Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
168278159 190336 0 None 23 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 839 15 5 15 6.6 Nc1sc(-c2ccc(-c3cn(CCCCCCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)nn3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5177040 190336 0 None 23 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 839 15 5 15 6.6 Nc1sc(-c2ccc(-c3cn(CCCCCCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)nn3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
168278159 190336 0 None 23 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 839 15 5 15 6.6 Nc1sc(-c2ccc(-c3cn(CCCCCCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)nn3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5177040 190336 0 None 23 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 839 15 5 15 6.6 Nc1sc(-c2ccc(-c3cn(CCCCCCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)nn3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
9975036 16296 0 None - 1 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 16296 0 None - 1 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 16296 0 None - 1 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 16296 0 None - 1 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
71657835 159713 3 None -1 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL4104819 159713 3 None -1 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
44423814 142073 0 None - 1 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 142073 0 None - 1 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 66800 11 None -213 5 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 66800 11 None -213 5 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 58790 0 None -831 2 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 58790 0 None -831 2 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 3275 65 None -51 5 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 3275 65 None -51 5 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 3275 65 None -51 5 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 3275 65 None -51 5 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 3275 65 None -51 5 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 70654 31 None - 1 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 70654 31 None - 1 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
118732976 118491 0 None -213 4 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 118491 0 None -213 4 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 85189 0 None - 1 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 85189 0 None - 1 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 85169 0 None -3 2 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 85169 0 None -3 2 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 164152 0 None - 1 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 164152 0 None - 1 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 159075 0 None -87 4 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 159075 0 None -87 4 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
123683 3099 63 None -1258 5 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 3099 63 None -1258 5 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 3099 63 None -1258 5 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 3099 63 None -1258 5 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 118496 0 None -38 4 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 118496 0 None -38 4 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 122941 0 None -416 3 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 122941 0 None -416 3 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 118490 0 None -173 4 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 118490 0 None -173 4 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 180774 0 None -123 4 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 180774 0 None -123 4 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 75454 0 None -17 4 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 75454 0 None -17 4 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 16277 28 None - 1 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 16277 28 None - 1 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
377 2738 53 None -48 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
425 2738 53 None -48 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
448222 2738 53 None -48 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
CHEMBL464859 2738 53 None -48 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
44423813 168725 0 None - 1 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 168725 0 None - 1 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 164465 0 None - 1 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 164465 0 None - 1 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 75460 0 None -60 4 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 75460 0 None -60 4 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 66855 0 None -389 2 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 66855 0 None -389 2 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 75459 0 None -134 4 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 75459 0 None -134 4 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 106035 0 None -3 4 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 106035 0 None -3 4 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 136653 0 None - 1 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 136653 0 None - 1 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 106031 0 None -31 3 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 106031 0 None -31 3 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
168282699 190994 0 None -12022 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 427 6 4 10 0.9 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5186757 190994 0 None -12022 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 427 6 4 10 0.9 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
57387824 75448 0 None -8 4 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 75448 0 None -8 4 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 85169 0 None -3 2 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 85169 0 None -3 2 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 157462 0 None -91 2 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 157462 0 None -91 2 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 159546 0 None -50 4 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 159546 0 None -50 4 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 66800 11 None -213 5 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 66800 11 None -213 5 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 122941 0 None -416 3 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 122941 0 None -416 3 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 123614 0 None -537 3 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 123614 0 None -537 3 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 79190 0 None - 1 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 79190 0 None - 1 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 118493 0 None -154 4 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 118493 0 None -154 4 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 163968 0 None - 1 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 163968 0 None - 1 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 75453 0 None -16 4 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 75453 0 None -16 4 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 96318 0 None - 1 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 96318 0 None - 1 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 137086 15 None - 1 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 137086 15 None - 1 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 75447 6 None -12 4 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 75447 6 None -12 4 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
168290627 191979 0 None 3 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 859 11 6 13 6.6 Nc1sc(-c2ccc(C(=O)NCCC#Cc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5201533 191979 0 None 3 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 859 11 6 13 6.6 Nc1sc(-c2ccc(C(=O)NCCC#Cc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
