)nc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
42626221 179411 14 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 412 4 1 8 2.7 COc1ccc(-n2nc3c(NC(=O)c4ccccc4)nc4ncccc4n3c2=O)cc1 10.1021/jm8014876
CHEMBL474016 179411 14 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 412 4 1 8 2.7 COc1ccc(-n2nc3c(NC(=O)c4ccccc4)nc4ncccc4n3c2=O)cc1 10.1021/jm8014876
393595 2635 51 None 16 3 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 10 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 10 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 403 4 1 6 4.4 O=C(Nc1nc2ccc(cc2c2n1nc(n2)c1ccco1)Cl)Cc1ccccc1 10.1021/acsmedchemlett.2c00052
448 2635 51 None 16 3 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 10 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 10 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 403 4 1 6 4.4 O=C(Nc1nc2ccc(cc2c2n1nc(n2)c1ccco1)Cl)Cc1ccccc1 10.1021/acsmedchemlett.2c00052
CHEMBL88147 2635 51 None 16 3 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 10 uM incubated with NECA for 30 mins by LANCE cAMP detection assayAntagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 10 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
ChEMBL 403 4 1 6 4.4 O=C(Nc1nc2ccc(cc2c2n1nc(n2)c1ccco1)Cl)Cc1ccccc1 10.1021/acsmedchemlett.2c00052
118732981 118520 0 None -1 4 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 495 5 3 12 2.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414947 118520 0 None -1 4 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 495 5 3 12 2.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
168274237 190467 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 524 10 5 11 1.0 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OCC4CC4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5178814 190467 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 524 10 5 11 1.0 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OCC4CC4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
98567 191779 18 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP productionAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP production
ChEMBL 294 2 4 9 -2.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/acsmedchemlett.5b00150
CHEMBL519809 191779 18 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP productionAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP production
ChEMBL 294 2 4 9 -2.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/acsmedchemlett.5b00150
168277923 190677 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 484 8 5 11 0.2 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OC)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5181821 190677 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 484 8 5 11 0.2 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OC)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
92208 142351 60 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 357 5 4 9 0.1 OC[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm981090+
CHEMBL388757 142351 60 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 357 5 4 9 0.1 OC[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm981090+
118732975 118514 0 None -4 4 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414941 118514 0 None -4 4 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
168281601 191269 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 594 7 5 11 2.3 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(O)c(OC)c4)nc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5190575 191269 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 594 7 5 11 2.3 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(O)c(OC)c4)nc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
76329264 106051 0 None 12 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 405 6 5 10 -0.0 CCNc1nc(NC2CCCC2)c2ncn([C@@H]3O[C@H](C(=O)NC)[C@@H](O)[C@H]3O)c2n1 10.1039/C3MD00364G
CHEMBL3133151 106051 0 None 12 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 405 6 5 10 -0.0 CCNc1nc(NC2CCCC2)c2ncn([C@@H]3O[C@H](C(=O)NC)[C@@H](O)[C@H]3O)c2n1 10.1039/C3MD00364G
76311197 106056 0 None 19 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 365 6 5 10 -1.0 CCCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
CHEMBL3133156 106056 0 None 19 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 365 6 5 10 -1.0 CCCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
3035850 950 73 None -14 2 Human 8.4 pEC50 = 8.4 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.0c00235
457 950 73 None -14 2 Human 8.4 pEC50 = 8.4 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.0c00235
CHEMBL431733 950 73 None -14 2 Human 8.4 pEC50 = 8.4 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.0c00235
DB12885 950 73 None -14 2 Human 8.4 pEC50 = 8.4 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.0c00235
44579716 186984 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECAAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECA
ChEMBL 449 4 3 7 2.8 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NCc3cccc(Br)c3)nc(Cl)nc21 10.1021/jm900426g
CHEMBL490606 186984 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECAAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECA
ChEMBL 449 4 3 7 2.8 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NCc3cccc(Br)c3)nc(Cl)nc21 10.1021/jm900426g
377 2756 53 None -3 10 Human 8.3 pEC50 = 8.3 Functional
Activity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cellsActivity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
425 2756 53 None -3 10 Human 8.3 pEC50 = 8.3 Functional
Activity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cellsActivity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
448222 2756 53 None -3 10 Human 8.3 pEC50 = 8.3 Functional
Activity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cellsActivity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
CHEMBL464859 2756 53 None -3 10 Human 8.3 pEC50 = 8.3 Functional
Activity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cellsActivity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
