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Ligand source activities (1 row/activity)

Ligand Receptor Assay information Chemical information
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9975036 15969 0 AA2BR A2B receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as increase in cAMP productionAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as increase in cAMP production
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1cccc(O)c1 10.1021/acs.jmedchem.6b00552
CHEMBL122806 15969 0 AA2BR A2B receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as increase in cAMP productionAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as increase in cAMP production
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1cccc(O)c1 10.1021/acs.jmedchem.6b00552
9975036 15969 0 AA2BR A2B receptor Human 8.0 pEC50 = 8 Functional
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1cccc(O)c1 10.1021/jm049947s
CHEMBL122806 15969 0 AA2BR A2B receptor Human 8.0 pEC50 = 8 Functional
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1cccc(O)c1 10.1021/jm049947s
44423814 141298 0 AA2BR A2B receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 611 9 5 11 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(Br)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL388193 141298 0 AA2BR A2B receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 611 9 5 11 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(Br)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
9869857 66268 3 AA2BR A2B receptor Human 6.0 pEC50 = 6 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL186113 66268 3 AA2BR A2B receptor Human 6.0 pEC50 = 6 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
49870952 58291 0 AA2BR A2B receptor Human 5.0 pEC50 = 5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells by cyclic AMP functional assayAgonist activity at human adenosine A2B receptor expressed in CHO cells by cyclic AMP functional assay
ChEMBL 333 3 3 8 0.9 CCCCC#Cc1nc(N)c2ncn([C@@H]3SC[C@@H](O)[C@H]3O)c2n1 10.1021/ml1001823
CHEMBL1688378 58291 0 AA2BR A2B receptor Human 5.0 pEC50 = 5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells by cyclic AMP functional assayAgonist activity at human adenosine A2B receptor expressed in CHO cells by cyclic AMP functional assay
ChEMBL 333 3 3 8 0.9 CCCCC#Cc1nc(N)c2ncn([C@@H]3SC[C@@H](O)[C@H]3O)c2n1 10.1021/ml1001823
219024 3099 50 AA2BR A2B receptor Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1021/jm4011669
2362 3099 50 AA2BR A2B receptor Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1021/jm4011669
5596 3099 50 AA2BR A2B receptor Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1021/jm4011669
CHEMBL317052 3099 50 AA2BR A2B receptor Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1021/jm4011669
DB06213 3099 50 AA2BR A2B receptor Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1021/jm4011669
9910098 70107 17 AA2BR A2B receptor Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 421 6 4 10 0.3 Nc1nc(OCCc2ccc(Cl)cc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm4011669
CHEMBL1950553 70107 17 AA2BR A2B receptor Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 421 6 4 10 0.3 Nc1nc(OCCc2ccc(Cl)cc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm4011669
10981286 1794 18 AA2BR A2B receptor Human 4.0 pEC50 = 4 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 10.1021/jm0109762
5599 1794 18 AA2BR A2B receptor Human 4.0 pEC50 = 4 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 10.1021/jm0109762
5736 1794 18 AA2BR A2B receptor Human 4.0 pEC50 = 4 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 10.1021/jm0109762
CHEMBL260563 1794 18 AA2BR A2B receptor Human 4.0 pEC50 = 4 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 10.1021/jm0109762
11014608 95672 0 AA2BR A2B receptor Human 4.0 pEC50 = 4 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 389 6 4 9 0.8 CCCCC#Cc1nc(NC(C)C)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
CHEMBL261623 95672 0 AA2BR A2B receptor Human 4.0 pEC50 = 4 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 389 6 4 9 0.8 CCCCC#Cc1nc(NC(C)C)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
10020580 107248 3 AA2BR A2B receptor Human 4.0 pEC50 = 4 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 347 4 4 9 -0.4 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
CHEMBL319387 107248 3 AA2BR A2B receptor Human 4.0 pEC50 = 4 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 347 4 4 9 -0.4 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
11112381 158616 0 AA2BR A2B receptor Human 4.0 pEC50 = 4 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL410115 158616 0 AA2BR A2B receptor Human 4.0 pEC50 = 4 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
10970819 167997 0 AA2BR A2B receptor Human 4.0 pEC50 = 4 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 375 6 4 9 0.4 CCCCC#Cc1nc(NCC)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
CHEMBL437842 167997 0 AA2BR A2B receptor Human 4.0 pEC50 = 4 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 375 6 4 9 0.4 CCCCC#Cc1nc(NCC)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
11068963 191711 1 AA2BR A2B receptor Human 4.0 pEC50 = 4 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 381 3 4 9 -0.1 CNc1nc(C#Cc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL574597 191711 1 AA2BR A2B receptor Human 4.0 pEC50 = 4 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 381 3 4 9 -0.1 CNc1nc(C#Cc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
118732976 117767 0 AA2BR A2B receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 427 5 3 12 0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N[C@H]5C[C@@H]6CC[C@@H]5C6)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414942 117767 0 AA2BR A2B receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of 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
377 2590 39 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm049947s
425 2590 39 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm049947s
448222 2590 39 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm049947s
CHEMBL464859 2590 39 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm049947s
44423816 84556 0 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 601 9 5 11 2.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccccc5C(F)(F)F)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL225579 84556 0 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 601 9 5 11 2.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccccc5C(F)(F)F)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
16203542 84536 0 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 504 6 5 10 0.9 Nc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL225459 84536 0 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 504 6 5 10 0.9 Nc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
145965471 163352 0 AA2BR A2B receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 376 6 2 7 3.5 CCOc1ccc(-c2c(C#N)c(N)nc(SCc3ncc[nH]3)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4210592 163352 0 AA2BR A2B receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 376 6 2 7 3.5 CCOc1ccc(-c2c(C#N)c(N)nc(SCc3ncc[nH]3)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
377 2590 39 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
425 2590 39 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
448222 2590 39 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
CHEMBL464859 2590 39 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
137659441 158275 0 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 441 6 3 12 0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4097468 158275 0 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity 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
9932840 77307 0 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#CC(O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
CHEMBL2094083 77307 0 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#CC(O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
123683 2931 50 AA2BR A2B receptor Human 5.0 pEC50 = 5.0 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
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/jm9804984
422 2931 50 AA2BR A2B receptor Human 5.0 pEC50 = 5.0 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
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/jm9804984
CHEMBL119709 2931 50 AA2BR A2B receptor Human 5.0 pEC50 = 5.0 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
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/jm9804984
DB05511 2931 50 AA2BR A2B receptor Human 5.0 pEC50 = 5.0 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
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/jm9804984
118732981 117772 0 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 495 5 3 12 2.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414947 117772 0 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of 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
11352497 122192 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 498 8 6 15 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(O)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL360837 122192 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 498 8 6 15 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(O)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
118732975 117766 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414941 117766 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of 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
132991435 179928 0 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Functional
Irreversible agonist activity at human adenosine A2B 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 A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 558 8 5 12 0.8 O=C(NCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccc(S(=O)(=O)F)cc1 10.1021/acs.jmedchem.6b01561
CHEMBL4756472 179928 0 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Functional
Irreversible agonist activity at human adenosine A2B 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 A2B 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
57388054 74894 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 607 12 5 10 3.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042305 74894 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 607 12 5 10 3.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
135543624 15950 16 AA2BR A2B receptor Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccc(O)cc1 10.1021/jm049947s
CHEMBL122622 15950 16 AA2BR A2B receptor Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccc(O)cc1 10.1021/jm049947s
44423813 167911 0 AA2BR A2B receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 567 9 5 11 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(Cl)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL437168 167911 0 AA2BR A2B receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 567 9 5 11 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(Cl)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
145974358 163665 0 AA2BR A2B receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 455 8 2 7 4.3 N#Cc1c(N)nc(SCc2cccc(C(N)=O)c2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4214347 163665 0 AA2BR A2B receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 455 8 2 7 4.3 N#Cc1c(N)nc(SCc2cccc(C(N)=O)c2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
57387596 74900 0 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 492 7 4 9 1.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042311 74900 0 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 492 7 4 9 1.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
11386951 66323 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 527 9 5 16 -0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc([N+](=O)[O-])cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL186403 66323 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 527 9 5 16 -0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc([N+](=O)[O-])cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
57385043 74899 0 AA2BR A2B receptor Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 810 18 6 13 6.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)CCCC[C@H]5CCSS5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042310 74899 0 AA2BR A2B receptor Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 810 18 6 13 6.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)CCCC[C@H]5CCSS5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
76329266 105343 0 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 399 5 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133160 105343 0 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B 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