137656845 159772 0 None 1 3 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 159772 0 None 1 3 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
118732972 118487 0 None -234 4 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 118487 0 None -234 4 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 75450 0 None -33 4 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 75450 0 None -33 4 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 7867 15 None - 1 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 7867 15 None - 1 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 85343 0 None - 1 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 85343 0 None - 1 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 137560 0 None - 1 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 137560 0 None - 1 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 157406 0 None -1 4 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 157406 0 None -1 4 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 106019 0 None -100 4 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 106019 0 None -100 4 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 106020 0 None -39 4 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 106020 0 None -39 4 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 106028 0 None -316 3 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 106028 0 None -316 3 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 106029 0 None -158 3 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 106029 0 None -158 3 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 142168 0 None - 1 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 142168 0 None - 1 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 162552 1 None - 1 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 162552 1 None - 1 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 79200 0 None - 1 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 79200 0 None - 1 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 163888 0 None - 1 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 163888 0 None - 1 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 155801 0 None -173 4 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 155801 0 None -173 4 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 3357 33 None -213 5 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 3357 33 None -213 5 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 3357 33 None -213 5 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 8301 0 None - 1 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 8301 0 None - 1 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 186490 0 None - 1 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 186490 0 None - 1 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
168280775 191133 0 None -1096 4 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 524 7 4 10 2.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(C(C)(C)C)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5188601 191133 0 None -1096 4 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 524 7 4 10 2.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(C(C)(C)C)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
137643164 158077 0 None 5 4 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 158077 0 None 5 4 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
46885471 8300 0 None - 1 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 8300 0 None - 1 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 159402 0 None - 1 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 159402 0 None - 1 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 83189 0 None - 1 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 83189 0 None - 1 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 85220 0 None - 1 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 85220 0 None - 1 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 85133 0 None - 1 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 85133 0 None - 1 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 157283 0 None 7 3 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 157283 0 None 7 3 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 164793 0 None - 1 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 164793 0 None - 1 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 84683 0 None - 1 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 84683 0 None - 1 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 16730 1 None -1 2 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 16730 1 None -1 2 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
168283013 190851 0 None -3715 4 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 516 8 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5184828 190851 0 None -3715 4 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 516 8 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
137650899 157179 0 None -35 4 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 157179 0 None -35 4 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 159744 0 None -269 4 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 159744 0 None -269 4 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 106021 0 None -39 4 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 106021 0 None -39 4 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 106032 0 None -39 4 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 106032 0 None -39 4 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 75446 0 None -6 4 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 75446 0 None -6 4 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 166019 0 None - 1 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 166019 0 None - 1 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 77948 0 None -954 3 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 77948 0 None -954 3 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 159629 0 None -371 2 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 159629 0 None -371 2 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 7766 0 None - 1 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 7766 0 None - 1 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 161754 0 None -758 4 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 161754 0 None -758 4 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 83354 0 None - 1 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 83354 0 None - 1 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 163747 0 None - 1 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 163747 0 None - 1 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 157231 0 None -56 4 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 157231 0 None -56 4 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 84710 0 None - 1 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 84710 0 None - 1 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 84632 0 None - 1 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 84632 0 None - 1 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 85100 0 None - 1 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 85100 0 None - 1 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
118732974 118489 0 None -47 4 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 118489 0 None -47 4 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 157221 0 None -6 4 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 157221 0 None -6 4 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 179934 0 None -23 4 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 179934 0 None -23 4 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 157457 0 None -70 4 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 157457 0 None -70 4 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 160634 0 None - 1 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 160634 0 None - 1 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 75457 0 None -6 4 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 75457 0 None -6 4 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 2625 52 None 1 4 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 2625 52 None 1 4 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 2625 52 None 1 4 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 2625 52 None 1 4 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 162340 4 None - 1 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 162340 4 None - 1 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