136048802 140014 0 None - 1 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassayAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
ChEMBL 507 4 4 8 2.3 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(/C=C(\O)c4ccccc4)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.5b01998
CHEMBL3800106 140014 0 None - 1 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassayAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
ChEMBL 507 4 4 8 2.3 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(/C=C(\O)c4ccccc4)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.5b01998
137649841 157428 0 None -3 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 656 14 5 12 3.8 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cc(C(=O)c3ccccc3)cs2)c1 10.1021/acs.jmedchem.8b00047
CHEMBL4078771 157428 0 None -3 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 656 14 5 12 3.8 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cc(C(=O)c3ccccc3)cs2)c1 10.1021/acs.jmedchem.8b00047
168269860 189974 0 None -1949 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 512 9 4 11 1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(OC)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5170857 189974 0 None -1949 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 512 9 4 11 1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(OC)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
168281601 191269 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 594 7 5 11 2.3 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(O)c(OC)c4)nc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5190575 191269 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 594 7 5 11 2.3 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(O)c(OC)c4)nc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
132991434 179956 0 None -4 4 Human 7.4 pEC50 = 7.4 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 564 8 6 12 2.4 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccc(CNC(=S)Nc5ccc(N=C=S)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.6b01561
CHEMBL4746617 179956 0 None -4 4 Human 7.4 pEC50 = 7.4 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 564 8 6 12 2.4 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccc(CNC(=S)Nc5ccc(N=C=S)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.6b01561
137650221 157253 0 None -1 4 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 463 6 3 13 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4076561 157253 0 None -1 4 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 463 6 3 13 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
137650918 157243 0 None -12 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 671 14 6 13 3.4 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)cc1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4076495 157243 0 None -12 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 671 14 6 13 3.4 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)cc1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
137650461 157254 0 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 857 16 6 13 6.4 CC(=O)Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4076565 157254 0 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 857 16 6 13 6.4 CC(=O)Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
76321824 105683 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 341 4 3 7 1.3 CCCCC#Cc1nc(NC)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
CHEMBL3125712 105683 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 341 4 3 7 1.3 CCCCC#Cc1nc(NC)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
168292629 192048 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 526 10 5 11 1.3 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OCC(C)C)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5202349 192048 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 526 10 5 11 1.3 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OCC(C)C)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
44436080 88638 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human adenosine A3 receptor after 15 to 30 minsAgonist activity at human adenosine A3 receptor after 15 to 30 mins
ChEMBL 308 3 3 9 -1.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](OC)[C@@H]1O 10.1016/j.bmc.2007.05.056
CHEMBL235742 88638 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human adenosine A3 receptor after 15 to 30 minsAgonist activity at human adenosine A3 receptor after 15 to 30 mins
ChEMBL 308 3 3 9 -1.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](OC)[C@@H]1O 10.1016/j.bmc.2007.05.056
377 2756 53 None -3 10 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
425 2756 53 None -3 10 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
448222 2756 53 None -3 10 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
CHEMBL464859 2756 53 None -3 10 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
10407895 79216 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 387 6 3 9 1.4 CSC[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm981090+
CHEMBL2113420 79216 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 387 6 3 9 1.4 CSC[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm981090+
168276950 190295 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 540 11 5 11 1.6 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OCCC(C)C)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5175945 190295 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 540 11 5 11 1.6 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OCCC(C)C)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
76322076 106046 0 None 39 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 489 7 5 10 1.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133080 106046 0 None 39 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 489 7 5 10 1.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