16203665 135892 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 456 7 5 11 0.1 COc1ccc2[nH]cc(CCOc3nc(N)c4ncn([C@@H]5O[C@H](CO)[C@@H](O)[C@H]5O)c4n3)c2c1 10.1021/jm061278q
CHEMBL374028 135892 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 456 7 5 11 0.1 COc1ccc2[nH]cc(CCOc3nc(N)c4ncn([C@@H]5O[C@H](CO)[C@@H](O)[C@H]5O)c4n3)c2c1 10.1021/jm061278q
76311197 105339 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 365 6 5 10 -1.0 CCCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
CHEMBL3133156 105339 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B 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
57387824 74888 0 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 442 7 6 11 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(N)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042299 74888 0 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 442 7 6 11 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(N)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
16203542 84536 0 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 504 6 5 10 0.9 Nc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL225459 84536 0 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 504 6 5 10 0.9 Nc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
137651756 156669 0 AA2BR A2B receptor Human 4.9 pEC50 = 4.9 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATPAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATP
ChEMBL 355 4 3 9 -0.1 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(N[C@@H]4CCOC4)ncnc32)[C@@H]1O 10.1021/acs.jmedchem.7b01399
CHEMBL4079464 156669 0 AA2BR A2B receptor Human 4.9 pEC50 = 4.9 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATPAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATP
ChEMBL 355 4 3 9 -0.1 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(N[C@@H]4CCOC4)ncnc32)[C@@H]1O 10.1021/acs.jmedchem.7b01399
137657841 158744 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4102750 158744 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity 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
9869857 66268 3 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm4011669
CHEMBL186113 66268 3 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm4011669
11352497 122192 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 498 8 6 15 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(O)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL360837 122192 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 498 8 6 15 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(O)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
11157262 122864 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 560 8 5 14 0.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Br)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL361925 122864 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 560 8 5 14 0.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Br)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
71459958 78573 0 AA2BR A2B receptor Human 4.9 pEC50 = 4.9 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 336 3 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=S)NC2CC2)[C@@H](O)[C@H]1O 10.1021/jm9804984
CHEMBL2113421 78573 0 AA2BR A2B receptor Human 4.9 pEC50 = 4.9 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 336 3 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=S)NC2CC2)[C@@H](O)[C@H]1O 10.1021/jm9804984
118732978 117769 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 403 5 3 13 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414944 117769 0 AA2BR A2B receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of 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
145977469 163167 0 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 402 7 2 7 3.9 N#Cc1c(N)nc(SCc2cnc[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4208189 163167 0 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 402 7 2 7 3.9 N#Cc1c(N)nc(SCc2cnc[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
57387594 74893 0 AA2BR A2B receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 506 8 4 9 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042304 74893 0 AA2BR A2B receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 506 8 4 9 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
377 2590 39 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based 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.8b01662
425 2590 39 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based 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.8b01662
448222 2590 39 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based 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.8b01662
CHEMBL464859 2590 39 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based 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.8b01662
377 2590 39 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
425 2590 39 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
448222 2590 39 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
CHEMBL464859 2590 39 AA2BR A2B receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
24827417 95660 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 729 12 6 12 4.1 O=C(COc1ccc(Nc2nc(OCCc3c[nH]c4cc(Br)ccc34)nc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)Nc1ccccc1 10.1021/jm701442d
CHEMBL261546 95660 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 729 12 6 12 4.1 O=C(COc1ccc(Nc2nc(OCCc3c[nH]c4cc(Br)ccc34)nc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)Nc1ccccc1 10.1021/jm701442d
9954747 136323 7 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 437 6 4 10 0.8 Nc1nc(OCCc2ccc3ccccc3c2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL374760 136323 7 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 437 6 4 10 0.8 Nc1nc(OCCc2ccc3ccccc3c2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
149362 74887 4 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 427 7 5 10 -0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042298 74887 4 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 427 7 5 10 -0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
137656845 158971 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 800 15 5 12 6.5 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccc(-c2scc(C(=O)c3ccccc3)c2-c2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.8b00047
CHEMBL4105473 158971 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 800 15 5 12 6.5 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccc(-c2scc(C(=O)c3ccccc3)c2-c2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.8b00047
377 2590 39 AA2BR A2B receptor Human 4.8 pEC50 = 4.8 Binding
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene 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.5b01402
425 2590 39 AA2BR A2B receptor Human 4.8 pEC50 = 4.8 Binding
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene 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.5b01402
448222 2590 39 AA2BR A2B receptor Human 4.8 pEC50 = 4.8 Binding
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene 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.5b01402
CHEMBL464859 2590 39 AA2BR A2B receptor Human 4.8 pEC50 = 4.8 Binding
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene 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.5b01402
118732972 117763 0 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 347 4 3 12 -1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414938 117763 0 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of 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
57384287 74890 0 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 658 9 6 11 3.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)cc(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042301 74890 0 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 658 9 6 11 3.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)cc(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
11776764 7636 6 AA2BR A2B receptor Human 4.8 pEC50 = 4.8 Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 248 2 1 8 1.1 CSc1nc(N)n2nc(-c3ccco3)nc2n1 10.1016/j.bmc.2010.02.039
CHEMBL1090123 7636 6 AA2BR A2B receptor Human 4.8 pEC50 = 4.8 Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 248 2 1 8 1.1 CSc1nc(N)n2nc(-c3ccco3)nc2n1 10.1016/j.bmc.2010.02.039
44423812 84710 0 AA2BR A2B receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 551 9 5 11 1.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(F)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226194 84710 0 AA2BR A2B receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 551 9 5 11 1.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(F)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
377 2590 39 AA2BR A2B receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
425 2590 39 AA2BR A2B receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
448222 2590 39 AA2BR A2B receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
CHEMBL464859 2590 39 AA2BR A2B receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 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
44423824 136795 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 547 10 5 11 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NCc5ccccc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL375501 136795 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 547 10 5 11 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NCc5ccccc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
377 2590 39 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter methodAgonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter method
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.7b00457
425 2590 39 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter methodAgonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter method
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.7b00457
448222 2590 39 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter methodAgonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter method
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.7b00457
CHEMBL464859 2590 39 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter methodAgonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter method
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.7b00457
377 2590 39 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmc.2007.01.055
425 2590 39 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmc.2007.01.055
448222 2590 39 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmc.2007.01.055
CHEMBL464859 2590 39 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmc.2007.01.055
137649841 156613 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 656 14 5 12 3.8 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cc(C(=O)c3ccccc3)cs2)c1 10.1021/acs.jmedchem.8b00047
CHEMBL4078771 156613 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 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
76311194 105327 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 525 5 5 10 -0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133078 105327 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B 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
76329263 105328 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 413 6 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133079 105328 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B 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
76332919 105336 0 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 323 3 5 10 -2.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133153 105336 0 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B 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
76336525 105337 0 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 337 4 5 10 -1.8 CCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
CHEMBL3133154 105337 0 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B 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
44423821 141393 0 AA2BR A2B receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 589 9 5 11 2.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(C(C)(C)C)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL388405 141393 0 AA2BR A2B receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 589 9 5 11 2.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(C(C)(C)C)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
72141742 161751 2 AA2BR A2B receptor Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 302 5 1 7 0.0 O=C(CN1CCOC(Cn2cncn2)C1)Nc1cccnc1 10.1016/j.ejmech.2017.05.035
CHEMBL4168653 161751 2 AA2BR A2B receptor Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 302 5 1 7 0.0 O=C(CN1CCOC(Cn2cncn2)C1)Nc1cccnc1 10.1016/j.ejmech.2017.05.035
377 2590 39 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061170a