168273986 190152 0 None -234422 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 505 6 4 10 1.6 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Br)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5174052 190152 0 None -234422 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 505 6 4 10 1.6 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Br)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
137648928 157381 0 None -97 4 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 157381 0 None -97 4 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 282 107 None -16 5 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 282 107 None -16 5 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
90 282 107 None -16 5 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 282 107 None -16 5 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 282 107 None -16 5 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 159151 0 None -316 4 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 159151 0 None -316 4 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 85371 0 None - 1 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 85371 0 None - 1 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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
2844 282 107 None -16 5 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 282 107 None -16 5 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
90 282 107 None -16 5 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 282 107 None -16 5 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 282 107 None -16 5 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 282 107 None -16 5 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 282 107 None -16 5 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
90 282 107 None -16 5 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 282 107 None -16 5 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 282 107 None -16 5 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 282 107 None -16 5 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 282 107 None -16 5 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
90 282 107 None -16 5 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 282 107 None -16 5 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 282 107 None -16 5 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
168278159 190336 0 None 23 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay
ChEMBL 839 15 5 15 6.6 Nc1sc(-c2ccc(-c3cn(CCCCCCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)nn3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5177040 190336 0 None 23 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay
ChEMBL 839 15 5 15 6.6 Nc1sc(-c2ccc(-c3cn(CCCCCCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)nn3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
377 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 106034 0 None -39 4 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 106034 0 None -39 4 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 75455 0 None -40 4 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 75455 0 None -40 4 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 158055 0 None -48 4 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 158055 0 None -48 4 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 84718 0 None - 1 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 84718 0 None - 1 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
168290340 191869 0 None -7943 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 475 7 4 10 1.6 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5199871 191869 0 None -7943 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 475 7 4 10 1.6 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
16103165 83353 0 None - 1 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 83353 0 None - 1 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 156860 0 None -1 3 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 156860 0 None -1 3 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 167399 0 None - 1 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 167399 0 None - 1 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 16451 6 None - 1 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 16451 6 None - 1 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 75456 0 None -9 4 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 75456 0 None -9 4 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 84778 0 None - 1 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 84778 0 None - 1 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 85355 0 None - 1 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 85355 0 None - 1 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 85370 0 None - 1 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 85370 0 None - 1 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 77948 0 None -954 3 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 77948 0 None -954 3 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 79204 0 None - 1 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 79204 0 None - 1 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 142252 0 None - 1 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 142252 0 None - 1 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 582 48 None - 1 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 582 48 None - 1 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 582 48 None - 1 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 3099 63 None -1258 5 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 3099 63 None -1258 5 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 3099 63 None -1258 5 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 3099 63 None -1258 5 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 85373 0 None - 1 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 85373 0 None - 1 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 118494 0 None -426 4 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 118494 0 None -426 4 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
44423823 142170 0 None - 1 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 142170 0 None - 1 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 85356 0 None - 1 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 85356 0 None - 1 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 76903 0 None - 1 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 76903 0 None - 1 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 96311 0 None - 1 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 96311 0 None - 1 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 76905 0 None -2187 3 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 76905 0 None -2187 3 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
377 2738 53 None -48 10 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
425 2738 53 None -48 10 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
448222 2738 53 None -48 10 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
CHEMBL464859 2738 53 None -48 10 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
