Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

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 DOI
168278159 190469 None 0 Human Functional pEC50 = 9.5 9.5 23 4
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 190469 None 0 Human Functional pEC50 = 9.5 9.5 23 4
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 190469 None 0 Human Functional pEC50 = 9.4 9.4 23 4
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 190469 None 0 Human Functional pEC50 = 9.4 9.4 23 4
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 16335 None 0 Human Functional pEC50 = 8 8.0 - 1
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 16335 None 0 Human Functional pEC50 = 8 8.0 - 1
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 16335 None 0 Human Functional pEC50 = 8 8.0 - 1
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 16335 None 0 Human Functional pEC50 = 8 8.0 - 1
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 159831 None 4 Human Functional pEC50 = 8.0 8.0 -1 4
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 159831 None 4 Human Functional pEC50 = 8.0 8.0 -1 4
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 142185 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 142185 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 66851 None 12 Human Functional pEC50 = 6 6.0 -213 5
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 66851 None 12 Human Functional pEC50 = 6 6.0 -213 5
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 58837 None 0 Human Functional pEC50 = 5 5.0 -831 2
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 58837 None 0 Human Functional pEC50 = 5 5.0 -831 2
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 3300 None 47 Human Functional pEC50 = 5 5.0 -51 5
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
219024.0 3300 None 47 Human Functional pEC50 = 5 5.0 -51 5
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 3300 None 47 Human Functional pEC50 = 5 5.0 -51 5
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 3300 None 47 Human Functional pEC50 = 5 5.0 -51 5
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 3300 None 47 Human Functional pEC50 = 5 5.0 -51 5
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 3300 None 47 Human Functional pEC50 = 5 5.0 -51 5
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 70707 None 26 Human Functional pEC50 = 5 5.0 - 1
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 70707 None 26 Human Functional pEC50 = 5 5.0 - 1
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 118581 None 0 Human Functional pEC50 = 6 6.0 -213 4
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 118581 None 0 Human Functional pEC50 = 6 6.0 -213 4
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 2758 None 42 Human Functional pEC50 = 7.0 7.0 -50 10
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 2758 None 42 Human Functional pEC50 = 7.0 7.0 -50 10
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 2758 None 42 Human Functional pEC50 = 7.0 7.0 -50 10
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 2758 None 42 Human Functional pEC50 = 7.0 7.0 -50 10
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 85252 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 85252 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 85232 None 0 Human Functional pEC50 = 7.0 7.0 -3 2
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 85232 None 0 Human Functional pEC50 = 7.0 7.0 -3 2
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 164271 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 164271 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 2758 None 42 Human Functional pEC50 = 7.0 7.0 -50 10
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 2758 None 42 Human Functional pEC50 = 7.0 7.0 -50 10
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 2758 None 42 Human Functional pEC50 = 7.0 7.0 -50 10
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 2758 None 42 Human Functional pEC50 = 7.0 7.0 -50 10
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 159192 None 0 Human Functional pEC50 = 6.0 6.0 -87 4
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 159192 None 0 Human Functional pEC50 = 6.0 6.0 -87 4
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 3121 None 46 Human Functional pEC50 = 5.0 5.0 -1258 5
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 3121 None 46 Human Functional pEC50 = 5.0 5.0 -1258 5
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 3121 None 46 Human Functional pEC50 = 5.0 5.0 -1258 5
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 3121 None 46 Human Functional pEC50 = 5.0 5.0 -1258 5
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 118586 None 0 Human Functional pEC50 = 6.0 6.0 -38 4
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 118586 None 0 Human Functional pEC50 = 6.0 6.0 -38 4
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 123033 None 0 Human Functional pEC50 = 5.9 5.9 -416 3
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 123033 None 0 Human Functional pEC50 = 5.9 5.9 -416 3
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 118580 None 0 Human Functional pEC50 = 5.9 5.9 -173 4
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 118580 None 0 Human Functional pEC50 = 5.9 5.9 -173 4
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 180904 None 0 Human Functional pEC50 = 6.9 6.9 -123 4
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 180904 None 0 Human Functional pEC50 = 6.9 6.9 -123 4
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 75510 None 0 Human Functional pEC50 = 5.9 5.9 -17 4
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 75510 None 0 Human Functional pEC50 = 5.9 5.9 -17 4
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 16316 None 25 Human Functional pEC50 = 7.9 7.9 - 1
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 16316 None 25 Human Functional pEC50 = 7.9 7.9 - 1
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 2758 None 42 Human Functional pEC50 = 7.9 7.9 -50 10
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 2758 None 42 Human Functional pEC50 = 7.9 7.9 -50 10
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 2758 None 42 Human Functional pEC50 = 7.9 7.9 -50 10
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 2758 None 42 Human Functional pEC50 = 7.9 7.9 -50 10
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 168852 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 168852 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 164584 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 164584 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 75516 None 0 Human Functional pEC50 = 6.9 6.9 -60 4
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 75516 None 0 Human Functional pEC50 = 6.9 6.9 -60 4
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 66906 None 0 Human Functional pEC50 = 5.9 5.9 -389 2
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 66906 None 0 Human Functional pEC50 = 5.9 5.9 -389 2
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 75515 None 0 Human Functional pEC50 = 4.9 4.9 -134 4
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 75515 None 0 Human Functional pEC50 = 4.9 4.9 -134 4
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 106118 None 0 Human Functional pEC50 = 6.9 6.9 -3 4
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 106118 None 0 Human Functional pEC50 = 6.9 6.9 -3 4
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 136765 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 136765 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 106114 None 0 Human Functional pEC50 = 5.9 5.9 -31 3
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 106114 None 0 Human Functional pEC50 = 5.9 5.9 -31 3
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 191127 None 0 Human Functional pEC50 = 4.9 4.9 -12022 3
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 191127 None 0 Human Functional pEC50 = 4.9 4.9 -12022 3
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 75504 None 0 Human Functional pEC50 = 6.9 6.9 -8 4
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 75504 None 0 Human Functional pEC50 = 6.9 6.9 -8 4
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 85232 None 0 Human Functional pEC50 = 6.9 6.9 -3 2
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 85232 None 0 Human Functional pEC50 = 6.9 6.9 -3 2
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 157578 None 0 Human Functional pEC50 = 4.9 4.9 -91 2
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 157578 None 0 Human Functional pEC50 = 4.9 4.9 -91 2
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 159664 None 0 Human Functional pEC50 = 5.9 5.9 -50 4
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 159664 None 0 Human Functional pEC50 = 5.9 5.9 -50 4
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 66851 None 12 Human Functional pEC50 = 5.9 5.9 -213 5
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 66851 None 12 Human Functional pEC50 = 5.9 5.9 -213 5
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 123033 None 0 Human Functional pEC50 = 5.9 5.9 -416 3
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 123033 None 0 Human Functional pEC50 = 5.9 5.9 -416 3
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 123707 None 0 Human Functional pEC50 = 5.9 5.9 -537 3
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 123707 None 0 Human Functional pEC50 = 5.9 5.9 -537 3
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 79250 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 79250 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 118583 None 0 Human Functional pEC50 = 5.9 5.9 -154 4
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 118583 None 0 Human Functional pEC50 = 5.9 5.9 -154 4
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 164087 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 164087 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 75509 None 0 Human Functional pEC50 = 7.9 7.9 -16 4
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 75509 None 0 Human Functional pEC50 = 7.9 7.9 -16 4
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 2758 None 42 Human Functional pEC50 = 6.9 6.9 -50 10
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 2758 None 42 Human Functional pEC50 = 6.9 6.9 -50 10
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 2758 None 42 Human Functional pEC50 = 6.9 6.9 -50 10
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 2758 None 42 Human Functional pEC50 = 6.9 6.9 -50 10
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 96400 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 96400 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 137198 None 14 Human Functional pEC50 = 5.8 5.8 - 1
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 137198 None 14 Human Functional pEC50 = 5.8 5.8 - 1
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 75503 None 4 Human Functional pEC50 = 6.8 6.8 -12 4
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 75503 None 4 Human Functional pEC50 = 6.8 6.8 -12 4
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 192112 None 0 Human Functional pEC50 = 6.8 6.8 3 4
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 192112 None 0 Human Functional pEC50 = 6.8 6.8 3 4
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 159890 None 0 Human Functional pEC50 = 6.8 6.8 1 3
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 159890 None 0 Human Functional pEC50 = 6.8 6.8 1 3
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 118577 None 0 Human Functional pEC50 = 5.8 5.8 -234 4
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 118577 None 0 Human Functional pEC50 = 5.8 5.8 -234 4
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 75506 None 0 Human Functional pEC50 = 5.8 5.8 -33 4
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 75506 None 0 Human Functional pEC50 = 5.8 5.8 -33 4
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 7901 None 19 Human Functional pEC50 = 4.8 4.8 - 1
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 7901 None 19 Human Functional pEC50 = 4.8 4.8 - 1
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 85406 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 85406 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 2758 None 42 Human Functional pEC50 = 7.8 7.8 -50 10
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 2758 None 42 Human Functional pEC50 = 7.8 7.8 -50 10
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 2758 None 42 Human Functional pEC50 = 7.8 7.8 -50 10
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 2758 None 42 Human Functional pEC50 = 7.8 7.8 -50 10
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 137672 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 137672 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 2758 None 42 Human Functional pEC50 = 5.8 5.8 -50 10
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 2758 None 42 Human Functional pEC50 = 5.8 5.8 -50 10
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 2758 None 42 Human Functional pEC50 = 5.8 5.8 -50 10
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 2758 None 42 Human Functional pEC50 = 5.8 5.8 -50 10
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 2758 None 42 Human Functional pEC50 = 6.8 6.8 -50 10
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 2758 None 42 Human Functional pEC50 = 6.8 6.8 -50 10
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 2758 None 42 Human Functional pEC50 = 6.8 6.8 -50 10
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 2758 None 42 Human Functional pEC50 = 6.8 6.8 -50 10
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 157522 None 0 Human Functional pEC50 = 6.8 6.8 -1 4
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 157522 None 0 Human Functional pEC50 = 6.8 6.8 -1 4
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 106102 None 0 Human Functional pEC50 = 6.8 6.8 -100 4
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 106102 None 0 Human Functional pEC50 = 6.8 6.8 -100 4
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 106103 None 0 Human Functional pEC50 = 6.8 6.8 -39 4
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 106103 None 0 Human Functional pEC50 = 6.8 6.8 -39 4
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 106111 None 0 Human Functional pEC50 = 5.8 5.8 -316 3
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 106111 None 0 Human Functional pEC50 = 5.8 5.8 -316 3
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 106112 None 0 Human Functional pEC50 = 5.8 5.8 -158 3
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 106112 None 0 Human Functional pEC50 = 5.8 5.8 -158 3
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 142280 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 142280 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 162671 None 1 Human Functional pEC50 = 7.8 7.8 - 1
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 162671 None 1 Human Functional pEC50 = 7.8 7.8 - 1
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 2758 None 42 Human Functional pEC50 = 6.8 6.8 -50 10
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 2758 None 42 Human Functional pEC50 = 6.8 6.8 -50 10
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 2758 None 42 Human Functional pEC50 = 6.8 6.8 -50 10
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 2758 None 42 Human Functional pEC50 = 6.8 6.8 -50 10
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 79260 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 79260 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 164007 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 164007 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 155915 None 0 Human Functional pEC50 = 5.8 5.8 -173 4
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 155915 None 0 Human Functional pEC50 = 5.8 5.8 -173 4
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 3382 None 22 Human Functional pEC50 = 5.8 5.8 -213 5
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 3382 None 22 Human Functional pEC50 = 5.8 5.8 -213 5
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 3382 None 22 Human Functional pEC50 = 5.8 5.8 -213 5