425 2590 39 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061170a
448222 2590 39 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061170a
CHEMBL464859 2590 39 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061170a
14157150 78583 0 AA2BR A2B receptor Human 4.8 pEC50 = 4.8 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 324 3 4 9 -1.0 CCNC(=S)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
CHEMBL2113431 78583 0 AA2BR A2B receptor Human 4.8 pEC50 = 4.8 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 324 3 4 9 -1.0 CCNC(=S)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
21893339 163087 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 366 5 3 7 1.6 CC(=O)Nc1ccc(-c2c(C#N)c(N)nc(SCC(N)=O)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4207286 163087 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 366 5 3 7 1.6 CC(=O)Nc1ccc(-c2c(C#N)c(N)nc(SCC(N)=O)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
137636099 155016 0 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 535 6 3 12 1.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4059961 155016 0 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 535 6 3 12 1.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
414 3180 23 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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/jm061278q
93205 3180 23 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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/jm061278q
CHEMBL139000 3180 23 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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/jm061278q
46885472 8068 0 AA2BR A2B receptor Human 4.8 pEC50 = 4.8 Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 381 4 2 8 3.5 CSc1nc(NC(=O)Nc2ccc(C)cc2)n2nc(-c3ccco3)nc2n1 10.1016/j.bmc.2010.02.039
CHEMBL1092869 8068 0 AA2BR A2B receptor Human 4.8 pEC50 = 4.8 Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 381 4 2 8 3.5 CSc1nc(NC(=O)Nc2ccc(C)cc2)n2nc(-c3ccco3)nc2n1 10.1016/j.bmc.2010.02.039
11395785 183918 0 AA2BR A2B receptor Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter methodAgonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter method
ChEMBL 410 5 4 9 0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.7b00457
CHEMBL487754 183918 0 AA2BR A2B receptor Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter methodAgonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter method
ChEMBL 410 5 4 9 0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.7b00457
137643164 157279 0 AA2BR A2B receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 552 12 5 11 2.6 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cccs2)c1 10.1021/acs.jmedchem.8b00047
CHEMBL4086624 157279 0 AA2BR A2B receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 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
70682890 77223 2 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL2092788 77223 2 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
46885471 8067 0 AA2BR A2B receptor Human 4.8 pEC50 = 4.8 Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 367 4 2 8 3.1 CSc1nc(NC(=O)Nc2ccccc2)n2nc(-c3ccco3)nc2n1 10.1016/j.bmc.2010.02.039
CHEMBL1092868 8067 0 AA2BR A2B receptor Human 4.8 pEC50 = 4.8 Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 367 4 2 8 3.1 CSc1nc(NC(=O)Nc2ccccc2)n2nc(-c3ccco3)nc2n1 10.1016/j.bmc.2010.02.039
24827415 158601 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 519 7 6 11 0.6 NNc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm701442d
CHEMBL410104 158601 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 519 7 6 11 0.6 NNc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm701442d
16103168 82569 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 481 6 5 11 0.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc(C)s4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL218585 82569 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 481 6 5 11 0.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc(C)s4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
44423837 84587 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 581 10 5 11 1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NCc5ccccc5)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL225944 84587 0 AA2BR A2B receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 581 10 5 11 1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NCc5ccccc5)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
44420921 84499 0 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 393 6 4 11 -0.3 Nc1nc(OCCc2cccs2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL225233 84499 0 AA2BR A2B receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 393 6 4 11 -0.3 Nc1nc(OCCc2cccs2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
137649083 156491 0 AA2BR A2B receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 849 15 6 13 6.7 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3nc(Cl)nc4c3ncn4[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
CHEMBL4077152 156491 0 AA2BR A2B receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 849 15 6 13 6.7 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3nc(Cl)nc4c3ncn4[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
145968949 163993 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 409 8 3 8 2.0 N#Cc1c(N)nc(SCC(=O)NCO)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4218613 163993 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 409 8 3 8 2.0 N#Cc1c(N)nc(SCC(=O)NCO)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
16202726 84051 0 AA2BR A2B receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 552 6 5 10 0.7 Nc1nc(OCCc2c[nH]c3ccc(I)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL222748 84051 0 AA2BR A2B receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 552 6 5 10 0.7 Nc1nc(OCCc2c[nH]c3ccc(I)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
11174953 16397 0 AA2BR A2B receptor Human 7.7 pEC50 = 7.7 Functional
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 332 4 2 6 3.1 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccccc1 10.1021/jm049947s
CHEMBL124345 16397 0 AA2BR A2B receptor Human 7.7 pEC50 = 7.7 Functional
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 332 4 2 6 3.1 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccccc1 10.1021/jm049947s
137650899 156387 0 AA2BR A2B receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 413 6 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4076003 156387 0 AA2BR A2B receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity 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
137657926 158942 0 AA2BR A2B receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 421 6 3 12 0.3 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4105164 158942 0 AA2BR A2B receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity 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
76322076 105329 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 489 7 5 10 1.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133080 105329 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B 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
76318403 105340 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 363 4 5 10 -1.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133157 105340 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B 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
57387337 74886 0 AA2BR A2B receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 326 3 4 9 -1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042297 74886 0 AA2BR A2B receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 326 3 4 9 -1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
16103185 165217 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 467 6 5 11 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4cccs4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL425643 165217 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 467 6 5 11 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4cccs4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
70689262 77386 0 AA2BR A2B receptor Human 5.7 pEC50 = 5.7 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL2096798 77386 0 AA2BR A2B receptor Human 5.7 pEC50 = 5.7 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
137656913 158827 0 AA2BR A2B receptor Human 4.7 pEC50 = 4.7 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATPAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATP
ChEMBL 389 4 3 9 0.5 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(N[C@@H]4CCOC4)nc(Cl)nc32)[C@@H]1O 10.1021/acs.jmedchem.7b01399
CHEMBL4103712 158827 0 AA2BR A2B receptor Human 4.7 pEC50 = 4.7 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATPAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATP
ChEMBL 389 4 3 9 0.5 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(N[C@@H]4CCOC4)nc(Cl)nc32)[C@@H]1O 10.1021/acs.jmedchem.7b01399
46885518 7535 0 AA2BR A2B receptor Human 4.7 pEC50 = 4.7 Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 427 5 2 8 4.5 Cc1ccc(NC(=O)Nc2nc(Oc3ccccc3)nc3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2010.02.039
CHEMBL1089441 7535 0 AA2BR A2B receptor Human 4.7 pEC50 = 4.7 Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 427 5 2 8 4.5 Cc1ccc(NC(=O)Nc2nc(Oc3ccccc3)nc3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2010.02.039
16109359 160952 0 AA2BR A2B receptor Human 5.7 pEC50 = 5.7 Functional
Activity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells
ChEMBL 924 21 6 14 4.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCNC(=O)CCCCCNC(=O)COc4ccc(/C=C/C5=[N+]6C(=Cc7ccc(-c8cccs8)n7[B-]6(F)F)C=C5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061279i
CHEMBL414055 160952 0 AA2BR A2B receptor Human 5.7 pEC50 = 5.7 Functional
Activity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2B receptor assessed as stimulation of [3H]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
16103167 82734 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 451 6 5 11 -0.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccco4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL219413 82734 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 451 6 5 11 -0.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccco4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
145977114 162946 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 367 6 2 7 2.3 CCOc1ccc(-c2c(C#N)c(N)nc(SCC(=O)NC)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4205729 162946 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 367 6 2 7 2.3 CCOc1ccc(-c2c(C#N)c(N)nc(SCC(=O)NC)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
137650221 156439 0 AA2BR A2B receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 463 6 3 13 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4076561 156439 0 AA2BR A2B receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity 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
16202727 84078 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 460 6 5 10 0.8 Nc1nc(OCCc2c[nH]c3cc(Cl)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL222907 84078 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 460 6 5 10 0.8 Nc1nc(OCCc2c[nH]c3cc(Cl)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
16202725 84001 0 AA2BR A2B receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 460 6 5 10 0.8 Nc1nc(OCCc2c[nH]c3ccc(Cl)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL222442 84001 0 AA2BR A2B receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 460 6 5 10 0.8 Nc1nc(OCCc2c[nH]c3ccc(Cl)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
23757284 84466 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#C[C@@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm061278q
CHEMBL224874 84466 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#C[C@@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm061278q
23757284 84466 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#C[C@@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
CHEMBL224874 84466 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#C[C@@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
118732974 117765 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL3414940 117765 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity 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
137650918 156429 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 671 14 6 13 3.4 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)cc1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4076495 156429 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 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
132991434 179092 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Irreversible agonist activity at human adenosine A2B 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 A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 564 8 6 12 2.4 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccc(CNC(=S)Nc5ccc(N=C=S)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.6b01561