76332919 106053 0 None 316 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 323 3 5 10 -2.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133153 106053 0 None 316 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 323 3 5 10 -2.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
76318403 106057 0 None 12 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 363 4 5 10 -1.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133157 106057 0 None 12 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 363 4 5 10 -1.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
57523213 2671 21 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.8b00435
8421 2671 21 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.8b00435
CHEMBL2064657 2671 21 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.8b00435
10254700 203524 6 None 2 3 Human 8.3 pEC50 = 8.3 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 483 5 4 9 0.7 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9905965
CHEMBL66393 203524 6 None 2 3 Human 8.3 pEC50 = 8.3 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 483 5 4 9 0.7 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9905965
162650156 180068 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Antagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 2 hrs by fluorescence based assayAntagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 2 hrs by fluorescence based assay
ChEMBL 524 5 1 7 6.7 O=C(Nc1nc(-c2ccccc2)c(-c2nc3ccccc3c(=O)n2-c2ccc(Cl)cc2)s1)c1ccco1 10.1016/j.ejmech.2019.111879
CHEMBL4747947 180068 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Antagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 2 hrs by fluorescence based assayAntagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 2 hrs by fluorescence based assay
ChEMBL 524 5 1 7 6.7 O=C(Nc1nc(-c2ccccc2)c(-c2nc3ccccc3c(=O)n2-c2ccc(Cl)cc2)s1)c1ccco1 10.1016/j.ejmech.2019.111879
118732974 118513 0 None -2 4 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL3414940 118513 0 None -2 4 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
44359364 30630 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 520 5 4 8 1.1 CNC(=O)C12CC1C(n1cnc3c(NCc4cccc(I)c4)ncnc31)C(O)C2O 10.1021/jm020211+
CHEMBL139417 30630 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 520 5 4 8 1.1 CNC(=O)C12CC1C(n1cnc3c(NCc4cccc(I)c4)ncnc31)C(O)C2O 10.1021/jm020211+
9996279 110353 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Effective concentration for inhibition of NECA-stimulated [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cellsEffective concentration for inhibition of NECA-stimulated [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cells
ChEMBL 323 2 1 7 1.2 O=c1[nH]c2ccccc2n2c(=O)n(-c3ccc([N+](=O)[O-])cc3)nc12 10.1021/jm031136l
CHEMBL324095 110353 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Effective concentration for inhibition of NECA-stimulated [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cellsEffective concentration for inhibition of NECA-stimulated [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cells
ChEMBL 323 2 1 7 1.2 O=c1[nH]c2ccccc2n2c(=O)n(-c3ccc([N+](=O)[O-])cc3)nc12 10.1021/jm031136l
16109362 137803 0 None -48 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at A3 adenosine receptor (unknown origin)Agonist activity at A3 adenosine receptor (unknown origin)
ChEMBL 883 20 6 14 4.3 O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c02067
CHEMBL375965 137803 0 None -48 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at A3 adenosine receptor (unknown origin)Agonist activity at A3 adenosine receptor (unknown origin)
ChEMBL 883 20 6 14 4.3 O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c02067
168277923 190677 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 484 8 5 11 0.2 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OC)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5181821 190677 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 484 8 5 11 0.2 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OC)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
168292629 192048 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 526 10 5 11 1.3 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OCC(C)C)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5202349 192048 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 526 10 5 11 1.3 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OCC(C)C)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
118732974 118513 0 None -2 4 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414940 118513 0 None -2 4 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
168290627 192001 0 None -3 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 859 11 6 13 6.6 Nc1sc(-c2ccc(C(=O)NCCC#Cc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5201533 192001 0 None -3 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 859 11 6 13 6.6 Nc1sc(-c2ccc(C(=O)NCCC#Cc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
137641990 158077 0 None 1 4 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 447 6 3 13 0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4086325 158077 0 None 1 4 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 447 6 3 13 0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
9850648 98148 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptorAgonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptor
ChEMBL 554 5 4 8 1.7 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1016/s0960-894x(01)00213-x
CHEMBL27376 98148 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptorAgonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptor
ChEMBL 554 5 4 8 1.7 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1016/s0960-894x(01)00213-x
71355811 79201 6 None 1348 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as cAMP level measured after 35 mins by cAMP enzyme immunoassayAgonist activity at human adenosine A3 receptor transfected in CHO cells assessed as cAMP level measured after 35 mins by cAMP enzyme immunoassay