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 8335 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 8335 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 186620 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 186620 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 191266 None 0 Human Functional pEC50 = 4.8 4.8 -1096 4
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 191266 None 0 Human Functional pEC50 = 4.8 4.8 -1096 4
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 158193 None 0 Human Functional pEC50 = 7.8 7.8 5 4
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 158193 None 0 Human Functional pEC50 = 7.8 7.8 5 4
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 8334 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 8334 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 159520 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 159520 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 83250 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 83250 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 85283 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 85283 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 85196 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 85196 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 157399 None 0 Human Functional pEC50 = 7.7 7.7 7 3
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 157399 None 0 Human Functional pEC50 = 7.7 7.7 7 3
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 164912 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 164912 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 84746 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 84746 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 16769 None 1 Human Functional pEC50 = 7.7 7.7 -1 2
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 16769 None 1 Human Functional pEC50 = 7.7 7.7 -1 2
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 190984 None 0 Human Functional pEC50 = 4.7 4.7 -3715 4
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 190984 None 0 Human Functional pEC50 = 4.7 4.7 -3715 4
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 157295 None 0 Human Functional pEC50 = 5.7 5.7 -35 4
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 157295 None 0 Human Functional pEC50 = 5.7 5.7 -35 4
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 159862 None 0 Human Functional pEC50 = 5.7 5.7 -269 4
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 159862 None 0 Human Functional pEC50 = 5.7 5.7 -269 4
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 106104 None 0 Human Functional pEC50 = 6.7 6.7 -39 4
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 106104 None 0 Human Functional pEC50 = 6.7 6.7 -39 4
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 106115 None 0 Human Functional pEC50 = 6.7 6.7 -39 4
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 106115 None 0 Human Functional pEC50 = 6.7 6.7 -39 4
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 75502 None 0 Human Functional pEC50 = 8.6 8.6 -6 4
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 75502 None 0 Human Functional pEC50 = 8.6 8.6 -6 4
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 166138 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 166138 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 78006 None 0 Human Functional pEC50 = 5.7 5.7 -954 3
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 78006 None 0 Human Functional pEC50 = 5.7 5.7 -954 3
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 159747 None 0 Human Functional pEC50 = 4.7 4.7 -371 2
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 159747 None 0 Human Functional pEC50 = 4.7 4.7 -371 2
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 7800 None 0 Human Functional pEC50 = 4.7 4.7 - 1
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 7800 None 0 Human Functional pEC50 = 4.7 4.7 - 1
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 161872 None 0 Human Functional pEC50 = 5.7 5.7 -758 4
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 161872 None 0 Human Functional pEC50 = 5.7 5.7 -758 4
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 83415 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 83415 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 163866 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 163866 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 157347 None 0 Human Functional pEC50 = 5.7 5.7 -56 4
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 157347 None 0 Human Functional pEC50 = 5.7 5.7 -56 4
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 84773 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 84773 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 84695 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 84695 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 85163 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 85163 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 118579 None 0 Human Functional pEC50 = 6.7 6.7 -47 4
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 118579 None 0 Human Functional pEC50 = 6.7 6.7 -47 4
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 157337 None 0 Human Functional pEC50 = 6.7 6.7 -6 4
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 157337 None 0 Human Functional pEC50 = 6.7 6.7 -6 4
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 180064 None 0 Human Functional pEC50 = 6.7 6.7 -23 4
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 180064 None 0 Human Functional pEC50 = 6.7 6.7 -23 4
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 157573 None 0 Human Functional pEC50 = 5.7 5.7 -70 4
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 157573 None 0 Human Functional pEC50 = 5.7 5.7 -70 4
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 160752 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 160752 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 75513 None 0 Human Functional pEC50 = 5.6 5.6 -6 4
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 75513 None 0 Human Functional pEC50 = 5.6 5.6 -6 4
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 2643 None 38 Human Functional pEC50 = 7.6 7.6 1 4
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 2643 None 38 Human Functional pEC50 = 7.6 7.6 1 4
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 2643 None 38 Human Functional pEC50 = 7.6 7.6 1 4
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 2643 None 38 Human Functional pEC50 = 7.6 7.6 1 4
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 162458 None 3 Human Functional pEC50 = 7.6 7.6 - 1
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 162458 None 3 Human Functional pEC50 = 7.6 7.6 - 1
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 190285 None 0 Human Functional pEC50 = 4.6 4.6 -234422 2
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 190285 None 0 Human Functional pEC50 = 4.6 4.6 -234422 2
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 157497 None 0 Human Functional pEC50 = 6.6 6.6 -97 4
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 157497 None 0 Human Functional pEC50 = 6.6 6.6 -97 4
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 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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
60961.0 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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
90 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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 159268 None 0 Human Functional pEC50 = 5.6 5.6 -316 4
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 159268 None 0 Human Functional pEC50 = 5.6 5.6 -316 4
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 85434 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 85434 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 2758 None 42 Human Functional pEC50 = 5.6 5.6 -50 10
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 2758 None 42 Human Functional pEC50 = 5.6 5.6 -50 10
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 2758 None 42 Human Functional pEC50 = 5.6 5.6 -50 10
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 2758 None 42 Human Functional pEC50 = 5.6 5.6 -50 10
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 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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
60961.0 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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
90 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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
60961.0 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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
90 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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
60961.0 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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
90 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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 283 None 61 Human Functional pEC50 = 4.6 4.6 -16 5
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 190469 None 0 Human Functional pEC50 = 6.6 6.6 23 4
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 190469 None 0 Human Functional pEC50 = 6.6 6.6 23 4
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 2758 None 42 Human Functional pEC50 = 6.6 6.6 -50 10
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 2758 None 42 Human Functional pEC50 = 6.6 6.6 -50 10
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 2758 None 42 Human Functional pEC50 = 6.6 6.6 -50 10
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 2758 None 42 Human Functional pEC50 = 6.6 6.6 -50 10
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 106117 None 0 Human Functional pEC50 = 5.6 5.6 -39 4
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 106117 None 0 Human Functional pEC50 = 5.6 5.6 -39 4
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
377 2758 None 42 Human Functional pEC50 = 6.6 6.6 -50 10
Agonist activity at human A2BAR expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 30 mins by TR-FRET assayAgonist activity at human A2BAR expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 30 mins by TR-FRET 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.2c01768
425 2758 None 42 Human Functional pEC50 = 6.6 6.6 -50 10
Agonist activity at human A2BAR expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 30 mins by TR-FRET assayAgonist activity at human A2BAR expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 30 mins by TR-FRET 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.2c01768
448222 2758 None 42 Human Functional pEC50 = 6.6 6.6 -50 10
Agonist activity at human A2BAR expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 30 mins by TR-FRET assayAgonist activity at human A2BAR expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 30 mins by TR-FRET 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.2c01768
CHEMBL464859 2758 None 42 Human Functional pEC50 = 6.6 6.6 -50 10
Agonist activity at human A2BAR expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 30 mins by TR-FRET assayAgonist activity at human A2BAR expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 30 mins by TR-FRET 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.2c01768
57388055 75511 None 0 Human Functional pEC50 = 6.6 6.6 -40 4
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 75511 None 0 Human Functional pEC50 = 6.6 6.6 -40 4
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 158171 None 0 Human Functional pEC50 = 5.6 5.6 -48 4
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 158171 None 0 Human Functional pEC50 = 5.6 5.6 -48 4
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 84781 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 84781 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 192002 None 0 Human Functional pEC50 = 4.6 4.6 -7943 3
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 192002 None 0 Human Functional pEC50 = 4.6 4.6 -7943 3
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 83414 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 83414 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 156976 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
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 156976 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
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 167519 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 167519 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 16490 None 4 Human Functional pEC50 = 4.5 4.5 - 1
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 16490 None 4 Human Functional pEC50 = 4.5 4.5 - 1
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 75512 None 0 Human Functional pEC50 = 6.5 6.5 -9 4
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 75512 None 0 Human Functional pEC50 = 6.5 6.5 -9 4
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 84841 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 84841 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 2758 None 42 Human Functional pEC50 = 8.5 8.5 -50 10
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 2758 None 42 Human Functional pEC50 = 8.5 8.5 -50 10
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 2758 None 42 Human Functional pEC50 = 8.5 8.5 -50 10
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 2758 None 42 Human Functional pEC50 = 8.5 8.5 -50 10
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 85418 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 85418 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 85433 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 85433 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 78006 None 0 Human Functional pEC50 = 5.5 5.5 -954 3
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 78006 None 0 Human Functional pEC50 = 5.5 5.5 -954 3
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 79264 None 0 Human Functional pEC50 = 4.5 4.5 - 1
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 79264 None 0 Human Functional pEC50 = 4.5 4.5 - 1
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 142364 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 142364 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 585 None 42 Human Functional pEC50 = 7.5 7.5 38 2
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 585 None 42 Human Functional pEC50 = 7.5 7.5 38 2
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 585 None 42 Human Functional pEC50 = 7.5 7.5 38 2
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 3121 None 46 Human Functional pEC50 = 7.5 7.5 -1258 5
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 3121 None 46 Human Functional pEC50 = 7.5 7.5 -1258 5
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 3121 None 46 Human Functional pEC50 = 7.5 7.5 -1258 5
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 3121 None 46 Human Functional pEC50 = 7.5 7.5 -1258 5
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 2758 None 42 Human Functional pEC50 = 5.5 5.5 -50 10
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 2758 None 42 Human Functional pEC50 = 5.5 5.5 -50 10
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 2758 None 42 Human Functional pEC50 = 5.5 5.5 -50 10
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 2758 None 42 Human Functional pEC50 = 5.5 5.5 -50 10
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 85436 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 85436 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 118584 None 0 Human Functional pEC50 = 5.5 5.5 -426 4
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 118584 None 0 Human Functional pEC50 = 5.5 5.5 -426 4
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 142282 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 142282 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 85419 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 85419 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 76960 None 0 Human Functional pEC50 = 4.5 4.5 - 1
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 76960 None 0 Human Functional pEC50 = 4.5 4.5 - 1