145967103 164113 0 None - 1 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 164113 0 None - 1 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 141100 0 None - 1 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 141100 0 None - 1 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 7868 0 None - 1 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 7868 0 None - 1 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 17912 0 None - 1 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 17912 0 None - 1 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 162211 6 None - 1 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 162211 6 None - 1 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 162447 3 None - 1 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 162447 3 None - 1 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 158824 0 None - 1 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 158824 0 None - 1 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 8365 7 None - 1 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 8365 7 None - 1 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 164176 0 None - 1 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 164176 0 None - 1 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 118485 0 None -147 4 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 118485 0 None -147 4 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 137032 12 None - 1 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 137032 12 None - 1 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 159472 0 None 2 4 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 159472 0 None 2 4 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 142074 0 None - 1 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 142074 0 None - 1 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 118488 0 None -446 4 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 118488 0 None -446 4 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 75449 0 None -8 4 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 75449 0 None -8 4 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 83268 0 None - 1 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 83268 0 None - 1 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 85372 0 None - 1 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 85372 0 None - 1 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 84597 0 None - 1 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 84597 0 None - 1 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 83340 0 None - 1 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 83340 0 None - 1 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 201640 0 None - 1 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 201640 0 None - 1 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 159158 0 None -66 3 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 159158 0 None -66 3 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 163841 0 None - 1 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 163841 0 None - 1 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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
168269860 189952 0 None -17782 3 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 512 9 4 11 1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(OC)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5170857 189952 0 None -17782 3 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 512 9 4 11 1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(OC)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
118734376 118612 0 None -14 2 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 118612 0 None -14 2 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 901 45 None -1 6 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
375 901 45 None -1 6 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
424 901 45 None -1 6 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 901 45 None -1 6 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 106036 0 None -630 4 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 106036 0 None -630 4 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
71657835 159713 3 None -1 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL4104819 159713 3 None -1 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
377 2738 53 None -48 10 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
425 2738 53 None -48 10 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
448222 2738 53 None -48 10 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
CHEMBL464859 2738 53 None -48 10 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
57384544 75458 0 None -57 4 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 75458 0 None -57 4 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 157677 0 None -194 4 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 157677 0 None -194 4 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 85384 0 None - 1 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 85384 0 None - 1 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 7991 0 None - 1 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 7991 0 None - 1 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
168293442 192111 0 None -17782 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 546 7 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Br)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5203632 192111 0 None -17782 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 546 7 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Br)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
168297905 192407 0 None -2041 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 516 8 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5208245 192407 0 None -2041 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 516 8 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
377 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 157602 0 None -6 4 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 157602 0 None -6 4 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 85357 0 None - 1 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 85357 0 None - 1 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 83267 0 None - 1 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 83267 0 None - 1 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 79203 2 None - 1 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 79203 2 None - 1 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 191757 18 None -1174 3 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 191757 18 None -1174 3 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 162874 3 None - 1 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 162874 3 None - 1 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 157121 0 None -6 4 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 157121 0 None -6 4 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 122903 0 None -47 2 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 122903 0 None -47 2 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 69795 7 None - 1 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 69795 7 None - 1 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
168285984 191718 0 None -5248 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5197358 191718 0 None -5248 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
76336526 106030 0 None -501 3 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 106030 0 None -501 3 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 164518 0 None - 1 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 164518 0 None - 1 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 66800 11 None -213 5 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 66800 11 None -213 5 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
168297825 192259 0 None -8317 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5205907 192259 0 None -8317 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
168286257 191572 0 None 6 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 863 14 6 13 6.3 Nc1sc(-c2ccc(C(=O)NCCc3ccc(CCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5195260 191572 0 None 6 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 863 14 6 13 6.3 Nc1sc(-c2ccc(C(=O)NCCc3ccc(CCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
2844 282 107 None -16 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
60961 282 107 None -16 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
90 282 107 None -16 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
CHEMBL477 282 107 None -16 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
DB00640 282 107 None -16 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
168293183 192102 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 767 16 6 13 4.7 Nc1sc(CCC(=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.2c00320
CHEMBL5203535 192102 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 767 16 6 13 4.7 Nc1sc(CCC(=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.2c00320