ChEMBL 399 8 4 9 0.9 OC[C@H]1O[C@@H](n2cnc3c(NCCCCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.ejmech.2021.113607
CHEMBL2113406 79201 6 None 1348 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as cAMP level measured after 35 mins by cAMP enzyme immunoassayAgonist activity at human adenosine A3 receptor transfected in CHO cells assessed as cAMP level measured after 35 mins by cAMP enzyme immunoassay
ChEMBL 399 8 4 9 0.9 OC[C@H]1O[C@@H](n2cnc3c(NCCCCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.ejmech.2021.113607
162650156 180068 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Antagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation at 3 uM incubated for 2 hrs by fluorescence based assayAntagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation at 3 uM incubated for 2 hrs by fluorescence based assay
ChEMBL 524 5 1 7 6.7 O=C(Nc1nc(-c2ccccc2)c(-c2nc3ccccc3c(=O)n2-c2ccc(Cl)cc2)s1)c1ccco1 10.1016/j.ejmech.2019.111879
CHEMBL4747947 180068 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Antagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation at 3 uM incubated for 2 hrs by fluorescence based assayAntagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation at 3 uM incubated for 2 hrs by fluorescence based assay
ChEMBL 524 5 1 7 6.7 O=C(Nc1nc(-c2ccccc2)c(-c2nc3ccccc3c(=O)n2-c2ccc(Cl)cc2)s1)c1ccco1 10.1016/j.ejmech.2019.111879
168286257 191594 0 None -11 4 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 863 14 6 13 6.3 Nc1sc(-c2ccc(C(=O)NCCc3ccc(CCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5195260 191594 0 None -11 4 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 863 14 6 13 6.3 Nc1sc(-c2ccc(C(=O)NCCc3ccc(CCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
137642153 158366 0 None -4 4 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 429 6 3 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4089741 158366 0 None -4 4 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 429 6 3 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
118732972 118511 0 None 15 4 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 347 4 3 12 -1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414938 118511 0 None 15 4 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 347 4 3 12 -1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
118732978 118517 0 None -7 4 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 403 5 3 13 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414944 118517 0 None -7 4 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 403 5 3 13 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
76325693 106048 0 None 7 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 405 5 4 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N(C)C)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133082 106048 0 None 7 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 405 5 4 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N(C)C)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
168293013 192107 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 548 6 4 9 2.6 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccccc4)nc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5203255 192107 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 548 6 4 9 2.6 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccccc4)nc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
137653409 159035 0 None -1 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 567 12 6 12 2.2 Nc1ccc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)s1 10.1021/acs.jmedchem.8b00047
CHEMBL4096796 159035 0 None -1 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 567 12 6 12 2.2 Nc1ccc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)s1 10.1021/acs.jmedchem.8b00047
168293013 192107 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 548 6 4 9 2.6 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccccc4)nc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5203255 192107 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 548 6 4 9 2.6 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccccc4)nc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
168285878 191631 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 594 8 4 10 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(OC)c4)nc(I)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5195772 191631 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
ChEMBL 594 8 4 10 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(OC)c4)nc(I)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
168269866 189986 0 None -229 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 468 7 4 10 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5171042 189986 0 None -229 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 468 7 4 10 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
10256116 99080 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptorAgonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptor
ChEMBL 520 5 4 8 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)ncnc31)[C@H](O)[C@@H]2O 10.1016/s0960-894x(01)00213-x
CHEMBL280580 99080 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptorAgonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptor
ChEMBL 520 5 4 8 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)ncnc31)[C@H](O)[C@@H]2O 10.1016/s0960-894x(01)00213-x
168276950 190295 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 540 11 5 11 1.6 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OCCC(C)C)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5175945 190295 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 540 11 5 11 1.6 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(O)c4)nc(OCCC(C)C)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
155540779 172513 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 581 6 4 10 3.3 COc1cc(CCNc2nc(C#Cc3ccc(Br)s3)nc3c2ncn3[C@H]2[C@H](O)[C@H](O)[C@@H]3C[C@@H]32)ccc1O 10.1021/acs.jmedchem.0c00235