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 96393 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 96393 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 2758 None 42 Human Functional pEC50 = 6.5 6.5 -50 10
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 2758 None 42 Human Functional pEC50 = 6.5 6.5 -50 10
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 2758 None 42 Human Functional pEC50 = 6.5 6.5 -50 10
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 2758 None 42 Human Functional pEC50 = 6.5 6.5 -50 10
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 76962 None 0 Human Functional pEC50 = 4.5 4.5 -2187 3
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 76962 None 0 Human Functional pEC50 = 4.5 4.5 -2187 3
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 2758 None 42 Human Functional pEC50 = 6.5 6.5 -50 10
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 2758 None 42 Human Functional pEC50 = 6.5 6.5 -50 10
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 2758 None 42 Human Functional pEC50 = 6.5 6.5 -50 10
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 2758 None 42 Human Functional pEC50 = 6.5 6.5 -50 10
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 164232 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 164232 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 141212 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 141212 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 7902 None 0 Human Functional pEC50 = 4.5 4.5 - 1
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 7902 None 0 Human Functional pEC50 = 4.5 4.5 - 1
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 17951 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 17951 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 162329 None 4 Human Functional pEC50 = 7.5 7.5 - 1
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 162329 None 4 Human Functional pEC50 = 7.5 7.5 - 1
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 162566 None 2 Human Functional pEC50 = 7.5 7.5 - 1
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 162566 None 2 Human Functional pEC50 = 7.5 7.5 - 1
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 158940 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 158940 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 8399 None 6 Human Functional pEC50 = 5.5 5.5 - 1
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 8399 None 6 Human Functional pEC50 = 5.5 5.5 - 1
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 164295 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 164295 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 118575 None 0 Human Functional pEC50 = 6.5 6.5 -147 4
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 118575 None 0 Human Functional pEC50 = 6.5 6.5 -147 4
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 137144 None 8 Human Functional pEC50 = 5.5 5.5 - 1
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 137144 None 8 Human Functional pEC50 = 5.5 5.5 - 1
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 159590 None 0 Human Functional pEC50 = 7.5 7.5 2 4
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 159590 None 0 Human Functional pEC50 = 7.5 7.5 2 4
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 142186 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 142186 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 118578 None 0 Human Functional pEC50 = 5.5 5.5 -446 4
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 118578 None 0 Human Functional pEC50 = 5.5 5.5 -446 4
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 75505 None 0 Human Functional pEC50 = 6.5 6.5 -8 4
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 75505 None 0 Human Functional pEC50 = 6.5 6.5 -8 4
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 83329 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 83329 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 85435 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 85435 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 2758 None 42 Human Functional pEC50 = 5.4 5.4 -50 10
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 2758 None 42 Human Functional pEC50 = 5.4 5.4 -50 10
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 2758 None 42 Human Functional pEC50 = 5.4 5.4 -50 10
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 2758 None 42 Human Functional pEC50 = 5.4 5.4 -50 10
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 84660 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 84660 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 83401 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 83401 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 204120 None 0 Human Functional pEC50 = 4.4 4.4 - 1
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 204120 None 0 Human Functional pEC50 = 4.4 4.4 - 1
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 159275 None 0 Human Functional pEC50 = 5.4 5.4 -66 3
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 159275 None 0 Human Functional pEC50 = 5.4 5.4 -66 3
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 163960 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 163960 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 2758 None 42 Human Functional pEC50 = 7.4 7.4 -50 10
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 2758 None 42 Human Functional pEC50 = 7.4 7.4 -50 10
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 2758 None 42 Human Functional pEC50 = 7.4 7.4 -50 10
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 2758 None 42 Human Functional pEC50 = 7.4 7.4 -50 10
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 190085 None 0 Human Functional pEC50 = 4.4 4.4 -17782 3
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 190085 None 0 Human Functional pEC50 = 4.4 4.4 -17782 3
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 118702 None 0 Human Functional pEC50 = 6.4 6.4 -14 2
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 118702 None 0 Human Functional pEC50 = 6.4 6.4 -14 2
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 904 None 36 Human Functional pEC50 = 7.4 7.4 -1 6
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
375 904 None 36 Human Functional pEC50 = 7.4 7.4 -1 6
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
424 904 None 36 Human Functional pEC50 = 7.4 7.4 -1 6
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 904 None 36 Human Functional pEC50 = 7.4 7.4 -1 6
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 106119 None 0 Human Functional pEC50 = 6.4 6.4 -630 4
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 106119 None 0 Human Functional pEC50 = 6.4 6.4 -630 4
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 159831 None 4 Human Functional pEC50 = 8.3 8.3 -1 4
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 159831 None 4 Human Functional pEC50 = 8.3 8.3 -1 4
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 2758 None 42 Human Functional pEC50 = 8.3 8.3 -50 10
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 2758 None 42 Human Functional pEC50 = 8.3 8.3 -50 10
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 2758 None 42 Human Functional pEC50 = 8.3 8.3 -50 10
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 2758 None 42 Human Functional pEC50 = 8.3 8.3 -50 10
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 75514 None 0 Human Functional pEC50 = 4.4 4.4 -57 4
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 75514 None 0 Human Functional pEC50 = 4.4 4.4 -57 4
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 157793 None 0 Human Functional pEC50 = 6.4 6.4 -194 4
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 157793 None 0 Human Functional pEC50 = 6.4 6.4 -194 4
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 85447 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 85447 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 2758 None 42 Human Functional pEC50 = 7.4 7.4 -50 10
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 2758 None 42 Human Functional pEC50 = 7.4 7.4 -50 10
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 2758 None 42 Human Functional pEC50 = 7.4 7.4 -50 10
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 2758 None 42 Human Functional pEC50 = 7.4 7.4 -50 10
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 8025 None 0 Human Functional pEC50 = 4.4 4.4 - 1
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 8025 None 0 Human Functional pEC50 = 4.4 4.4 - 1
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 192244 None 0 Human Functional pEC50 = 5.4 5.4 -17782 4
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 192244 None 0 Human Functional pEC50 = 5.4 5.4 -17782 4
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 192540 None 0 Human Functional pEC50 = 5.4 5.4 -2041 4
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 192540 None 0 Human Functional pEC50 = 5.4 5.4 -2041 4
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 2758 None 42 Human Functional pEC50 = 6.4 6.4 -50 10
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 2758 None 42 Human Functional pEC50 = 6.4 6.4 -50 10
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 2758 None 42 Human Functional pEC50 = 6.4 6.4 -50 10
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 2758 None 42 Human Functional pEC50 = 6.4 6.4 -50 10
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 157718 None 0 Human Functional pEC50 = 6.4 6.4 -6 4
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 157718 None 0 Human Functional pEC50 = 6.4 6.4 -6 4
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 85420 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 85420 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 83328 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 83328 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 79263 None 1 Human Functional pEC50 = 4.4 4.4 - 1
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 79263 None 1 Human Functional pEC50 = 4.4 4.4 - 1
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 191890 None 12 Human Functional pEC50 = 4.4 4.4 -1174 3
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 191890 None 12 Human Functional pEC50 = 4.4 4.4 -1174 3
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 162993 None 2 Human Functional pEC50 = 7.3 7.3 - 1
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 162993 None 2 Human Functional pEC50 = 7.3 7.3 - 1
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 157237 None 0 Human Functional pEC50 = 6.3 6.3 -6 4
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 157237 None 0 Human Functional pEC50 = 6.3 6.3 -6 4
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 122995 None 0 Human Functional pEC50 = 5.3 5.3 -47 2
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 122995 None 0 Human Functional pEC50 = 5.3 5.3 -47 2
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 69846 None 6 Human Functional pEC50 = 6.3 6.3 - 1
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 69846 None 6 Human Functional pEC50 = 6.3 6.3 - 1
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 191851 None 0 Human Functional pEC50 = 5.3 5.3 -5248 4
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 191851 None 0 Human Functional pEC50 = 5.3 5.3 -5248 4
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 106113 None 0 Human Functional pEC50 = 5.3 5.3 -501 3
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 106113 None 0 Human Functional pEC50 = 5.3 5.3 -501 3
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 164637 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 164637 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 66851 None 12 Human Functional pEC50 = 7.3 7.3 -213 5
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 66851 None 12 Human Functional pEC50 = 7.3 7.3 -213 5
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 192392 None 0 Human Functional pEC50 = 5.3 5.3 -8317 4
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 192392 None 0 Human Functional pEC50 = 5.3 5.3 -8317 4
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 191705 None 0 Human Functional pEC50 = 7.3 7.3 6 4
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 191705 None 0 Human Functional pEC50 = 7.3 7.3 6 4
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 283 None 61 Human Functional pEC50 = 7.3 7.3 -16 5
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 283 None 61 Human Functional pEC50 = 7.3 7.3 -16 5
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
60961.0 283 None 61 Human Functional pEC50 = 7.3 7.3 -16 5
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
90 283 None 61 Human Functional pEC50 = 7.3 7.3 -16 5
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 283 None 61 Human Functional pEC50 = 7.3 7.3 -16 5
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 283 None 61 Human Functional pEC50 = 7.3 7.3 -16 5
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 192235 None 0 Human Functional pEC50 = 6.3 6.3 1 3
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 192235 None 0 Human Functional pEC50 = 6.3 6.3 1 3
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 158460 None 0 Human Functional pEC50 = 6.3 6.3 -35 4
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 158460 None 0 Human Functional pEC50 = 6.3 6.3 -35 4
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 85421 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 85421 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 118585 None 0 Human Functional pEC50 = 6.3 6.3 -63 4
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 118585 None 0 Human Functional pEC50 = 6.3 6.3 -63 4
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 96386 None 27 Human Functional pEC50 = 5.3 5.3 -501 3
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 96386 None 27 Human Functional pEC50 = 5.3 5.3 -501 3
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 138151 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 138151 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 76963 None 2 Human Functional pEC50 = 4.3 4.3 -239 2
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 76963 None 2 Human Functional pEC50 = 4.3 4.3 -239 2
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 118576 None 0 Human Functional pEC50 = 6.3 6.3 -141 4
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 118576 None 0 Human Functional pEC50 = 6.3 6.3 -141 4
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 123707 None 0 Human Functional pEC50 = 6.3 6.3 -537 3
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 123707 None 0 Human Functional pEC50 = 6.3 6.3 -537 3
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 156927 None 0 Human Functional pEC50 = 6.2 6.2 -269 4
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 156927 None 0 Human Functional pEC50 = 6.2 6.2 -269 4
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 192266 None 0 Human Functional pEC50 = 8.2 8.2 45 4
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 192266 None 0 Human Functional pEC50 = 8.2 8.2 45 4
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 159129 None 0 Human Functional pEC50 = 7.2 7.2 -1 4
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 159129 None 0 Human Functional pEC50 = 7.2 7.2 -1 4
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 191737 None 0 Human Functional pEC50 = 6.2 6.2 -4897 4
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 191737 None 0 Human Functional pEC50 = 6.2 6.2 -4897 4
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 82702 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 82702 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 75507 None 0 Human Functional pEC50 = 5.2 5.2 -426 4
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 75507 None 0 Human Functional pEC50 = 5.2 5.2 -426 4
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 115499 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 115499 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 157348 None 0 Human Functional pEC50 = 6.2 6.2 -1 4
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 157348 None 0 Human Functional pEC50 = 6.2 6.2 -1 4
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 156254 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 156254 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 2758 None 42 Human Functional pEC50 = 7.2 7.2 -50 10