CHEMBL4746617 179092 0 AA2BR A2B receptor Human 6.7 pEC50 = 6.7 Functional
Irreversible agonist activity at human adenosine A2B 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 A2B 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
137651747 156664 0 AA2BR A2B receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4079433 156664 0 AA2BR A2B receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity 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
16103178 159833 0 AA2BR A2B receptor Human 6.6 pEC50 = 6.6 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 431 6 5 11 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc(C)o4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL411332 159833 0 AA2BR A2B receptor Human 6.6 pEC50 = 6.6 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 431 6 5 11 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc(C)o4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
57384543 74897 0 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 838 14 6 11 7.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)cc(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042308 74897 0 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 838 14 6 11 7.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)cc(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
449 2484 38 AA2BR A2B receptor Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2017.05.035
453 2484 38 AA2BR A2B receptor Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2017.05.035
6603931 2484 38 AA2BR A2B receptor Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2017.05.035
CHEMBL273807 2484 38 AA2BR A2B receptor Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2017.05.035
136015813 161539 4 AA2BR A2B receptor Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 322 6 2 7 2.6 CCCc1cc(O)nc(SC(C)C(=O)Nc2cc(C)no2)n1 10.1016/j.ejmech.2017.05.035
CHEMBL4165135 161539 4 AA2BR A2B receptor Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 322 6 2 7 2.6 CCCc1cc(O)nc(SC(C)C(=O)Nc2cc(C)no2)n1 10.1016/j.ejmech.2017.05.035
137648928 156588 0 AA2BR A2B receptor Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 549 6 3 12 1.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(I)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4078479 156588 0 AA2BR A2B receptor Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity 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
2844 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
60961 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
90 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
CHEMBL477 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
DB00640 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2B 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
137661132 158351 0 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 491 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4098377 158351 0 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity 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
44423825 84738 0 AA2BR A2B receptor Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 577 11 5 12 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NCc5ccc(OC)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226304 84738 0 AA2BR A2B receptor Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 577 11 5 12 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NCc5ccc(OC)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
377 2590 39 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Functional
Receptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptorReceptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/s0960-894x(01)00347-x
425 2590 39 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Functional
Receptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptorReceptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/s0960-894x(01)00347-x
448222 2590 39 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Functional
Receptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptorReceptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/s0960-894x(01)00347-x
CHEMBL464859 2590 39 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Functional
Receptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptorReceptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/s0960-894x(01)00347-x
13830108 77244 1 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL2092941 77244 1 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
23900137 95081 0 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#C[C@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
CHEMBL258534 95081 0 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#C[C@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
2844 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Binding
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
60961 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Binding
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
90 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Binding
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
CHEMBL477 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Binding
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
DB00640 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Binding
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
2844 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cellsAgonist activity at human adenosine A2B receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
60961 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cellsAgonist activity at human adenosine A2B receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
90 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cellsAgonist activity at human adenosine A2B receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
CHEMBL477 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cellsAgonist activity at human adenosine A2B receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
DB00640 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cellsAgonist activity at human adenosine A2B receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
2844 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
60961 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
90 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
CHEMBL477 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
DB00640 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
2844 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
60961 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
90 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
CHEMBL477 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
DB00640 269 95 AA2BR A2B receptor Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b 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 2590 39 AA2BR A2B receptor Human 6.6 pEC50 = 6.6 Functional
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
425 2590 39 AA2BR A2B receptor Human 6.6 pEC50 = 6.6 Functional
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
448222 2590 39 AA2BR A2B receptor Human 6.6 pEC50 = 6.6 Functional
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
CHEMBL464859 2590 39 AA2BR A2B receptor Human 6.6 pEC50 = 6.6 Functional
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
76325694 105342 0 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 391 4 5 10 -0.5 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133159 105342 0 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B 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
57388055 74895 0 AA2BR A2B receptor Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 622 12 6 11 3.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(N)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042306 74895 0 AA2BR A2B receptor Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 622 12 6 11 3.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(N)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
137641990 157257 0 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 447 6 3 13 0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4086325 157257 0 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity 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
16204411 84086 0 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 376 6 5 10 -1.0 Nc1nc(OCCc2cc[nH]c2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL222945 84086 0 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 376 6 5 10 -1.0 Nc1nc(OCCc2cc[nH]c2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
11026001 95640 0 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL261453 95640 0 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
69427076 77221 0 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL2092786 77221 0 AA2BR A2B receptor Human 5.6 pEC50 = 5.6 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
16103165 82733 0 AA2BR A2B receptor Human 6.6 pEC50 = 6.6 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 447 6 5 11 -0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc(C)s4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL219411 82733 0 AA2BR A2B receptor Human 6.6 pEC50 = 6.6 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 447 6 5 11 -0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc(C)s4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
137639588 156070 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccccc2C(=O)NCCCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4072009 156070 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 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
24827289 166597 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 613 9 6 12 1.7 O=C(NNc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccco1 10.1021/jm701442d
CHEMBL429684 166597 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 613 9 6 12 1.7 O=C(NNc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccco1 10.1021/jm701442d
3044933 16121 4 AA2BR A2B receptor Human 4.5 pEC50 = 4.5 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 322 4 4 9 -1.4 CCCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
CHEMBL1235128 16121 4 AA2BR A2B receptor Human 4.5 pEC50 = 4.5 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 322 4 4 9 -1.4 CCCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
57388056 74896 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 685 12 5 10 4.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(Br)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042307 74896 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 685 12 5 10 4.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(Br)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
16203429 84146 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 426 6 5 10 0.1 Nc1nc(OCCc2c[nH]c3ccccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL223366 84146 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 426 6 5 10 0.1 Nc1nc(OCCc2c[nH]c3ccccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
377 2590 39 AA2BR A2B receptor Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
425 2590 39 AA2BR A2B receptor Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
448222 2590 39 AA2BR A2B receptor Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
CHEMBL464859 2590 39 AA2BR A2B receptor Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B 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
44423815 84722 0 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 659 9 5 11 1.9 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(I)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226242 84722 0 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 659 9 5 11 1.9 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(I)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
44423822 84737 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 618 10 5 13 1.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(N6CCOCC6)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226303 84737 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 618 10 5 13 1.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(N6CCOCC6)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
70689262 77386 0 AA2BR A2B receptor Human 5.5 pEC50 = 5.5 Functional
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL2096798 77386 0 AA2BR A2B receptor Human 5.5 pEC50 = 5.5 Functional
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
71456259 78587 0 AA2BR A2B receptor Human 4.5 pEC50 = 4.5 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 376 4 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCC(F)(F)F)[C@@H](O)[C@H]1O 10.1021/jm9804984