137642153 158344 0 None -35 4 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 158344 0 None -35 4 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 85358 0 None - 1 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 85358 0 None - 1 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 118495 0 None -63 4 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 118495 0 None -63 4 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 96304 33 None -501 3 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 96304 33 None -501 3 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 138039 0 None - 1 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 138039 0 None - 1 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 76906 4 None -239 2 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 76906 4 None -239 2 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 118486 0 None -141 4 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 118486 0 None -141 4 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 123614 0 None -537 3 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 123614 0 None -537 3 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 156811 0 None -269 4 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 156811 0 None -269 4 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
168293564 192133 0 None 45 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 849 13 6 13 6.8 Nc1sc(-c2ccc(C(=O)NCCCc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5203917 192133 0 None 45 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 849 13 6 13 6.8 Nc1sc(-c2ccc(C(=O)NCCCc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
137653409 159013 0 None -1 4 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 159013 0 None -1 4 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
168288912 191604 0 None -4897 4 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5195714 191604 0 None -4897 4 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
16103169 82641 0 None - 1 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 82641 0 None - 1 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 75451 0 None -426 4 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 75451 0 None -426 4 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 115409 0 None - 1 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 115409 0 None - 1 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
137650461 157232 0 None -1 4 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 157232 0 None -1 4 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
137634444 156139 0 None 1 3 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 156139 0 None 1 3 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
377 2738 53 None -48 10 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
425 2738 53 None -48 10 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
448222 2738 53 None -48 10 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
CHEMBL464859 2738 53 None -48 10 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
137642036 158128 0 None -177 4 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 158128 0 None -177 4 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 75461 0 None -3 3 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 75461 0 None -3 3 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 118489 0 None -47 4 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 118489 0 None -47 4 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 118490 0 None -173 4 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 118490 0 None -173 4 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 131347 0 None -478 2 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 131347 0 None -478 2 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 85342 0 None - 1 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 85342 0 None - 1 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
162645916 179472 0 None -9 4 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
CHEMBL4741079 179472 0 None -9 4 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 118585 0 None -45 2 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 118585 0 None -45 2 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
57384289 75452 0 None -112 4 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 75452 0 None -112 4 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 157982 0 None -1 4 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 157982 0 None -1 4 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 136324 0 None - 1 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 136324 0 None - 1 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 106033 0 None -50 4 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 106033 0 None -50 4 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
168283120 191037 0 None -60255 4 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 498 8 4 11 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(OC)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5187330 191037 0 None -60255 4 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 498 8 4 11 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(OC)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
168287894 191327 0 None -776 4 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(Cl)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5191989 191327 0 None -776 4 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(Cl)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
71657835 159713 3 None -1 4 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL4104819 159713 3 None -1 4 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
16103176 83194 0 None - 1 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 83194 0 None - 1 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 118497 0 None -91 4 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 118497 0 None -91 4 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 163563 0 None - 1 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 163563 0 None - 1 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 172066 0 None -14 2 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 172066 0 None -14 2 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 118609 0 None -22 2 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 118609 0 None -22 2 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 175708 0 None -8 2 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 175708 0 None -8 2 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 7765 0 None - 1 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 7765 0 None - 1 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
16202841 84647 0 None - 1 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 84647 0 None - 1 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 16104 0 None - 1 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 16104 0 None - 1 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 164653 0 None - 1 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 164653 0 None - 1 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 158283 0 None 1 4 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 158283 0 None 1 4 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
168269866 189964 0 None -3090 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 468 7 4 10 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5171042 189964 0 None -3090 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 468 7 4 10 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
118734372 118607 0 None -17 2 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 118607 0 None -17 2 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 118583 0 None -301 2 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 118583 0 None -301 2 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 118584 0 None -218 2 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 118584 0 None -218 2 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 164407 0 None - 1 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 164407 0 None - 1 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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 2738 53 None -48 10 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
168272212 190407 0 None -2 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 518 10 5 10 1.9 O=C(NCCCCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5178142 190407 0 None -2 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 518 10 5 10 1.9 O=C(NCCCCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccccc1 10.1021/acs.jmedchem.2c00320
71657835 159713 3 None -1 4 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 159713 3 None -1 4 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 66800 11 None -213 5 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 66800 11 None -213 5<