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 2758 None 42 Human Functional pEC50 = 7.2 7.2 -50 10
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 2758 None 42 Human Functional pEC50 = 7.2 7.2 -50 10
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 2758 None 42 Human Functional pEC50 = 7.2 7.2 -50 10
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 158244 None 0 Human Functional pEC50 = 6.2 6.2 -177 4
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 158244 None 0 Human Functional pEC50 = 6.2 6.2 -177 4
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 75517 None 0 Human Functional pEC50 = 5.2 5.2 -3 3
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 75517 None 0 Human Functional pEC50 = 5.2 5.2 -3 3
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 118579 None 0 Human Functional pEC50 = 6.2 6.2 -47 4
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 118579 None 0 Human Functional pEC50 = 6.2 6.2 -47 4
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 118580 None 0 Human Functional pEC50 = 6.2 6.2 -173 4
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 118580 None 0 Human Functional pEC50 = 6.2 6.2 -173 4
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 131441 None 0 Human Functional pEC50 = 6.2 6.2 -478 2
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 131441 None 0 Human Functional pEC50 = 6.2 6.2 -478 2
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 85405 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 85405 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 179602 None 0 Human Functional pEC50 = 6.2 6.2 -9 4
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 179602 None 0 Human Functional pEC50 = 6.2 6.2 -9 4
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 118675 None 0 Human Functional pEC50 = 5.2 5.2 -45 2
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 118675 None 0 Human Functional pEC50 = 5.2 5.2 -45 2
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 75508 None 0 Human Functional pEC50 = 6.1 6.1 -112 4
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 75508 None 0 Human Functional pEC50 = 6.1 6.1 -112 4
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 158098 None 0 Human Functional pEC50 = 7.1 7.1 -1 4
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 158098 None 0 Human Functional pEC50 = 7.1 7.1 -1 4
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 136436 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 136436 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 106116 None 0 Human Functional pEC50 = 6.1 6.1 -50 4
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 106116 None 0 Human Functional pEC50 = 6.1 6.1 -50 4
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 191170 None 0 Human Functional pEC50 = 5.1 5.1 -60255 4
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 191170 None 0 Human Functional pEC50 = 5.1 5.1 -60255 4
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 191460 None 0 Human Functional pEC50 = 5.1 5.1 -776 4
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 191460 None 0 Human Functional pEC50 = 5.1 5.1 -776 4
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 159831 None 4 Human Functional pEC50 = 4.1 4.1 -1 4
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 159831 None 4 Human Functional pEC50 = 4.1 4.1 -1 4
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 83255 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 83255 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 118587 None 0 Human Functional pEC50 = 6.1 6.1 -91 4
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 118587 None 0 Human Functional pEC50 = 6.1 6.1 -91 4
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 163682 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 163682 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 172193 None 0 Human Functional pEC50 = 6.1 6.1 -14 2
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 172193 None 0 Human Functional pEC50 = 6.1 6.1 -14 2
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 118699 None 0 Human Functional pEC50 = 6.1 6.1 -22 2
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 118699 None 0 Human Functional pEC50 = 6.1 6.1 -22 2
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 175836 None 0 Human Functional pEC50 = 6.1 6.1 -8 2
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 175836 None 0 Human Functional pEC50 = 6.1 6.1 -8 2
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 7799 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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 7799 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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 84710 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 84710 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 16143 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 16143 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 164772 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 164772 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 158399 None 0 Human Functional pEC50 = 7.0 7.0 1 4
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 158399 None 0 Human Functional pEC50 = 7.0 7.0 1 4
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 190097 None 0 Human Functional pEC50 = 6.0 6.0 -3090 4
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 190097 None 0 Human Functional pEC50 = 6.0 6.0 -3090 4
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 118697 None 0 Human Functional pEC50 = 6.0 6.0 -17 2
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 118697 None 0 Human Functional pEC50 = 6.0 6.0 -17 2
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 118673 None 0 Human Functional pEC50 = 5.0 5.0 -301 2
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 118673 None 0 Human Functional pEC50 = 5.0 5.0 -301 2
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 118674 None 0 Human Functional pEC50 = 5.0 5.0 -218 2
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 118674 None 0 Human Functional pEC50 = 5.0 5.0 -218 2
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 164526 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 164526 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 2758 None 42 Human Functional pEC50 = 7.0 7.0 -50 10
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 2758 None 42 Human Functional pEC50 = 7.0 7.0 -50 10
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 2758 None 42 Human Functional pEC50 = 7.0 7.0 -50 10
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 2758 None 42 Human Functional pEC50 = 7.0 7.0 -50 10
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 190540 None 0 Human Functional pEC50 = 7.0 7.0 -2 4
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 190540 None 0 Human Functional pEC50 = 7.0 7.0 -2 4
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 159831 None 4 Human Functional pEC50 = 7.0 7.0 -1 4
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 159831 None 4 Human Functional pEC50 = 7.0 7.0 -1 4
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 66851 None 12 Human Functional pEC50 = 6.0 6.0 -213 5
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 66851 None 12 Human Functional pEC50 = 6.0 6.0 -213 5
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+
24827290 156446 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 707 11 5 12 3.0 O=C(COc1ccc(Nc2nc(OCCc3c[nH]c4cc(Br)ccc34)nc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)N1CCCC1 10.1021/jm701442d
CHEMBL406594 156446 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 707 11 5 12 3.0 O=C(COc1ccc(Nc2nc(OCCc3c[nH]c4cc(Br)ccc34)nc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)N1CCCC1 10.1021/jm701442d
137634052 156736 None 0 Human Functional pEC50 = 7.0 7.0 6 3
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 830 15 7 14 5.7 Nc1nc(NCCCCCCNC(=O)c2ccc(-c3sc(N)c(C(=O)c4ccccc4)c3-c3cccc(C(F)(F)F)c3)cc2)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/acs.jmedchem.8b00047
CHEMBL4069296 156736 None 0 Human Functional pEC50 = 7.0 7.0 6 3
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 830 15 7 14 5.7 Nc1nc(NCCCCCCNC(=O)c2ccc(-c3sc(N)c(C(=O)c4ccccc4)c3-c3cccc(C(F)(F)F)c3)cc2)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/acs.jmedchem.8b00047
168276883 190309 None 0 Human Functional pEC50 = 6.0 6.0 -1862 4
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]4Oc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5174429 190309 None 0 Human Functional pEC50 = 6.0 6.0 -1862 4
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]4Oc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
155541051 173069 None 0 Human Functional pEC50 = 6.0 6.0 -251 2
Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assayAgonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay
ChEMBL 406 5 1 8 4.2 COC(=O)c1cccc(CSc2nc(N)c(C#N)c(-c3cccs3)c2C#N)c1 10.1021/acs.jmedchem.9b00106
CHEMBL4517597 173069 None 0 Human Functional pEC50 = 6.0 6.0 -251 2
Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assayAgonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay
ChEMBL 406 5 1 8 4.2 COC(=O)c1cccc(CSc2nc(N)c(C#N)c(-c3cccs3)c2C#N)c1 10.1021/acs.jmedchem.9b00106
16203669 85039 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 467 7 5 10 0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(OCCc4c[nH]c5ccccc45)nc32)[C@H](O)[C@@H]1O 10.1021/jm061278q
CHEMBL223845 85039 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 467 7 5 10 0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(OCCc4c[nH]c5ccccc45)nc32)[C@H](O)[C@@H]1O 10.1021/jm061278q
156018418 177898 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 500 7 3 11 1.8 Nc1nc(NCCN2CCN(c3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
CHEMBL4643397 177898 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 500 7 3 11 1.8 Nc1nc(NCCN2CCN(c3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
3284 3216 None 29 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
44185871 3216 None 29 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
5728 3216 None 29 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
CHEMBL483688 3216 None 29 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
12066874 206711 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 262 1 1 5 2.7 Oc1c(-c2ccccc2)nnc2nc3ccccc3n12 10.1021/jm201177b
CHEMBL7113 206711 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 262 1 1 5 2.7 Oc1c(-c2ccccc2)nnc2nc3ccccc3n12 10.1021/jm201177b
25207803 5687 None 0 Human Functional pIC50 = 8.9 8.9 10 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL1077943 5687 None 0 Human Functional pIC50 = 8.9 8.9 10 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
156821415 185579 None 0 Human Functional pIC50 = 8.8 8.8 5 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 398 4 1 8 3.0 Nc1nc(-c2ccccc2)c(-c2ccnnc2)c2nc(Cc3ncccc3F)nn12 10.1021/acsmedchemlett.1c00620
CHEMBL4862010 185579 None 0 Human Functional pIC50 = 8.8 8.8 5 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 398 4 1 8 3.0 Nc1nc(-c2ccccc2)c(-c2ccnnc2)c2nc(Cc3ncccc3F)nn12 10.1021/acsmedchemlett.1c00620
44186667 185765 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL486479 185765 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44186622 184335 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL483469 184335 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
10641040 9767 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 342 3 0 6 3.4 O=c1c(-c2ccco2)nnc2n(Cc3ccccc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL113518 9767 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 342 3 0 6 3.4 O=c1c(-c2ccco2)nnc2n(Cc3ccccc3)c3ccccc3n12 10.1021/jm201177b
11605883 79983 None 3 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL212625 79983 None 3 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44185933 186815 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 522 8 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(CCc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL488541 186815 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 522 8 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(CCc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
135493268 110549 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32481 110549 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
134142435 145426 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 341 4 2 7 3.7 Nc1nc(NCc2cccc(F)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3913413 145426 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 341 4 2 7 3.7 Nc1nc(NCc2cccc(F)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
45481749 200990 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 437 5 1 8 4.1 CCn1cc2c(nc(NC(=O)Cc3ccc4ccccc4c3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL578008 200990 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 437 5 1 8 4.1 CCn1cc2c(nc(NC(=O)Cc3ccc4ccccc4c3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
60156108 77014 None 0 Human Functional pIC50 = 6.0 6.0 -69 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 532 5 3 9 2.9 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccc(F)cc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2071046 77014 None 0 Human Functional pIC50 = 6.0 6.0 -69 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 532 5 3 9 2.9 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccc(F)cc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
135874429 95808 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 483 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4cccc(Cl)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL258473 95808 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 483 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4cccc(Cl)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
57429602 157331 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 releaseAntagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
CHEMBL4076435 157331 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 releaseAntagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
51039214 71547 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 342 5 3 9 1.5 NCC1CCC(CNc2nc(N)n3nc(-c4ccco4)nc3n2)CC1 10.1021/jm101349u
CHEMBL1927444 71547 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 342 5 3 9 1.5 NCC1CCC(CNc2nc(N)n3nc(-c4ccco4)nc3n2)CC1 10.1021/jm101349u
CHEMBL1962813 71547 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 342 5 3 9 1.5 NCC1CCC(CNc2nc(N)n3nc(-c4ccco4)nc3n2)CC1 10.1021/jm101349u
135522388 100166 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 543 9 2 9 2.9 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(Br)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL287529 100166 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 543 9 2 9 2.9 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(Br)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
46883206 6319 None 0 Human Functional pIC50 = 7.0 7.0 10 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 347 5 1 7 3.3 O=C(c1cccnc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1081873 6319 None 0 Human Functional pIC50 = 7.0 7.0 10 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 347 5 1 7 3.3 O=C(c1cccnc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
145436767 162573 None 0 Human Functional pIC50 = 7.0 7.0 -4365 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2cccnc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4167125 162573 None 0 Human Functional pIC50 = 7.0 7.0 -4365 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2cccnc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
136042340 71190 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 527 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Br)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955916 71190 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 527 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Br)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
10007115 116408 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 527 8 1 8 5.7 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL335950 116408 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 527 8 1 8 5.7 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
52947525 17666 None 0 Human Functional pIC50 = 6.0 6.0 -389 3