CHEMBL4483546 172513 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 581 6 4 10 3.3 COc1cc(CCNc2nc(C#Cc3ccc(Br)s3)nc3c2ncn3[C@H]2[C@H](O)[C@H](O)[C@@H]3C[C@@H]32)ccc1O 10.1021/acs.jmedchem.0c00235
137661132 159173 0 None 2 4 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 491 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4098377 159173 0 None 2 4 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 491 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
118732973 118512 0 None 30 4 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 381 4 3 12 -0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414939 118512 0 None 30 4 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 381 4 3 12 -0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
57523251 76697 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 604 6 4 8 4.2 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc(-c5ccccc5)cc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL2064660 76697 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 604 6 4 8 4.2 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc(-c5ccccc5)cc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
118732977 118516 0 None -70 3 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 461 5 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N[C@H]5C[C@@H]6CC[C@@H]5C6)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414943 118516 0 None -70 3 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 461 5 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N[C@H]5C[C@@H]6CC[C@@H]5C6)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
168285878 191631 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 594 8 4 10 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(OC)c4)nc(I)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
CHEMBL5195772 191631 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assayAgonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay
ChEMBL 594 8 4 10 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccc(OC)c(OC)c4)nc(I)nc31)[C@H](O)[C@@H]2O 10.1016/j.ejmech.2021.113983
377 2756 53 None -3 10 Human 7.1 pEC50 = 7.1 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
425 2756 53 None -3 10 Human 7.1 pEC50 = 7.1 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
448222 2756 53 None -3 10 Human 7.1 pEC50 = 7.1 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
CHEMBL464859 2756 53 None -3 10 Human 7.1 pEC50 = 7.1 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
168293564 192155 0 None -125 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 849 13 6 13 6.8 Nc1sc(-c2ccc(C(=O)NCCCc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5203917 192155 0 None -125 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 849 13 6 13 6.8 Nc1sc(-c2ccc(C(=O)NCCCc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
71657835 159735 3 None -7 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4104819 159735 3 None -7 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
380 1286 54 None -724 5 Human 5.1 pEC50 = 5.1 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1021/jm9905965
657378 1286 54 None -724 5 Human 5.1 pEC50 = 5.1 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1021/jm9905965
CHEMBL68738 1286 54 None -724 5 Human 5.1 pEC50 = 5.1 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1021/jm9905965
11962166 77875 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inhibition of isoproterenol-induced increase of cAMP in HEK293 cell expressing human adenosine A3 receptorInhibition of isoproterenol-induced increase of cAMP in HEK293 cell expressing human adenosine A3 receptor
ChEMBL 559 8 5 12 -0.8 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cc(Cl)ccc4OCC(=O)N4CCNCC4)ncnc32)[C@H](O)[C@@H]1N 10.1016/j.bmcl.2006.01.088
CHEMBL209352 77875 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inhibition of isoproterenol-induced increase of cAMP in HEK293 cell expressing human adenosine A3 receptorInhibition of isoproterenol-induced increase of cAMP in HEK293 cell expressing human adenosine A3 receptor
ChEMBL 559 8 5 12 -0.8 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cc(Cl)ccc4OCC(=O)N4CCNCC4)ncnc32)[C@H](O)[C@@H]1N 10.1016/j.bmcl.2006.01.088
44359214 116757 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 311 2 4 8 -0.7 Nc1nc(Cl)nc2c1ncn2C1C(O)C(O)C2(CO)CC12 10.1021/jm020211+
CHEMBL337602 116757 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 311 2 4 8 -0.7 Nc1nc(Cl)nc2c1ncn2C1C(O)C(O)C2(CO)CC12 10.1021/jm020211+
11743031 29825 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 423 8 3 10 -0.7 CCCCn1c(=O)c2c(ncn2[C@@H]2O[C@H](C(=O)NC)[C@@H](O)[C@H]2O)n(CCCC)c1=O 10.1021/jm020211+
CHEMBL138746 29825 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 423 8 3 10 -0.7 CCCCn1c(=O)c2c(ncn2[C@@H]2O[C@H](C(=O)NC)[C@@H](O)[C@H]2O)n(CCCC)c1=O 10.1021/jm020211+
118732976 118515 0 None -17 4 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 427 5 3 12 0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N[C@H]5C[C@@H]6CC[C@@H]5C6)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414942 118515 0 None -17 4 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 427 5 3 12 0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N[C@H]5C[C@@H]6CC[C@@H]5C6)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
137643164 158099 0 None -46 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 552 12 5 11 2.6 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cccs2)c1 10.1021/acs.jmedchem.8b00047
CHEMBL4086624 158099 0 None -46 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 552 12 5 11 2.6 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cccs2)c1 10.1021/acs.jmedchem.8b00047
168274691 190537 0 None -457 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 519 7 4 10 1.8 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(Br)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5179726 190537 0 None -457 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 519 7 4 10 1.8 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(Br)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
377 2756 53 None