CHEMBL2113435 78587 0 AA2BR A2B receptor Human 4.5 pEC50 = 4.5 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 376 4 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCC(F)(F)F)[C@@H](O)[C@H]1O 10.1021/jm9804984
44423838 141477 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 573 9 5 11 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NC5CCCCC5)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL388505 141477 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 573 9 5 11 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NC5CCCCC5)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
11717831 556 30 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 379 7 2 7 2.4 N#Cc1c(N)nc(c(c1c1ccc(cc1)OCC1CC1)C#N)SCC(=O)N 10.1016/j.ejmech.2018.02.081
3289 556 30 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 379 7 2 7 2.4 N#Cc1c(N)nc(c(c1c1ccc(cc1)OCC1CC1)C#N)SCC(=O)N 10.1016/j.ejmech.2018.02.081
CHEMBL4202825 556 30 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 379 7 2 7 2.4 N#Cc1c(N)nc(c(c1c1ccc(cc1)OCC1CC1)C#N)SCC(=O)N 10.1016/j.ejmech.2018.02.081
123683 2931 50 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
422 2931 50 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
CHEMBL119709 2931 50 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
DB05511 2931 50 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B 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
377 2590 39 AA2BR A2B receptor Human 5.5 pEC50 = 5.5 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9804984
425 2590 39 AA2BR A2B receptor Human 5.5 pEC50 = 5.5 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9804984
448222 2590 39 AA2BR A2B receptor Human 5.5 pEC50 = 5.5 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9804984
CHEMBL464859 2590 39 AA2BR A2B receptor Human 5.5 pEC50 = 5.5 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9804984
44423826 84740 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 539 9 5 11 1.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NC5CCCCC5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226307 84740 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 539 9 5 11 1.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NC5CCCCC5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
118732979 117770 0 AA2BR A2B receptor Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 437 5 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414945 117770 0 AA2BR A2B receptor Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of 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
377 2590 39 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Binding
Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
425 2590 39 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Binding
Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
448222 2590 39 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Binding
Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
CHEMBL464859 2590 39 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Binding
Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
44423823 141395 0 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 534 9 5 12 0.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccncc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL388406 141395 0 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 534 9 5 12 0.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccncc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
44423817 84723 0 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 563 10 5 12 1.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(OC)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226243 84723 0 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 563 10 5 12 1.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(OC)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
10688700 76341 0 AA2BR A2B receptor Human 4.5 pEC50 = 4.5 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 342 4 4 9 -1.6 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCCl)[C@@H](O)[C@H]1O 10.1021/jm9804984
CHEMBL2070399 76341 0 AA2BR A2B receptor Human 4.5 pEC50 = 4.5 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 342 4 4 9 -1.6 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCCl)[C@@H](O)[C@H]1O 10.1021/jm9804984
16203668 95653 0 AA2BR A2B receptor Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 454 8 5 10 1.0 CCNc1nc(OCCc2c[nH]c3ccccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL261515 95653 0 AA2BR A2B receptor Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 454 8 5 10 1.0 CCNc1nc(OCCc2c[nH]c3ccccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
377 2590 39 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by 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/jm4011669
425 2590 39 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by 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/jm4011669
448222 2590 39 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by 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/jm4011669
CHEMBL464859 2590 39 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by 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/jm4011669
10449535 76343 0 AA2BR A2B receptor Human 4.5 pEC50 = 4.5 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 334 3 4 9 -1.3 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CCC2)[C@@H](O)[C@H]1O 10.1021/jm9804984
CHEMBL2070507 76343 0 AA2BR A2B receptor Human 4.5 pEC50 = 4.5 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 334 3 4 9 -1.3 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CCC2)[C@@H](O)[C@H]1O 10.1021/jm9804984
145967103 163313 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 376 6 2 7 3.5 CCOc1ccc(-c2c(C#N)c(N)nc(SCc3ccn[nH]3)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4210096 163313 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 376 6 2 7 3.5 CCOc1ccc(-c2c(C#N)c(N)nc(SCc3ccn[nH]3)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
127043828 140324 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Antagonist activity at human adenosine receptor A2b expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation measured as NECA EC50 at 2 uM incubated for 15 mins in presence of [3H]cAMP by liquid scintillation counting (Rvb = 73 nM)Antagonist activity at human adenosine receptor A2b expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation measured as NECA EC50 at 2 uM incubated for 15 mins in presence of [3H]cAMP by liquid scintillation counting (Rvb = 73 nM)
ChEMBL 538 15 0 9 4.1 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCCN(CC)CC)cc2)n(CCCC)c1=O 10.1016/j.bmc.2016.07.028
CHEMBL3827331 140324 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Antagonist activity at human adenosine receptor A2b expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation measured as NECA EC50 at 2 uM incubated for 15 mins in presence of [3H]cAMP by liquid scintillation counting (Rvb = 73 nM)Antagonist activity at human adenosine receptor A2b expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation measured as NECA EC50 at 2 uM incubated for 15 mins in presence of [3H]cAMP by liquid scintillation counting (Rvb = 73 nM)
ChEMBL 538 15 0 9 4.1 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCCN(CC)CC)cc2)n(CCCC)c1=O 10.1016/j.bmc.2016.07.028
15729982 7637 0 AA2BR A2B receptor Human 4.5 pEC50 = 4.5 Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 245 2 1 8 0.4 CN(C)c1nc(N)n2nc(-c3ccco3)nc2n1 10.1016/j.bmc.2010.02.039
CHEMBL1090124 7637 0 AA2BR A2B receptor Human 4.5 pEC50 = 4.5 Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 245 2 1 8 0.4 CN(C)c1nc(N)n2nc(-c3ccco3)nc2n1 10.1016/j.bmc.2010.02.039
11256992 17576 0 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 362 5 2 7 3.1 COc1cccc(-c2c(C#N)c(N)nc(SCc3ncc[nH]3)c2C#N)c1 10.1021/jm049947s
CHEMBL125979 17576 0 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 362 5 2 7 3.1 COc1cccc(-c2c(C#N)c(N)nc(SCc3ncc[nH]3)c2C#N)c1 10.1021/jm049947s
51112335 161410 6 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 311 4 2 6 2.4 Cc1cc(NC(=O)CNc2ccc3c(c2)OC(F)(F)O3)on1 10.1016/j.ejmech.2017.05.035
CHEMBL4163380 161410 6 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 311 4 2 6 2.4 Cc1cc(NC(=O)CNc2ccc3c(c2)OC(F)(F)O3)on1 10.1016/j.ejmech.2017.05.035
56783276 161646 5 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 319 6 1 7 1.6 CC(C)c1noc(OCC(=O)NCc2ccc3c(c2)OCO3)n1 10.1016/j.ejmech.2017.05.035
CHEMBL4167064 161646 5 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 319 6 1 7 1.6 CC(C)c1noc(OCC(=O)NCc2ccc3c(c2)OCO3)n1 10.1016/j.ejmech.2017.05.035
16103186 158024 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 481 6 5 11 0.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4sccc4C)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL409483 158024 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 481 6 5 11 0.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4sccc4C)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
3071852 8131 3 AA2BR A2B receptor Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 294 3 1 8 2.2 Nc1nc(Oc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmc.2010.02.039
CHEMBL1093313 8131 3 AA2BR A2B receptor Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 294 3 1 8 2.2 Nc1nc(Oc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmc.2010.02.039
145965011 163376 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 470 8 1 8 4.9 COC(=O)c1cccc(CSc2nc(N)c(C#N)c(-c3ccc(OCC4CC4)cc3)c2C#N)c1 10.1016/j.ejmech.2018.02.081
CHEMBL4210852 163376 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 470 8 1 8 4.9 COC(=O)c1cccc(CSc2nc(N)c(C#N)c(-c3ccc(OCC4CC4)cc3)c2C#N)c1 10.1016/j.ejmech.2018.02.081
118732971 117761 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 333 3 3 12 -1.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414936 117761 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 333 3 3 12 -1.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
131432 136269 7 AA2BR A2B receptor Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 387 6 4 10 -0.4 Nc1nc(OCCc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL374685 136269 7 AA2BR A2B receptor Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 387 6 4 10 -0.4 Nc1nc(OCCc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
137661505 158670 0 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4101850 158670 0 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 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
44423820 141299 0 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 577 9 5 13 1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc6c(c5)OCO6)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL388194 141299 0 AA2BR A2B receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 577 9 5 13 1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc6c(c5)OCO6)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
118732973 117764 0 AA2BR A2B receptor Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 381 4 3 12 -0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414939 117764 0 AA2BR A2B receptor Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of 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
57387825 74889 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 505 7 5 10 0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(Br)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042300 74889 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 505 7 5 10 0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(Br)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
16103187 82648 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 450 6 6 10 -0.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc[nH]4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL218989 82648 0 AA2BR A2B receptor Human 6.5 pEC50 = 6.5 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 450 6 6 10 -0.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc[nH]4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
44423828 84739 0 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 597 10 5 12 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(OC)cc5)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226305 84739 0 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 597 10 5 12 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(OC)cc5)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
377 2590 39 AA2BR A2B receptor Human 5.4 pEC50 = 5.4 Functional
Activity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
425 2590 39 AA2BR A2B receptor Human 5.4 pEC50 = 5.4 Functional
Activity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
448222 2590 39 AA2BR A2B receptor Human 5.4 pEC50 = 5.4 Functional
Activity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
CHEMBL464859 2590 39 AA2BR A2B receptor Human 5.4 pEC50 = 5.4 Functional