Antagonist activity at adenosine A2B receptor by cAMP assayAntagonist activity at adenosine A2B receptor by cAMP assay
ChEMBL 451 6 2 7 5.2 COc1ccc(Nc2c(-c3ccc4nccnc4c3)c(C)nn2-c2ccccc2)c(C(=O)O)c1 10.1016/j.bmcl.2010.07.095
CHEMBL1258397 17666 None 0 Human Functional pIC50 = 6.0 6.0 -389 3
Antagonist activity at adenosine A2B receptor by cAMP assayAntagonist activity at adenosine A2B receptor by cAMP assay
ChEMBL 451 6 2 7 5.2 COc1ccc(Nc2c(-c3ccc4nccnc4c3)c(C)nn2-c2ccccc2)c(C(=O)O)c1 10.1016/j.bmcl.2010.07.095
1922 205276 None 33 Rat Functional pIC50 = 6.0 6.0 -363 9
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O 10.1021/jm990499b
CHEMBL62350 205276 None 33 Rat Functional pIC50 = 6.0 6.0 -363 9
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O 10.1021/jm990499b
145960667 161576 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 285 4 2 6 2.6 Cc1nc2c(N)nc(NCCc3ccccc3)nc2s1 10.1016/j.bmc.2018.05.048
CHEMBL4127811 161576 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 285 4 2 6 2.6 Cc1nc2c(N)nc(NCCc3ccccc3)nc2s1 10.1016/j.bmc.2018.05.048
60156105 77012 None 0 Human Functional pIC50 = 6.0 6.0 -38 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 514 5 3 9 2.8 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2071044 77012 None 0 Human Functional pIC50 = 6.0 6.0 -38 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 514 5 3 9 2.8 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
45481761 200461 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 539 8 1 8 5.8 O=C(Cc1ccc(-c2ccccc2)cc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2009.05.038
CHEMBL573771 200461 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 539 8 1 8 5.8 O=C(Cc1ccc(-c2ccccc2)cc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2009.05.038
51051249 69309 None 3 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 217 1 2 8 -0.1 Nc1nc(N)n2nc(-c3ccco3)nc2n1 10.1021/jm101349u
CHEMBL1927632 69309 None 3 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 217 1 2 8 -0.1 Nc1nc(N)n2nc(-c3ccco3)nc2n1 10.1021/jm101349u
127046494 139832 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 307 3 2 7 2.4 Nc1nc(-c2ccco2)nc2cn(Cc3ccccc3O)nc12 10.1016/j.bmc.2016.04.048
CHEMBL3798383 139832 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 307 3 2 7 2.4 Nc1nc(-c2ccco2)nc2cn(Cc3ccccc3O)nc12 10.1016/j.bmc.2016.04.048
145436765 162890 None 0 Human Functional pIC50 = 7.0 7.0 -2511 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 343 5 2 8 3.6 Nc1nc(NCCc2cccs2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4172264 162890 None 0 Human Functional pIC50 = 7.0 7.0 -2511 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 343 5 2 8 3.6 Nc1nc(NCCc2cccs2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
136042342 71192 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 479 9 2 10 2.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(OC)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955918 71192 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 479 9 2 10 2.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(OC)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
135874414 96308 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 575 8 2 8 3.1 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(I)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL261027 96308 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 575 8 2 8 3.1 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(I)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
135443359 490 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 509 9 3 11 -0.1 CCCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)Nc3ccc(cc3)C(=O)O)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
441 490 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 509 9 3 11 -0.1 CCCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)Nc3ccc(cc3)C(=O)O)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
CHEMBL431703 490 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 509 9 3 11 -0.1 CCCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)Nc3ccc(cc3)C(=O)O)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
127036844 137645 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 397 7 2 8 4.0 c1ccc(CNc2nc(NCc3ccccc3)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.ejmech.2015.12.019
CHEMBL3754573 137645 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 397 7 2 8 4.0 c1ccc(CNc2nc(NCc3ccccc3)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.ejmech.2015.12.019
49797906 10748 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 467 7 1 7 4.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(F)c4)c3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171165 10748 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 467 7 1 7 4.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(F)c4)c3)sc12 10.1016/j.bmcl.2010.05.056
9930130 10805 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 387 5 1 5 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171897 10805 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 387 5 1 5 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
25231167 6219 None 0 Human Functional pIC50 = 6.9 6.9 20 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 313 5 2 6 2.4 CCNC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1081335 6219 None 0 Human Functional pIC50 = 6.9 6.9 20 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 313 5 2 6 2.4 CCNC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
16071896 58042 None 39 Human Functional pIC50 = 6.9 6.9 4 2
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISAAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISA
ChEMBL 335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2cccnc2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672627 58042 None 39 Human Functional pIC50 = 6.9 6.9 4 2
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISAAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISA
ChEMBL 335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2cccnc2)n1)C1CC1 10.1021/ml100249e
71508481 86310 None 6 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2b receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation by scintillation countingAntagonist activity at human adenosine A2b receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation by scintillation counting
ChEMBL 250 1 1 5 2.7 Nc1nc2ccccc2c2cc(-c3ccco3)nn12 10.1016/j.bmc.2012.10.031
CHEMBL2312725 86310 None 6 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2b receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation by scintillation countingAntagonist activity at human adenosine A2b receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation by scintillation counting
ChEMBL 250 1 1 5 2.7 Nc1nc2ccccc2c2cc(-c3ccco3)nn12 10.1016/j.bmc.2012.10.031
135529386 489 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 537 10 2 12 0.4 CCOC(=O)c1ccc(cc1)NC(=O)COc1c/c(=C\2/N=c3c(=N2)c(=O)n(c(=O)n3CCC)CCC)/n([nH]1)C 10.1021/jm0309654
440 489 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 537 10 2 12 0.4 CCOC(=O)c1ccc(cc1)NC(=O)COc1c/c(=C\2/N=c3c(=N2)c(=O)n(c(=O)n3CCC)CCC)/n([nH]1)C 10.1021/jm0309654
CHEMBL284615 489 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 537 10 2 12 0.4 CCOC(=O)c1ccc(cc1)NC(=O)COc1c/c(=C\2/N=c3c(=N2)c(=O)n(c(=O)n3CCC)CCC)/n([nH]1)C 10.1021/jm0309654
135546657 157790 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 509 10 2 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(NC(=O)Cc4ccc(OC)c(OC)c4)nn3C)nc2n(CCC)c1=O 10.1021/jm0309654
CHEMBL408186 157790 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 509 10 2 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(NC(=O)Cc4ccc(OC)c(OC)c4)nn3C)nc2n(CCC)c1=O 10.1021/jm0309654
145954471 162476 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 5 2 8 3.9 COc1cccc(CNc2nc(N)c3nc(-c4ccc(C)o4)sc3n2)c1 10.1016/j.ejmech.2018.06.020
CHEMBL4165484 162476 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 5 2 8 3.9 COc1cccc(CNc2nc(N)c3nc(-c4ccc(C)o4)sc3n2)c1 10.1016/j.ejmech.2018.06.020
11793210 185978 None 0 Rat Functional pIC50 = 5.9 5.9 -7 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 365 1 2 6 2.8 Cn1c(-c2ccc(F)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL48681 185978 None 0 Rat Functional pIC50 = 5.9 5.9 -7 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 365 1 2 6 2.8 Cn1c(-c2ccc(F)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
57395163 69811 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3cnn(C)c3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
CHEMBL1935756 69811 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3cnn(C)c3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
45482090 200412 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 463 7 1 8 4.6 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL573327 200412 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 463 7 1 8 4.6 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
118708225 113421 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 319 3 1 5 3.1 Nc1nc(Cc2ccccc2F)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
CHEMBL3317565 113421 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 319 3 1 5 3.1 Nc1nc(Cc2ccccc2F)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
45482075 200759 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 451 6 1 8 4.5 CCCn1cc2c(nc(NC(=O)Cc3cccc4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL576018 200759 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 451 6 1 8 4.5 CCCn1cc2c(nc(NC(=O)Cc3cccc4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
46882998 5643 None 0 Human Functional pIC50 = 5.9 5.9 -10 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 303 4 1 6 3.7 CCNc1nc(C(=O)c2ccc(C)s2)c2sccc2n1 10.1016/j.bmcl.2009.08.040
CHEMBL1077752 5643 None 0 Human Functional pIC50 = 5.9 5.9 -10 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 303 4 1 6 3.7 CCNc1nc(C(=O)c2ccc(C)s2)c2sccc2n1 10.1016/j.bmcl.2009.08.040
164627235 186519 None 0 Human Functional pIC50 = 6.9 6.9 -22 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 433 4 2 7 3.2 Cc1cc(-c2c(-c3ccc(F)cc3)nc(N)n3nc(CN4CCCCC4)nc23)c[nH]c1=O 10.1021/acsmedchemlett.1c00620
CHEMBL4876056 186519 None 0 Human Functional pIC50 = 6.9 6.9 -22 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 433 4 2 7 3.2 Cc1cc(-c2c(-c3ccc(F)cc3)nc(N)n3nc(CN4CCCCC4)nc23)c[nH]c1=O 10.1021/acsmedchemlett.1c00620
135493281 109682 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 483 8 2 8 2.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(Cl)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32225 109682 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 483 8 2 8 2.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(Cl)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
46883205 5852 None 0 Human Functional pIC50 = 5.9 5.9 -2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 376 6 1 7 3.9 COc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)cc1 10.1016/j.bmcl.2009.08.040
CHEMBL1079232 5852 None 0 Human Functional pIC50 = 5.9 5.9 -2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 376 6 1 7 3.9 COc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)cc1 10.1016/j.bmcl.2009.08.040
155554091 175795 None 0 Human Functional pIC50 = 7.9 7.9 -4 3
Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assayAntagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay
ChEMBL 375 5 2 7 3.1 N#Cc1c(N)nc(SCc2cccc(C(N)=O)c2)c(C#N)c1-c1ccco1 10.1021/acs.jmedchem.9b00106
CHEMBL4581984 175795 None 0 Human Functional pIC50 = 7.9 7.9 -4 3
Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assayAntagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay
ChEMBL 375 5 2 7 3.1 N#Cc1c(N)nc(SCc2cccc(C(N)=O)c2)c(C#N)c1-c1ccco1 10.1021/acs.jmedchem.9b00106
49798140 10874 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 484 9 1 7 3.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N(C)CCOC)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172442 10874 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 484 9 1 7 3.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N(C)CCOC)cc3)sc12 10.1016/j.bmcl.2010.05.056
25231166 6355 None 0 Human Functional pIC50 = 7.9 7.9 181 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 CC(Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
CHEMBL1082064 6355 None 0 Human Functional pIC50 = 7.9 7.9 181 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 CC(Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
54581142 60752 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 598 8 2 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NS(=O)(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760896 60752 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 598 8 2 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NS(=O)(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
145436761 162932 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 325 4 2 9 2.3 Nc1nc(NCc2cnccn2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4172818 162932 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 325 4 2 9 2.3 Nc1nc(NCc2cnccn2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
11826924 118809 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 479 8 1 9 4.0 O=C(COc1ccccc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL341777 118809 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 479 8 1 9 4.0 O=C(COc1ccccc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
10665407 190857 None 0 Rat Functional pIC50 = 5.9 5.9 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 348 1 2 7 2.1 Cn1c(-c2ccccn2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL51829 190857 None 0 Rat Functional pIC50 = 5.9 5.9 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 348 1 2 7 2.1 Cn1c(-c2ccccn2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
45482076 200558 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 391 4 1 8 2.6 Cn1cc2c(nc(NC(=O)Cc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL574483 200558 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 391 4 1 8 2.6 Cn1cc2c(nc(NC(=O)Cc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
46238067 8508 None 0 Human Functional pIC50 = 5.9 5.9 -229 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 420 5 2 5 5.2 O=C(Nc1ccccc1)Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12 10.1021/jm901785w
CHEMBL1094132 8508 None 0 Human Functional pIC50 = 5.9 5.9 -229 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 420 5 2 5 5.2 O=C(Nc1ccccc1)Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12 10.1021/jm901785w
46238066 8507 None 0 Human Functional pIC50 = 5.9 5.9 -173 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 439 5 1 5 5.4 O=C(Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12)c1cccc(Cl)c1 10.1021/jm901785w
CHEMBL1094131 8507 None 0 Human Functional pIC50 = 5.9 5.9 -173 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 439 5 1 5 5.4 O=C(Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12)c1cccc(Cl)c1 10.1021/jm901785w
145962529 161485 None 0 Human Functional pIC50 = 6.9 6.9 -1 3
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 291 4 2 7 2.7 Cc1nc2c(N)nc(NCCc3cccs3)nc2s1 10.1016/j.bmc.2018.05.048
CHEMBL4126427 161485 None 0 Human Functional pIC50 = 6.9 6.9 -1 3
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 291 4 2 7 2.7 Cc1nc2c(N)nc(NCCc3cccs3)nc2s1 10.1016/j.bmc.2018.05.048
15729970 137385 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 299 3 2 8 2.1 Nc1nc(NC2CCCCC2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2015.12.019
CHEMBL3752431 137385 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 299 3 2 8 2.1 Nc1nc(NC2CCCCC2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2015.12.019
145964662 164533 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 433 8 3 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4213768 164533 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 433 8 3 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
45481758 200802 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 379 4 1 9 2.5 Cn1cc2c(nc(NC(=O)Cc3ccsc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL576369 200802 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 379 4 1 9 2.5 Cn1cc2c(nc(NC(=O)Cc3ccsc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
45481619 200783 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 463 7 1 8 4.6 CC(C)CCn1cc2c(nc(NC(=O)Cc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL576185 200783 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 463 7 1 8 4.6 CC(C)CCn1cc2c(nc(NC(=O)Cc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
53248698 60743 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 6 1 6 4.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CCN(C(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760886 60743 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 6 1 6 4.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CCN(C(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
10544916 188416 None 0 Human Functional pIC50 = 7.9 7.9 15 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 337 1 2 7 2.3 Cn1c(-c2ccco2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL50051 188416 None 0 Human Functional pIC50 = 7.9 7.9 15 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 337 1 2 7 2.3 Cn1c(-c2ccco2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
145436762 162605 None 0 Human Functional pIC50 = 7.9 7.9 -3 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 327 5 2 8 3.2 Nc1nc(NCCc2ccco2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4167557 162605 None 0 Human Functional pIC50 = 7.9 7.9 -3 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 327 5 2 8 3.2 Nc1nc(NCCc2ccco2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
11027412 29637 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 493 9 1 9 4.4 O=C(COc1ccccc1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL138593 29637 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 493 9 1 9 4.4 O=C(COc1ccccc1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
135465785 488 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 496 8 2 12 0.0 CCCn1c2=N/C(=c/3\o[nH]c(c3)OCC(=O)Nc3ccc4c(c3)OCO4)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
439 488 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 496 8 2 12 0.0 CCCn1c2=N/C(=c/3\o[nH]c(c3)OCC(=O)Nc3ccc4c(c3)OCO4)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
CHEMBL32582 488 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 496 8 2 12 0.0 CCCn1c2=N/C(=c/3\o[nH]c(c3)OCC(=O)Nc3ccc4c(c3)OCO4)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
10665761 189385 None 0 Human Functional pIC50 = 6.9 6.9 3 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 353 3 2 6 2.7 CCC(O)(C#Cc1nc(N)c2nc(-c3cccc(F)c3)n(C)c2n1)CC 10.1021/jm990499b
CHEMBL51192 189385 None 0 Human Functional pIC50 = 6.9 6.9 3 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 353 3 2 6 2.7 CCC(O)(C#Cc1nc(N)c2nc(-c3cccc(F)c3)n(C)c2n1)CC 10.1021/jm990499b
145976828 163773 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 447 9 3 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4204683 163773 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 447 9 3 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
45482081 200385 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 497 7 1 8 5.3 CC(C)CCn1cc2c(nc(NC(=O)Cc3c(Cl)cccc3Cl)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL573089 200385 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 497 7 1 8 5.3 CC(C)CCn1cc2c(nc(NC(=O)Cc3c(Cl)cccc3Cl)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
156010667 177222 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP productionInhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP production
ChEMBL 556 9 4 11 2.0 Nc1nc(NCC2CCN(CC(=O)NCc3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
CHEMBL4633630 177222 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP productionInhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP production
ChEMBL 556 9 4 11 2.0 Nc1nc(NCC2CCN(CC(=O)NCc3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
46238068 8737 None 0 Human Functional pIC50 = 5.8 5.8 -181 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 450 6 2 6 5.2 COc1ccc(NC(=O)Nc2nc(-c3ccccc3)nc3nn(Cc4ccccc4)cc23)cc1 10.1021/jm901785w
CHEMBL1096078 8737 None 0 Human Functional pIC50 = 5.8 5.8 -181 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 450 6 2 6 5.2 COc1ccc(NC(=O)Nc2nc(-c3ccccc3)nc3nn(Cc4ccccc4)cc23)cc1 10.1021/jm901785w
46883157 5824 None 0 Human Functional pIC50 = 6.8 6.8 11 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 5 1 8 3.4 O=C(c1cncs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079044 5824 None 0 Human Functional pIC50 = 6.8 6.8 11 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 5 1 8 3.4 O=C(c1cncs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
46883155 5839 None 0 Human Functional pIC50 = 6.8 6.8 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 352 5 1 7 4.0 O=C(c1ccsc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079132 5839 None 0 Human Functional pIC50 = 6.8 6.8 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 352 5 1 7 4.0 O=C(c1ccsc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
10449783 9648 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 338 2 0 5 3.7 O=c1c(-c2ccccc2)nnc2n(-c3ccccc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL112756 9648 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 338 2 0 5 3.7 O=c1c(-c2ccccc2)nnc2n(-c3ccccc3)c3ccccc3n12 10.1021/jm201177b
10237267 10806 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 373 4 1 5 3.7 COc1ccc(N(C)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171898 10806 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 373 4 1 5 3.7 COc1ccc(N(C)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
136042350 71174 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 496 8 2 9 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955899 71174 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 496 8 2 9 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
10824674 207366 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 252 1 1 6 2.2 Oc1c(-c2ccco2)nnc2nc3ccccc3n12 10.1021/jm201177b
CHEMBL7608 207366 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 252 1 1 6 2.2 Oc1c(-c2ccco2)nnc2nc3ccccc3n12 10.1021/jm201177b
10895565 168555 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 445 8 1 9 3.8 CC(C)CCn1cc2c(nc(NC(=O)COc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
CHEMBL435022 168555 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 445 8 1 9 3.8 CC(C)CCn1cc2c(nc(NC(=O)COc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
10616023 101917 None 0 Human Functional pIC50 = 6.8 6.8 3 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 325 1 2 6 1.9 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC(C)(C)O)nc21 10.1021/jm990499b
CHEMBL300624 101917 None 0 Human Functional pIC50 = 6.8 6.8 3 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 325 1 2 6 1.9 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC(C)(C)O)nc21 10.1021/jm990499b
6448585 98392 None 6 Human Functional pIC50 = 5.8 5.8 -1513 3
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 412 8 0 8 2.9 CCCn1c(=O)c2c(nc(/C=C/c3ccc(OC)c(OC)c3)n2C)n(CCC)c1=O 10.1021/jm990499b
CHEMBL2311150 98392 None 6 Human Functional pIC50 = 5.8 5.8 -1513 3
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 412 8 0 8 2.9 CCCn1c(=O)c2c(nc(/C=C/c3ccc(OC)c(OC)c3)n2C)n(CCC)c1=O 10.1021/jm990499b
CHEMBL27508 98392 None 6 Human Functional pIC50 = 5.8 5.8 -1513 3
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 412 8 0 8 2.9 CCCn1c(=O)c2c(nc(/C=C/c3ccc(OC)c(OC)c3)n2C)n(CCC)c1=O 10.1021/jm990499b
45481757 200463 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 393 5 1 9 3.0 CCn1cc2c(nc(NC(=O)Cc3cccs3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL573779 200463 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 393 5 1 9 3.0 CCn1cc2c(nc(NC(=O)Cc3cccs3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
155554464 174706 None 0 Human Functional pIC50 = 6.8 6.8 -30 3
Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assayAntagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay
ChEMBL 362 5 2 7 3.5 N#Cc1c(N)nc(SCc2cccc(CO)c2)c(C#N)c1-c1ccco1 10.1021/acs.jmedchem.9b00106
CHEMBL4557250 174706 None 0 Human Functional pIC50 = 6.8 6.8 -30 3
Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assayAntagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay
ChEMBL 362 5 2 7 3.5 N#Cc1c(N)nc(SCc2cccc(CO)c2)c(C#N)c1-c1ccco1 10.1021/acs.jmedchem.9b00106
127045701 140057 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 339 3 1 6 3.7 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4Cl)cc3n2)o1 10.1016/j.bmc.2016.04.048
CHEMBL3799848 140057 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 339 3 1 6 3.7 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4Cl)cc3n2)o1 10.1016/j.bmc.2016.04.048
136002186 109757 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)n(C)n3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32281 109757 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)n(C)n3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
23656936 154986 None 0 Human Functional pIC50 = 5.8 5.8 -2630 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP accumulationAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP accumulation
ChEMBL 425 4 1 7 3.6 COc1ccc(C(=O)Nc2nc3ccccc3n3c(=O)c(-c4ccc(C)cc4)nn23)cc1 10.1021/jm0708376
CHEMBL400812 154986 None 0 Human Functional pIC50 = 5.8 5.8 -2630 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP accumulationAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP accumulation
ChEMBL 425 4 1 7 3.6 COc1ccc(C(=O)Nc2nc3ccccc3n3c(=O)c(-c4ccc(C)cc4)nn23)cc1 10.1021/jm0708376
60156107 77013 None 0 Human Functional pIC50 = 5.8 5.8 -33 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 542 7 3 9 3.2 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCCCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2071045 77013 None 0 Human Functional pIC50 = 5.8 5.8 -33 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 542 7 3 9 3.2 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCCCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
135874415 95947 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 527 8 2 8 3.3 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Br)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL259177 95947 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 527 8 2 8 3.3 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Br)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
156018055 178025 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP productionInhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP production
ChEMBL 570 10 4 11 2.1 Nc1nc(NCC2CCN(CC(=O)NCCc3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
CHEMBL4645283 178025 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP productionInhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP production
ChEMBL 570 10 4 11 2.1 Nc1nc(NCC2CCN(CC(=O)NCCc3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
49797748 10623 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 480 6 1 6 4.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCCCC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170135 10623 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 480 6 1 6 4.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCCCC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
49798137 10749 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 466 6 1 6 4.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCCC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171200 10749 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 466 6 1 6 4.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCCC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
46883208 5982 None 0 Human Functional pIC50 = 7.8 7.8 3 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 386 5 1 7 4.6 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2cc(Cl)sc12 10.1016/j.bmcl.2009.08.040
CHEMBL1080068 5982 None 0 Human Functional pIC50 = 7.8 7.8 3 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 386 5 1 7 4.6 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2cc(Cl)sc12 10.1016/j.bmcl.2009.08.040
54581142 60741 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 598 8 2 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@@H](NS(=O)(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760884 60741 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 598 8 2 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@@H](NS(=O)(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
44186717 184251 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 538 8 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL482855 184251 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 538 8 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
135465774 111542 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 467 8 2 8 2.4 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4cccc(F)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32770 111542 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 467 8 2 8 2.4 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4cccc(F)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
11793210 185978 None 0 Human Functional pIC50 = 6.8 6.8 7 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 365 1 2 6 2.8 Cn1c(-c2ccc(F)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL48681 185978 None 0 Human Functional pIC50 = 6.8 6.8 7 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 365 1 2 6 2.8 Cn1c(-c2ccc(F)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
10667322 101556 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 377 2 2 7 2.7 COc1cccc(-c2nc3c(N)nc(C#CC4(O)CCCCC4)nc3n2C)c1 10.1021/jm990499b
CHEMBL297949 101556 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 377 2 2 7 2.7 COc1cccc(-c2nc3c(N)nc(C#CC4(O)CCCCC4)nc3n2C)c1 10.1021/jm990499b
46883107 5834 None 0 Human Functional pIC50 = 7.8 7.8 5 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 1 7 4.9 Cc1ccc(C(=O)c2nc(NC(C)c3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1079115 5834 None 0 Human Functional pIC50 = 7.8 7.8 5 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 1 7 4.9 Cc1ccc(C(=O)c2nc(NC(C)c3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
54584124 60748 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 6 1 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)C3CCN(C(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760892 60748 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 6 1 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)C3CCN(C(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
10906943 116594 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 479 7 1 8 5.1 CC(C)CCn1cc2c(nc(NC(=O)Cc3cccc4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
CHEMBL336217 116594 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 479 7 1 8 5.1 CC(C)CCn1cc2c(nc(NC(=O)Cc3cccc4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
155520955 170673 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 351 2 4 9 1.2 Nc1nc(-c2cc(O)c(O)c(O)c2)cn2c(=O)n(-c3ccccc3)nc12 10.1021/acs.jmedchem.9b00778
CHEMBL4450312 170673 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 351 2 4 9 1.2 Nc1nc(-c2cc(O)c(O)c(O)c2)cn2c(=O)n(-c3ccccc3)nc12 10.1021/acs.jmedchem.9b00778
145964230 164106 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 461 10 3 6 2.6 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4208432 164106 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 461 10 3 6 2.6 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
60156106 76831 None 0 Human Functional pIC50 = 5.8 5.8 -75 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 528 6 3 9 2.8 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2069325 76831 None 0 Human Functional pIC50 = 5.8 5.8 -75 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 528 6 3 9 2.8 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
46883156 5823 None 0 Human Functional pIC50 = 6.8 6.8 4 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 5 1 8 3.4 O=C(c1nccs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079043 5823 None 0 Human Functional pIC50 = 6.8 6.8 4 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 5 1 8 3.4 O=C(c1nccs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