Activity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2B receptor assessed as stimulation of [3H]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
16203540 83966 0 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 504 6 5 10 0.9 Nc1nc(OCCc2c[nH]c3ccc(Br)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL222194 83966 0 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 504 6 5 10 0.9 Nc1nc(OCCc2c[nH]c3ccc(Br)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
16103177 82720 0 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 495 6 5 11 -0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc(Br)o4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL219361 82720 0 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 495 6 5 11 -0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc(Br)o4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
21128750 195247 0 AA2BR A2B receptor Human 4.4 pEC50 = 4.4 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 322 3 4 9 -1.4 CC(C)NC(=O)[C@H]1OC(n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
CHEMBL606095 195247 0 AA2BR A2B receptor Human 4.4 pEC50 = 4.4 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 322 3 4 9 -1.4 CC(C)NC(=O)[C@H]1OC(n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
137658761 158358 0 AA2BR A2B receptor Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATPAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATP
ChEMBL 413 4 3 8 2.2 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(Nc4ccc(Cl)cc4F)ncnc32)[C@@H]1O 10.1021/acs.jmedchem.7b01399
CHEMBL4098408 158358 0 AA2BR A2B receptor Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATPAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATP
ChEMBL 413 4 3 8 2.2 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(Nc4ccc(Cl)cc4F)ncnc32)[C@@H]1O 10.1021/acs.jmedchem.7b01399
145975919 163040 0 AA2BR A2B receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 353 6 2 7 2.1 CCOc1ccc(-c2c(C#N)c(N)nc(SCC(N)=O)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4206762 163040 0 AA2BR A2B receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 353 6 2 7 2.1 CCOc1ccc(-c2c(C#N)c(N)nc(SCC(N)=O)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
377 2590 39 AA2BR A2B receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assayAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2009.11.131
425 2590 39 AA2BR A2B receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assayAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2009.11.131
448222 2590 39 AA2BR A2B receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assayAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2009.11.131
CHEMBL464859 2590 39 AA2BR A2B receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assayAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2009.11.131
118734376 117888 0 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 602 10 4 12 1.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCCCc6ccccc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416810 117888 0 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 602 10 4 12 1.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCCCc6ccccc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
3086599 858 30 AA2BR A2B receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
375 858 30 AA2BR A2B receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
424 858 30 AA2BR A2B receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
CHEMBL331372 858 30 AA2BR A2B receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B 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
76336527 105344 0 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 433 5 5 10 0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(Cl)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133161 105344 0 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B 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
57384544 74898 0 AA2BR A2B receptor Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 854 14 7 12 7.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042309 74898 0 AA2BR A2B receptor Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 854 14 7 12 7.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
137647420 156883 0 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 501 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4081876 156883 0 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity 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
44423827 84750 0 AA2BR A2B receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 567 9 5 11 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccccc5)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226356 84750 0 AA2BR A2B receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 567 9 5 11 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccccc5)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
377 2590 39 AA2BR A2B receptor Human 7.4 pEC50 = 7.4 Functional
Irreversible agonist activity at human adenosine A2B 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 A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
425 2590 39 AA2BR A2B receptor Human 7.4 pEC50 = 7.4 Functional
Irreversible agonist activity at human adenosine A2B 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 A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
448222 2590 39 AA2BR A2B receptor Human 7.4 pEC50 = 7.4 Functional
Irreversible agonist activity at human adenosine A2B 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 A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
CHEMBL464859 2590 39 AA2BR A2B receptor Human 7.4 pEC50 = 7.4 Functional
Irreversible agonist activity at human adenosine A2B 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 A2B 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
46885404 7760 0 AA2BR A2B receptor Human 4.4 pEC50 = 4.4 Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 396 6 1 9 2.7 COc1ccc(CC(=O)Nc2nc(SC)nc3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2010.02.039
CHEMBL1090806 7760 0 AA2BR A2B receptor Human 4.4 pEC50 = 4.4 Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 396 6 1 9 2.7 COc1ccc(CC(=O)Nc2nc(SC)nc3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2010.02.039
377 2590 39 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
425 2590 39 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
448222 2590 39 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
CHEMBL464859 2590 39 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
137646655 156809 0 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 711 13 6 12 4.8 Nc1cc(-c2cccc(C(F)(F)F)c2)c(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)s1 10.1021/acs.jmedchem.8b00047
CHEMBL4081224 156809 0 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 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
44423818 84724 0 AA2BR A2B receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 593 11 5 13 1.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(OC)c(OC)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226244 84724 0 AA2BR A2B receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 593 11 5 13 1.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(OC)c(OC)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
16103184 82647 0 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 467 6 5 11 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccsc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL218988 82647 0 AA2BR A2B receptor Human 6.4 pEC50 = 6.4 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 467 6 5 11 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccsc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
3042985 78586 1 AA2BR A2B receptor Human 4.4 pEC50 = 4.4 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 310 3 4 10 -2.3 CONC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
CHEMBL2113434 78586 1 AA2BR A2B receptor Human 4.4 pEC50 = 4.4 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 310 3 4 10 -2.3 CONC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
98567 187370 14 AA2BR A2B receptor Human 4.4 pEC50 = 4.4 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
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/jm9804984
CHEMBL519809 187370 14 AA2BR A2B receptor Human 4.4 pEC50 = 4.4 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
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/jm9804984
16365293 162073 4 AA2BR A2B receptor Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 344 5 2 8 0.6 CC(OC(=O)c1nccnc1N)C(=O)NCc1ccc2c(c1)OCO2 10.1016/j.ejmech.2017.05.035
CHEMBL4173768 162073 4 AA2BR A2B receptor Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 344 5 2 8 0.6 CC(OC(=O)c1nccnc1N)C(=O)NCc1ccc2c(c1)OCO2 10.1016/j.ejmech.2017.05.035
137652475 156331 0 AA2BR A2B receptor Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 829 16 6 13 6.5 Nc1sc(-c2ccc(C(=O)NCCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4075186 156331 0 AA2BR A2B receptor Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 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
10256007 122154 0 AA2BR A2B receptor Human 5.3 pEC50 = 5.3 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 516 8 5 14 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Cl)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL360646 122154 0 AA2BR A2B receptor Human 5.3 pEC50 = 5.3 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 516 8 5 14 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Cl)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
10388920 69248 5 AA2BR A2B receptor Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assayAgonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assay
ChEMBL 447 7 4 9 1.7 OC[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acsmedchemlett.0c00509
CHEMBL193692 69248 5 AA2BR A2B receptor Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assayAgonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assay
ChEMBL 447 7 4 9 1.7 OC[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acsmedchemlett.0c00509
76336526 105338 0 AA2BR A2B receptor Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 351 5 5 10 -1.4 CCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
CHEMBL3133155 105338 0 AA2BR A2B receptor Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B 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
145972065 163718 0 AA2BR A2B receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 403 7 2 8 3.3 N#Cc1c(N)nc(SCc2ncn[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4215091 163718 0 AA2BR A2B receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 403 7 2 8 3.3 N#Cc1c(N)nc(SCc2ncn[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
9869857 66268 3 AA2BR A2B receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assayAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1016/j.bmcl.2009.11.131
CHEMBL186113 66268 3 AA2BR A2B receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assayAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1016/j.bmcl.2009.11.131
2844 269 95 AA2BR A2B receptor Human 4.3 pEC50 = 4.3 Binding
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene 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.5b01402
60961 269 95 AA2BR A2B receptor Human 4.3 pEC50 = 4.3 Binding
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene 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.5b01402
90 269 95 AA2BR A2B receptor Human 4.3 pEC50 = 4.3 Binding
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene 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.5b01402
CHEMBL477 269 95 AA2BR A2B receptor Human 4.3 pEC50 = 4.3 Binding
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene 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.5b01402
DB00640 269 95 AA2BR A2B receptor Human 4.3 pEC50 = 4.3 Binding
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene 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.5b01402
137642153 157546 0 AA2BR A2B receptor Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 429 6 3 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4089741 157546 0 AA2BR A2B receptor Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity 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
44423819 84725 0 AA2BR A2B receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 593 11 5 13 1.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5cc(OC)cc(OC)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226245 84725 0 AA2BR A2B receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 593 11 5 13 1.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5cc(OC)cc(OC)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
118732980 117771 0 AA2BR A2B receptor Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 461 5 3 12 1.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414946 117771 0 AA2BR A2B receptor Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of 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