134147994 150198 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 351 6 2 7 4.0 Nc1nc(NCCCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3951103 150198 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 351 6 2 7 4.0 Nc1nc(NCCCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
46883110 5837 None 0 Human Functional pIC50 = 7.8 7.8 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 352 5 1 7 4.0 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079118 5837 None 0 Human Functional pIC50 = 7.8 7.8 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 352 5 1 7 4.0 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
25230181 5961 None 0 Human Functional pIC50 = 7.8 7.8 26 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 C[C@H](Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
CHEMBL1079894 5961 None 0 Human Functional pIC50 = 7.8 7.8 26 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 C[C@H](Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
54585058 60755 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 520 5 1 5 6.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)N3CCC(c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760900 60755 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 520 5 1 5 6.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)N3CCC(c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
134152846 153631 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 369 5 4 9 3.0 Nc1nc(NCCc2ccc(O)c(O)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3980049 153631 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 369 5 4 9 3.0 Nc1nc(NCCc2ccc(O)c(O)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
3284 3216 None 29 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
44185871 3216 None 29 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
5728 3216 None 29 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
CHEMBL483688 3216 None 29 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
136042335 71186 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 490 8 2 10 1.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc(=O)c5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955911 71186 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 490 8 2 10 1.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc(=O)c5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
11762982 26213 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 513 7 1 8 5.3 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL135719 26213 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 513 7 1 8 5.3 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
145960536 161722 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 271 3 2 6 2.6 Cc1nc2c(N)nc(NCc3ccccc3)nc2s1 10.1016/j.bmc.2018.05.048
CHEMBL4130003 161722 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 271 3 2 6 2.6 Cc1nc2c(N)nc(NCc3ccccc3)nc2s1 10.1016/j.bmc.2018.05.048
45482085 200561 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 421 7 1 9 3.8 CCCCn1cc2c(nc(NC(=O)Cc3cccs3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL574489 200561 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 421 7 1 9 3.8 CCCCn1cc2c(nc(NC(=O)Cc3cccs3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
135529391 481 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 555 10 2 10 1.5 CCCn1c2=N/C(=c\3/cc([nH]n3C)NC(=O)Cc3ccc(cc3)OCc3ccccc3)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
438 481 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 555 10 2 10 1.5 CCCn1c2=N/C(=c\3/cc([nH]n3C)NC(=O)Cc3ccc(cc3)OCc3ccccc3)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
CHEMBL285900 481 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 555 10 2 10 1.5 CCCn1c2=N/C(=c\3/cc([nH]n3C)NC(=O)Cc3ccc(cc3)OCc3ccccc3)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
134157761 154118 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 289 5 2 7 3.1 CCCCNc1nc(N)c2nc(-c3ccco3)sc2n1 10.1021/acs.jmedchem.6b01068
CHEMBL3984266 154118 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 289 5 2 7 3.1 CCCCNc1nc(N)c2nc(-c3ccco3)sc2n1 10.1021/acs.jmedchem.6b01068
135874430 160224 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 517 8 2 8 3.8 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Cl)c(Cl)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL410895 160224 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 517 8 2 8 3.8 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Cl)c(Cl)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
25231168 5700 None 0 Human Functional pIC50 = 6.7 6.7 32 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 339 4 1 6 2.9 O=C(c1nc(NCc2cccnc2)nc2ccsc12)N1CCCC1 10.1016/j.bmcl.2009.08.040
CHEMBL1078030 5700 None 0 Human Functional pIC50 = 6.7 6.7 32 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 339 4 1 6 2.9 O=C(c1nc(NCc2cccnc2)nc2ccsc12)N1CCCC1 10.1016/j.bmcl.2009.08.040
49797856 10855 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 401 5 1 5 4.5 COc1ccc(N(C(C)=O)C(C)C)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172270 10855 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 401 5 1 5 4.5 COc1ccc(N(C(C)=O)C(C)C)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
49797771 10859 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 435 6 1 7 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4ccnc4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172275 10859 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 435 6 1 7 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4ccnc4)cc3)sc12 10.1016/j.bmcl.2010.05.056
49797773 10861 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 490 8 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(CN(C)S(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172277 10861 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 490 8 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(CN(C)S(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
46883106 5685 None 0 Human Functional pIC50 = 7.7 7.7 6 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 1 7 4.9 Cc1ccc(C(=O)c2nc(NC(C)c3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1077915 5685 None 0 Human Functional pIC50 = 7.7 7.7 6 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 1 7 4.9 Cc1ccc(C(=O)c2nc(NC(C)c3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
25230948 6037 None 0 Human Functional pIC50 = 7.7 7.7 3 4
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 395 7 2 8 4.4 CCNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
CHEMBL1080421 6037 None 0 Human Functional pIC50 = 7.7 7.7 3 4
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 395 7 2 8 4.4 CCNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
54583134 63129 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 8 2 6 5.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CC[C@H](NCc4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760891 63129 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 8 2 6 5.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CC[C@H](NCc4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1789250 63129 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 8 2 6 5.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CC[C@H](NCc4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
11080491 22804 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 429 7 1 8 4.0 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
CHEMBL132806 22804 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 429 7 1 8 4.0 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
10597086 210542 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor at 50 uMInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor at 50 uM
ChEMBL 399 6 2 7 3.4 O=C(O)CCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
CHEMBL97753 210542 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor at 50 uMInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor at 50 uM
ChEMBL 399 6 2 7 3.4 O=C(O)CCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
52948788 17737 None 0 Human Functional pIC50 = 4.7 4.7 -2137 2
Antagonist activity at adenosine A2B receptor by cAMP assayAntagonist activity at adenosine A2B receptor by cAMP assay
ChEMBL 489 5 2 6 6.3 Cc1ccccc1-n1nc(C(F)(F)F)c(-c2ccc3nccnc3c2)c1Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.07.095
CHEMBL1258622 17737 None 0 Human Functional pIC50 = 4.7 4.7 -2137 2
Antagonist activity at adenosine A2B receptor by cAMP assayAntagonist activity at adenosine A2B receptor by cAMP assay
ChEMBL 489 5 2 6 6.3 Cc1ccccc1-n1nc(C(F)(F)F)c(-c2ccc3nccnc3c2)c1Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.07.095
136042345 71195 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 585 8 2 9 4.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C(F)(F)F)cc(C(F)(F)F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955921 71195 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 585 8 2 9 4.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C(F)(F)F)cc(C(F)(F)F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
56964460 74749 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 362 2 0 6 3.9 O=c1c(-c2ccco2)nnc2n(-c3ccc(Cl)cc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL2030704 74749 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 362 2 0 6 3.9 O=c1c(-c2ccco2)nnc2n(-c3ccc(Cl)cc3)c3ccccc3n12 10.1021/jm201177b
44186668 191619 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 562 6 2 7 2.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL519390 191619 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 562 6 2 7 2.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
56964459 74748 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 372 2 0 5 4.4 O=c1c(-c2ccccc2)nnc2n(-c3ccc(Cl)cc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL2030703 74748 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 372 2 0 5 4.4 O=c1c(-c2ccccc2)nnc2n(-c3ccc(Cl)cc3)c3ccccc3n12 10.1021/jm201177b
56964461 74750 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 366 4 0 5 4.0 O=c1c(-c2ccccc2)nnc2n(CCc3ccccc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL2030705 74750 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 366 4 0 5 4.0 O=c1c(-c2ccccc2)nnc2n(CCc3ccccc3)c3ccccc3n12 10.1021/jm201177b
56924646 71196 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 332 5 2 7 0.4 CCCn1c(=O)c2[nH]c(-c3cc(=O)[nH]n3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955922 71196 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 332 5 2 7 0.4 CCCn1c(=O)c2[nH]c(-c3cc(=O)[nH]n3C)nc2n(CCC)c1=O 10.1021/jm201292w
53242165 60756 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 584 6 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)N3CCC(S(=O)(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760901 60756 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 584 6 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)N3CCC(S(=O)(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
10539663 206690 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 266 1 0 6 1.8 Cn1c2ccccc2n2c(=O)c(-c3ccco3)nnc12 10.1021/jm201177b
CHEMBL7098 206690 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 266 1 0 6 1.8 Cn1c2ccccc2n2c(=O)c(-c3ccco3)nnc12 10.1021/jm201177b
135874421 169061 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 477 8 2 8 3.1 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(C)c(C)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL438938 169061 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 477 8 2 8 3.1 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(C)c(C)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
51050845 69285 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 374 6 3 10 1.7 CC(C)(C)OC(=O)NCCCNc1nc(N)n2nc(-c3ccco3)nc2n1 10.1021/jm101349u
CHEMBL1927428 69285 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 374 6 3 10 1.7 CC(C)(C)OC(=O)NCCCNc1nc(N)n2nc(-c3ccco3)nc2n1 10.1021/jm101349u
60155796 76994 None 0 Human Functional pIC50 = 5.7 5.7 -16 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 471 5 2 9 3.1 Cn1cc2c(nc(NC(=O)NC3CCN(Cc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2070886 76994 None 0 Human Functional pIC50 = 5.7 5.7 -16 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 471 5 2 9 3.1 Cn1cc2c(nc(NC(=O)NC3CCN(Cc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
145962364 161542 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 277 3 2 7 2.7 Cc1nc2c(N)nc(NCc3cccs3)nc2s1 10.1016/j.bmc.2018.05.048
CHEMBL4127395 161542 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 277 3 2 7 2.7 Cc1nc2c(N)nc(NCc3cccs3)nc2s1 10.1016/j.bmc.2018.05.048
49797747 10622 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 482 6 1 7 3.4 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCOCC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170134 10622 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 482 6 1 7 3.4 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCOCC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
49797749 10624 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 435 6 1 7 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4cccn4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170136 10624 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 435 6 1 7 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4cccn4)cc3)sc12 10.1016/j.bmcl.2010.05.056
46911060 10651 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccnn3C)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170367 10651 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccnn3C)sc12 10.1016/j.bmcl.2010.05.056
49798138 10674 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 426 6 2 6 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)NC)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170582 10674 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 426 6 2 6 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)NC)cc3)sc12 10.1016/j.bmcl.2010.05.056
49797903 10745 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 359 5 2 6 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cn[nH]c3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171162 10745 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 359 5 2 6 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cn[nH]c3)sc12 10.1016/j.bmcl.2010.05.056
46911060 10651 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccnn3C)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1170367 10651 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccnn3C)sc12 10.1016/j.bmcl.2011.02.053
10994216 195980 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 463 7 1 8 4.2 O=C(Cc1ccccc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL541455 195980 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 463 7 1 8 4.2 O=C(Cc1ccccc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
1922 205276 None 33 Human Functional pIC50 = 6.7 6.7 -97 9
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O 10.1021/jm990499b
CHEMBL62350 205276 None 33 Human Functional pIC50 = 6.7 6.7 -97 9
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O 10.1021/jm990499b
135874431 96309 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 463 8 2 8 2.8 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(C)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL261028 96309 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 463 8 2 8 2.8 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(C)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
60154739 77016 None 0 Human Functional pIC50 = 5.7 5.7 -177 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 528 5 3 9 3.1 Cc1ccc(CNC(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)cc1 10.1021/jm300323t
CHEMBL2071048 77016 None 0 Human Functional pIC50 = 5.7 5.7 -177 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 528 5 3 9 3.1 Cc1ccc(CNC(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)cc1 10.1021/jm300323t
60154835 77228 None 0 Human Functional pIC50 = 5.7 5.7 -17 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 507 3 2 10 1.2 CN1CCN(C(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)CC1 10.1021/jm300323t
CHEMBL2071051 77228 None 0 Human Functional pIC50 = 5.7 5.7 -17 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 507 3 2 10 1.2 CN1CCN(C(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)CC1 10.1021/jm300323t