10403711 95646 19 AA2BR A2B receptor Human 5.3 pEC50 = 5.3 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 320 3 4 9 -1.7 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CC2)[C@@H](O)[C@H]1O 10.1021/jm9804984
CHEMBL261482 95646 19 AA2BR A2B receptor Human 5.3 pEC50 = 5.3 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 320 3 4 9 -1.7 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CC2)[C@@H](O)[C@H]1O 10.1021/jm9804984
44420926 137271 0 AA2BR A2B receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 350 4 6 9 -2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NC(=N)N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061278q
CHEMBL376542 137271 0 AA2BR A2B receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 350 4 6 9 -2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NC(=N)N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061278q
215610 76344 2 AA2BR A2B receptor Human 4.3 pEC50 = 4.3 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 348 3 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CCCC2)[C@@H](O)[C@H]1O 10.1021/jm9804984
CHEMBL2070508 76344 2 AA2BR A2B receptor Human 4.3 pEC50 = 4.3 Functional
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 348 3 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CCCC2)[C@@H](O)[C@H]1O 10.1021/jm9804984
56627882 117762 0 AA2BR A2B receptor Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 367 3 3 12 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414937 117762 0 AA2BR A2B receptor Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of 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
11157262 122864 0 AA2BR A2B receptor Human 6.3 pEC50 = 6.3 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 560 8 5 14 0.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Br)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL361925 122864 0 AA2BR A2B receptor Human 6.3 pEC50 = 6.3 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 560 8 5 14 0.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Br)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
137638080 156021 0 AA2BR A2B receptor Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 457 6 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4071338 156021 0 AA2BR A2B receptor Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity 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
137653409 158213 0 AA2BR A2B receptor Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 567 12 6 12 2.2 Nc1ccc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)s1 10.1021/acs.jmedchem.8b00047
CHEMBL4096796 158213 0 AA2BR A2B receptor Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 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
16103169 82022 0 AA2BR A2B receptor Human 6.2 pEC50 = 6.2 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 481 7 5 11 -0.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)Cc4cccs4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL217952 82022 0 AA2BR A2B receptor Human 6.2 pEC50 = 6.2 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 481 7 5 11 -0.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)Cc4cccs4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
57384288 74891 0 AA2BR A2B receptor Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 674 9 7 12 3.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042302 74891 0 AA2BR A2B receptor Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 674 9 7 12 3.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
118719026 114693 0 AA2BR A2B receptor Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 582 13 4 8 2.1 CC(C)(C)OC(=O)C1CCCN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)OCc1ccccc1 10.1021/jm4011669
CHEMBL3350613 114693 0 AA2BR A2B receptor Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 582 13 4 8 2.1 CC(C)(C)OC(=O)C1CCCN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)OCc1ccccc1 10.1021/jm4011669
70697521 77222 0 AA2BR A2B receptor Human 5.2 pEC50 = 5.2 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL2092787 77222 0 AA2BR A2B receptor Human 5.2 pEC50 = 5.2 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
118719026 114693 0 AA2BR A2B receptor Human 5.2 pEC50 = 5.2 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 582 13 4 8 2.1 CC(C)(C)OC(=O)C1CCCN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)OCc1ccccc1 10.1021/jm0109762
CHEMBL3350613 114693 0 AA2BR A2B receptor Human 5.2 pEC50 = 5.2 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 582 13 4 8 2.1 CC(C)(C)OC(=O)C1CCCN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)OCc1ccccc1 10.1021/jm0109762
137650461 156440 0 AA2BR A2B receptor Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 857 16 6 13 6.4 CC(=O)Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4076565 156440 0 AA2BR A2B receptor Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 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
9978117 157498 0 AA2BR A2B receptor Human 5.2 pEC50 = 5.2 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL408918 157498 0 AA2BR A2B receptor Human 5.2 pEC50 = 5.2 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
137634444 155354 0 AA2BR A2B receptor Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 801 14 6 13 5.7 Nc1sc(-c2ccc(C(=O)NCCCCCNc3ncnc4c3ncn4[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
CHEMBL4063841 155354 0 AA2BR A2B receptor Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 801 14 6 13 5.7 Nc1sc(-c2ccc(C(=O)NCCCCCNc3ncnc4c3ncn4[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
137642036 157330 0 AA2BR A2B receptor Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 387 6 3 12 -0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4087306 157330 0 AA2BR A2B receptor Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity 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
57387822 74901 0 AA2BR A2B receptor Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 840 13 7 12 6.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042312 74901 0 AA2BR A2B receptor Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 840 13 7 12 6.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
118732974 117765 0 AA2BR A2B receptor Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414940 117765 0 AA2BR A2B receptor Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of 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
118732975 117766 0 AA2BR A2B receptor Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL3414941 117766 0 AA2BR A2B receptor Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity 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
10436433 130588 0 AA2BR A2B receptor Human 6.2 pEC50 = 6.2 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 512 9 5 15 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL368880 130588 0 AA2BR A2B receptor Human 6.2 pEC50 = 6.2 Functional
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 512 9 5 15 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
44423811 84709 0 AA2BR A2B receptor Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 533 9 5 11 1.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccccc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226193 84709 0 AA2BR A2B receptor Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 533 9 5 11 1.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccccc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL4741079 178631 0 AA2BR A2B receptor Human 6.2 pEC50 = 6.2 Functional
Irreversible agonist activity at human adenosine A2B 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 A2B 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
118734347 117861 0 AA2BR A2B receptor Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 637 8 5 12 0.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(I)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416782 117861 0 AA2BR A2B receptor Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 637 8 5 12 0.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(I)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
123807 825 40 AA2BR A2B receptor Human 4.1 pEC50 = 4.1 Binding
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/acs.jmedchem.5b01402
374 825 40 AA2BR A2B receptor Human 4.1 pEC50 = 4.1 Binding
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/acs.jmedchem.5b01402
379 825 40 AA2BR A2B receptor Human 4.1 pEC50 = 4.1 Binding
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/acs.jmedchem.5b01402
CHEMBL284969 825 40 AA2BR A2B receptor Human 4.1 pEC50 = 4.1 Binding
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/acs.jmedchem.5b01402
10455080 95082 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL258535 95082 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
57384289 74892 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 630 13 6 13 2.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)CCCC[C@H]5CCSS5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042303 74892 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 630 13 6 13 2.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)CCCC[C@H]5CCSS5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
137646828 157186 0 AA2BR A2B receptor Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 856 16 6 13 6.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCCCNC(=O)c4ccc(-c5sc(N)c(C(=O)c6ccccc6)c5-c5cccc(C(F)(F)F)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.8b00047
CHEMBL4085418 157186 0 AA2BR A2B receptor Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 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
16203539 135564 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 444 6 5 10 0.3 Nc1nc(OCCc2c[nH]c3ccc(F)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL373478 135564 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 444 6 5 10 0.3 Nc1nc(OCCc2c[nH]c3ccc(F)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
76329265 105341 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 377 4 5 10 -0.9 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133158 105341 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B 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
16103176 82574 0 AA2BR A2B receptor Human 7.1 pEC50 = 7.1 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 417 6 5 11 -1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccco4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL218596 82574 0 AA2BR A2B receptor Human 7.1 pEC50 = 7.1 Functional
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 417 6 5 11 -1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccco4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
118732982 117773 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 583 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccccc5I)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414948 117773 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of 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
145976032 162761 0 AA2BR A2B receptor Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 402 7 2 7 3.9 N#Cc1c(N)nc(SCc2ccn[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4203420 162761 0 AA2BR A2B receptor Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 402 7 2 7 3.9 N#Cc1c(N)nc(SCc2ccn[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
155535452 171250 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assayAgonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay
ChEMBL 286 4 2 7 1.8 N#Cc1c(N)nc(SCCO)c(C#N)c1-c1ccoc1 10.1021/acs.jmedchem.9b00106
CHEMBL4472401 171250 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assayAgonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay
ChEMBL 286 4 2 7 1.8 N#Cc1c(N)nc(SCCO)c(C#N)c1-c1ccoc1 10.1021/acs.jmedchem.9b00106
118734374 117885 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 642 8 4 12 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCc6ccc(C(F)(F)F)cc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416808 117885 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 642 8 4 12 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCc6ccc(C(F)(F)F)cc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
69961639 174885 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assayAgonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay
ChEMBL 302 4 2 7 2.2 N#Cc1c(N)nc(SCCO)c(C#N)c1-c1cccs1 10.1021/acs.jmedchem.9b00106
CHEMBL4582726 174885 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assayAgonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay
ChEMBL 302 4 2 7 2.2 N#Cc1c(N)nc(SCCO)c(C#N)c1-c1cccs1 10.1021/acs.jmedchem.9b00106
46865897 7534 0 AA2BR A2B receptor Human 5.1 pEC50 = 5.1 Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 413 5 2 8 4.2 O=C(Nc1ccccc1)Nc1nc(Oc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmc.2010.02.039
CHEMBL1089440 7534 0 AA2BR A2B receptor Human 5.1 pEC50 = 5.1 Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 413 5 2 8 4.2 O=C(Nc1ccccc1)Nc1nc(Oc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmc.2010.02.039
11048438 168058 0 AA2BR A2B receptor Human 5.1 pEC50 = 5.1 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL438418 168058 0 AA2BR A2B receptor Human 5.1 pEC50 = 5.1 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
16202841 84016 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 442 6 6 11 -0.2 Nc1nc(OCCc2c[nH]c3ccc(O)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL222500 84016 0 AA2BR A2B receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 442 6 6 11 -0.2 Nc1nc(OCCc2c[nH]c3ccc(O)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
11164346 15777 0 AA2BR A2B receptor Human 8.1 pEC50 = 8.1 Functional
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 362 5 2 7 3.1 COc1ccc(-c2c(C#N)c(N)nc(SCc3ncc[nH]3)c2C#N)cc1 10.1021/jm049947s
CHEMBL122396 15777 0 AA2BR A2B receptor Human 8.1 pEC50 = 8.1 Functional
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 362 5 2 7 3.1 COc1ccc(-c2c(C#N)c(N)nc(SCc3ncc[nH]3)c2C#N)cc1 10.1021/jm049947s
145973077 163853 0 AA2BR A2B receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 402 7 2 7 3.9 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4216880 163853 0 AA2BR A2B receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 402 7 2 7 3.9 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
137641858 157485 0 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 696 13 5 11 5.3 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccc(-c2sccc2-c2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.8b00047
CHEMBL4089092 157485 0 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 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
11112711 158596 0 AA2BR A2B receptor Human 5.0 pEC50 = 5.0 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL410095 158596 0 AA2BR A2B receptor Human 5.0 pEC50 = 5.0 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
44450290 95788 0 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL262363 95788 0 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
118734372 117883 0 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 608 8 4 12 1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCc6ccc(Cl)cc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416806 117883 0 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 608 8 4 12 1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCc6ccc(Cl)cc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
118734345 117859 0 AA2BR A2B receptor Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 545 8 5 12 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(Cl)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416780 117859 0 AA2BR A2B receptor Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 545 8 5 12 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(Cl)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
118734346 117860 0 AA2BR A2B receptor Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 589 8 5 12 0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(Br)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416781 117860 0 AA2BR A2B receptor Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 589 8 5 12 0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(Br)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
89534951 163607 0 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 393 7 2 7 2.7 CNC(=O)CSc1nc(N)c(C#N)c(-c2ccc(OCC3CC3)cc2)c1C#N 10.1016/j.ejmech.2018.02.081
CHEMBL4213681 163607 0 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 393 7 2 7 2.7 CNC(=O)CSc1nc(N)c(C#N)c(-c2ccc(OCC3CC3)cc2)c1C#N 10.1016/j.ejmech.2018.02.081
377 2590 39 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assayAgonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen 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/acsmedchemlett.0c00509
425 2590 39 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assayAgonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen 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/acsmedchemlett.0c00509
448222 2590 39 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assayAgonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen 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/acsmedchemlett.0c00509
CHEMBL464859 2590 39 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assayAgonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen 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/acsmedchemlett.0c00509
215492 16110 2 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based assay
ChEMBL 324 4 5 10 -2.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCO)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.8b01662
CHEMBL1234591 16110 2 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based assay
ChEMBL 324 4 5 10 -2.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCO)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.8b01662
71657835 158911 0 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4104819 158911 0 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 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
9869857 66268 3 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Functional
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL186113 66268 3 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Functional
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
10455852 95367 0 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL259938 95367 0 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Binding
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
24827290 155545 0 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 707 11 5 12 3.0 O=C(COc1ccc(Nc2nc(OCCc3c[nH]c4cc(Br)ccc34)nc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)N1CCCC1 10.1021/jm701442d
CHEMBL406594 155545 0 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 707 11 5 12 3.0 O=C(COc1ccc(Nc2nc(OCCc3c[nH]c4cc(Br)ccc34)nc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)N1CCCC1 10.1021/jm701442d
137634052 155833 0 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 830 15 7 14 5.7 Nc1nc(NCCCCCCNC(=O)c2ccc(-c3sc(N)c(C(=O)c4ccccc4)c3-c3cccc(C(F)(F)F)c3)cc2)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/acs.jmedchem.8b00047
CHEMBL4069296 155833 0 AA2BR A2B receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 830 15 7 14 5.7 Nc1nc(NCCCCCCNC(=O)c2ccc(-c3sc(N)c(C(=O)c4ccccc4)c3-c3cccc(C(F)(F)F)c3)cc2)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/acs.jmedchem.8b00047
155541051 172122 0 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assayAgonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay
ChEMBL 406 5 1 8 4.2 COC(=O)c1cccc(CSc2nc(N)c(C#N)c(-c3cccs3)c2C#N)c1 10.1021/acs.jmedchem.9b00106
CHEMBL4517597 172122 0 AA2BR A2B receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assayAgonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay
ChEMBL 406 5 1 8 4.2 COC(=O)c1cccc(CSc2nc(N)c(C#N)c(-c3cccs3)c2C#N)c1 10.1021/acs.jmedchem.9b00106
16203669 84342 0 AA2BR A2B receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 467 7 5 10 0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(OCCc4c[nH]c5ccccc45)nc32)[C@H](O)[C@@H]1O 10.1021/jm061278q
CHEMBL223845 84342 0 AA2BR A2B receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 467 7 5 10 0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(OCCc4c[nH]c5ccccc45)nc32)[C@H](O)[C@@H]1O 10.1021/jm061278q
CHEMBL4643397 176942 0 AA2BR A2B receptor Human 9.5 pIC50 = 9.5 Functional
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 500 7 3 11 1.8 Nc1nc(NCCN2CCN(c3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
3284 3020 20 AA2BR A2B receptor Human 9.3 pIC50 = 9.3 Binding
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
44185871 3020 20 AA2BR A2B receptor Human 9.3 pIC50 = 9.3 Binding
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
5728 3020 20 AA2BR A2B receptor Human 9.3 pIC50 = 9.3 Binding
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
CHEMBL483688 3020 20 AA2BR A2B receptor Human 9.3 pIC50 = 9.3 Binding
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
3284 3020 20 AA2BR A2B receptor Human 9.1 pIC50 = 9.1 Binding
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
44185871 3020 20 AA2BR A2B receptor Human 9.1 pIC50 = 9.1 Binding
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
5728 3020 20 AA2BR A2B receptor Human 9.1 pIC50 = 9.1 Binding
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
CHEMBL483688 3020 20 AA2BR A2B receptor Human 9.1 pIC50 = 9.1 Binding
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
16037920 167924 0 AA2BR A2B receptor Human 9.0 pIC50 = 9 Binding
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 571 5 1 7 2.5 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Br)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL437309 167924 0 AA2BR A2B receptor Human 9.0 pIC50 = 9 Binding
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 571 5 1 7 2.5 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Br)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
74944536 163765 3 AA2BR A2B receptor Human 9.0 pIC50 = 9.0 Binding
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 540 7 0 7 2.8 CCCN1C(=O)N=C2N=C(c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)cc5)CC4)cc3)N=C2C1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4215606 163765 3 AA2BR A2B receptor Human 9.0 pIC50 = 9.0 Binding
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 540 7 0 7 2.8 CCCN1C(=O)N=C2N=C(c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)cc5)CC4)cc3)N=C2C1=O 10.1021/acs.jmedchem.7b01627
3284 3020 20 AA2BR A2B receptor Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
44185871 3020 20 AA2BR A2B receptor Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
5728 3020 20 AA2BR A2B receptor Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
CHEMBL483688 3020 20 AA2BR A2B receptor Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
CHEMBL7113 197821 0 AA2BR A2B receptor Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 262 1 1 5 2.7 Oc1c(-c2ccccc2)nnc2nc3ccccc3n12 10.1021/jm201177b
25207803 5427 0 AA2BR A2B receptor Human 8.9 pIC50 = 8.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL1077943 5427 0 AA2BR A2B receptor Human 8.9 pIC50 = 8.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
44186667 183751 0 AA2BR A2B receptor Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL486479 183751 0 AA2BR A2B receptor Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44186622 183353 0 AA2BR A2B receptor Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL483469 183353 0 AA2BR A2B receptor Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
10641040 9493 0 AA2BR A2B receptor Human 8.0 pIC50 = 8 Functional
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 342 3 0 6 3.4 O=c1c(-c2ccco2)nnc2n(Cc3ccccc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL113518 9493 0 AA2BR A2B receptor Human 8.0 pIC50 = 8 Functional
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 342 3 0 6 3.4 O=c1c(-c2ccco2)nnc2n(Cc3ccccc3)c3ccccc3n12 10.1021/jm201177b
44413112 138510 0 AA2BR A2B receptor Human 8.0 pIC50 = 8 Binding
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 511 5 1 7 1.9 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL379217 138510 0 AA2BR A2B receptor Human 8.0 pIC50 = 8 Binding
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 511 5 1 7 1.9 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
11605883 79306 5 AA2BR A2B receptor Human 8.0 pIC50 = 8 Functional
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL212625 79306 5 AA2BR A2B receptor Human 8.0 pIC50 = 8 Functional
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44185933 184032 0 AA2BR A2B receptor Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 522 8 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(CCc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL488541 184032 0 AA2BR A2B receptor Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 522 8 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(CCc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL3937015 147526 0 AA2BR A2B receptor Human 6.0 pIC50 = 6 Binding
Displacement of [3H]PSB603 from recombinant human adenosine A2B receptor expressed in HEK293 cell membranes after 1 hr by beta scintillation counting methodDisplacement of [3H]PSB603 from recombinant human adenosine A2B receptor expressed in HEK293 cell membranes after 1 hr by beta scintillation counting method
ChEMBL 395 4 2 4 5.7 O[C@H]1CC[C@H](Nc2ncc(-c3ccc4ccccc4c3)c(-c3ccccc3)n2)CC1 10.1016/j.ejmech.2016.09.081
135493268 109758 0 AA2BR A2B receptor Human 7.0 pIC50 = 7.0 Functional
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32481 109758 0 AA2BR A2B receptor Human 7.0 pIC50 = 7.0 Functional
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
134142435 144535 0 AA2BR A2B receptor Human 7.0 pIC50 = 7.0 Functional