CHEMBL2079181 77228 None 0 Human Functional pIC50 = 5.7 5.7 -17 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 507 3 2 10 1.2 CN1CCN(C(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)CC1 10.1021/jm300323t
46883159 5841 None 0 Human Functional pIC50 = 6.7 6.7 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 360 5 1 6 4.2 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)cc1 10.1016/j.bmcl.2009.08.040
CHEMBL1079142 5841 None 0 Human Functional pIC50 = 6.7 6.7 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 360 5 1 6 4.2 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)cc1 10.1016/j.bmcl.2009.08.040
136042337 71187 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 520 10 1 12 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4noc(-c5cccc(OC)c5)n4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955913 71187 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 520 10 1 12 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4noc(-c5cccc(OC)c5)n4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
136042330 71180 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 506 9 3 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(=O)O)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955905 71180 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 506 9 3 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(=O)O)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
10544916 188416 None 0 Rat Functional pIC50 = 6.7 6.7 -15 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 337 1 2 7 2.3 Cn1c(-c2ccco2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL50051 188416 None 0 Rat Functional pIC50 = 6.7 6.7 -15 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 337 1 2 7 2.3 Cn1c(-c2ccco2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
9839545 137399 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 307 4 2 8 2.0 Nc1nc(NCc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2015.12.019
CHEMBL3752514 137399 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 307 4 2 8 2.0 Nc1nc(NCc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2015.12.019
135874422 159178 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 509 10 2 10 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(OC)c(OC)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL409736 159178 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 509 10 2 10 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(OC)c(OC)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
49797796 10620 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 391 4 1 4 4.7 CCN(C(C)=O)c1ccc(Cl)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170130 10620 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 391 4 1 4 4.7 CCN(C(C)=O)c1ccc(Cl)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
49797878 10786 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 415 6 1 5 4.7 COc1ccc(N(CC(C)C)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171718 10786 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 415 6 1 5 4.7 COc1ccc(N(CC(C)C)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
9842054 184046 None 0 Human Functional pIC50 = 7.6 7.6 10 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 365 1 2 6 2.8 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL48153 184046 None 0 Human Functional pIC50 = 7.6 7.6 10 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 365 1 2 6 2.8 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
44186719 186022 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 552 7 2 9 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL486893 186022 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 552 7 2 9 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
49797854 10853 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 409 5 1 5 4.3 COc1ccc(N(C(C)=O)C(F)F)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172268 10853 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 409 5 1 5 4.3 COc1ccc(N(C(C)=O)C(F)F)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
136042348 71200 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 508 9 2 10 2.5 CCCn1c(=O)c2[nH]c(-c3cc(OCC(=O)Nc4ccc5c(c4)OCO5)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955926 71200 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 508 9 2 10 2.5 CCCn1c(=O)c2[nH]c(-c3cc(OCC(=O)Nc4ccc5c(c4)OCO5)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
145962202 161632 None 0 Human Functional pIC50 = 5.6 5.6 -64 3
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 2 7 4.0 COc1cccc(CNc2nc(N)c3nc(-c4ccccc4)sc3n2)c1 10.1016/j.bmc.2018.05.048
CHEMBL4128596 161632 None 0 Human Functional pIC50 = 5.6 5.6 -64 3
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 2 7 4.0 COc1cccc(CNc2nc(N)c3nc(-c4ccccc4)sc3n2)c1 10.1016/j.bmc.2018.05.048
156821341 186522 None 0 Human Functional pIC50 = 7.6 7.6 -2 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 461 4 2 9 2.5 Cn1cc(-c2c(-c3ccc(F)cc3)nc(N)n3nc([C@H](O)c4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
CHEMBL4876080 186522 None 0 Human Functional pIC50 = 7.6 7.6 -2 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 461 4 2 9 2.5 Cn1cc(-c2c(-c3ccc(F)cc3)nc(N)n3nc([C@H](O)c4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
134138275 147841 None 0 Human Functional pIC50 = 7.6 7.6 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 339 4 3 8 3.2 Nc1nc(NCc2cccc(O)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3932413 147841 None 0 Human Functional pIC50 = 7.6 7.6 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 339 4 3 8 3.2 Nc1nc(NCc2cccc(O)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
60155712 76989 None 0 Human Functional pIC50 = 5.6 5.6 -9 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 381 3 3 9 1.1 Cn1cc2c(nc(NC(=O)NC3CCNCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2070880 76989 None 0 Human Functional pIC50 = 5.6 5.6 -9 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 381 3 3 9 1.1 Cn1cc2c(nc(NC(=O)NC3CCNCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
11497239 11816 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 390 3 2 8 1.7 Cn1cc2c(nc(NC(=O)Nc3ccc[n+](C)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
CHEMBL1181982 11816 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 390 3 2 8 1.7 Cn1cc2c(nc(NC(=O)Nc3ccc[n+](C)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
CHEMBL203660 11816 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 390 3 2 8 1.7 Cn1cc2c(nc(NC(=O)Nc3ccc[n+](C)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
118708238 113431 None 0 Human Functional pIC50 = 6.6 6.6 -57 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 345 5 2 6 3.3 Nc1nc(CCCc2ccccc2O)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
CHEMBL3317578 113431 None 0 Human Functional pIC50 = 6.6 6.6 -57 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 345 5 2 6 3.3 Nc1nc(CCCc2ccccc2O)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
134142611 145973 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 3 8 3.3 Nc1nc(NCCc2cccc(O)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3917647 145973 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 3 8 3.3 Nc1nc(NCCc2cccc(O)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
11625796 74727 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 414 3 2 9 3.7 Cn1cc2c(nc(NC(=O)Nc3cc4ccccc4o3)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
CHEMBL203054 74727 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 414 3 2 9 3.7 Cn1cc2c(nc(NC(=O)Nc3cc4ccccc4o3)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
11733496 24913 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 477 8 1 8 4.5 O=C(Cc1ccccc1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL134566 24913 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 477 8 1 8 4.5 O=C(Cc1ccccc1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
9842054 184046 None 0 Rat Functional pIC50 = 6.6 6.6 -10 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 365 1 2 6 2.8 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL48153 184046 None 0 Rat Functional pIC50 = 6.6 6.6 -10 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 365 1 2 6 2.8 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
57391653 69800 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 358 5 1 7 3.6 Nc1nc2cn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
CHEMBL1935746 69800 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 358 5 1 7 3.6 Nc1nc2cn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
25231169 5516 None 0 Human Functional pIC50 = 6.6 6.6 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 325 5 2 6 2.6 O=C(NC1CC1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1076503 5516 None 0 Human Functional pIC50 = 6.6 6.6 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 325 5 2 6 2.6 O=C(NC1CC1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
136002248 71182 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 564 8 2 9 4.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(Cl)cc(C(F)(F)F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955907 71182 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 564 8 2 9 4.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(Cl)cc(C(F)(F)F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
54585057 60753 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 562 7 2 6 5.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@@H](NC(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760898 60753 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 562 7 2 6 5.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@@H](NC(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
11560202 74728 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 391 3 2 9 1.5 Cn1cc2c(nc(NC(=O)Nc3ccc[n+]([O-])c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
CHEMBL203060 74728 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 391 3 2 9 1.5 Cn1cc2c(nc(NC(=O)Nc3ccc[n+]([O-])c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
145977111 163860 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 617 9 3 7 3.9 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4205635 163860 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 617 9 3 7 3.9 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
145962355 161530 None 0 Human Functional pIC50 = 5.6 5.6 -416 3
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 2 7 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3ccccc3)sc2n1 10.1016/j.bmc.2018.05.048
CHEMBL4127213 161530 None 0 Human Functional pIC50 = 5.6 5.6 -416 3
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 2 7 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3ccccc3)sc2n1 10.1016/j.bmc.2018.05.048
135874428 167661 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 479 9 2 9 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4cccc(OC)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL430044 167661 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 479 9 2 9 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4cccc(OC)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
57403905 69817 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 345 4 1 8 2.6 Nc1nc2cn(CCc3ccccc3)nc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
CHEMBL1935762 69817 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 345 4 1 8 2.6 Nc1nc2cn(CCc3ccccc3)nc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
136042346 71198 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 461 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955924 71198 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 461 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
46238064 8512 None 0 Human Functional pIC50 = 6.6 6.6 -5 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 405 5 1 5 4.8 O=C(Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12)c1ccccc1 10.1021/jm901785w
CHEMBL1094143 8512 None 0 Human Functional pIC50 = 6.6 6.6 -5 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 405 5 1 5 4.8 O=C(Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12)c1ccccc1 10.1021/jm901785w
145972655 163125 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 369 5 2 8 4.0 COc1cccc(CNc2nc(N)c3nc(-c4cccs4)sc3n2)c1 10.1016/j.ejmech.2018.06.020
CHEMBL4175878 163125 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 369 5 2 8 4.0 COc1cccc(CNc2nc(N)c3nc(-c4cccs4)sc3n2)c1 10.1016/j.ejmech.2018.06.020
49797794 10591 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 394 5 1 6 3.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C#N)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1169934 10591 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 394 5 1 6 3.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C#N)cc3)sc12 10.1016/j.bmcl.2010.05.056
49797750 10757 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 437 6 1 9 2.9 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4cnnn4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171349 10757 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 437 6 1 9 2.9 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4cnnn4)cc3)sc12 10.1016/j.bmcl.2010.05.056
49797772 10860 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 466 7 1 6 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(CN4CCCC4=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172276 10860 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 466 7 1 6 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(CN4CCCC4=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
156017813 177932 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP productionInhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP production
ChEMBL 402 5 3 9 2.2 Nc1nc(NCc2ccc(S(N)(=O)=O)cc2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
CHEMBL4643898 177932 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP productionInhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP production
ChEMBL 402 5 3 9 2.2 Nc1nc(NCc2ccc(S(N)(=O)=O)cc2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
54585057 60751 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 562 7 2 6 5.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NC(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760895 60751 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 562 7 2 6 5.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NC(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
11684980 12317 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 390 3 2 8 1.7 Cn1cc2c(nc(NC(=O)Nc3cccc[n+]3C)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
CHEMBL1185010 12317 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 390 3 2 8 1.7 Cn1cc2c(nc(NC(=O)Nc3cccc[n+]3C)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
CHEMBL383689 12317 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 390 3 2 8 1.7 Cn1cc2c(nc(NC(=O)Nc3cccc[n+]3C)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
164611330 185190 None 0 Human Functional pIC50 = 6.6 6.6 -380 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 418 4 2 6 3.4 Nc1nc(-c2ccc(F)cc2)c(-c2ccc(=O)[nH]c2)c2nc(CCC(F)(F)F)nn12 10.1021/acsmedchemlett.1c00620
CHEMBL4855908 185190 None 0 Human Functional pIC50 = 6.6 6.6 -380 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 418 4 2 6 3.4 Nc1nc(-c2ccc(F)cc2)c(-c2ccc(=O)[nH]c2)c2nc(CCC(F)(F)F)nn12 10.1021/acsmedchemlett.1c00620
134138961 147712 None 0 Human Functional pIC50 = 6.6 6.6 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1ccc(CNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1 10.1021/acs.jmedchem.6b01068
CHEMBL3931329 147712 None 0 Human Functional pIC50 = 6.6 6.6 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1ccc(CNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1 10.1021/acs.jmedchem.6b01068
46883071 5695 None 0 Human Functional pIC50 = 6.5 6.5 -1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 4 1 7 3.9 Cc1ccc(C(=O)c2nc(NC(=O)c3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078001 5695 None 0 Human Functional pIC50 = 6.5 6.5 -1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 4 1 7 3.9 Cc1ccc(C(=O)c2nc(NC(=O)c3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
49797904 10746 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(C)c3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171163 10746 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(C)c3)sc12 10.1016/j.bmcl.2010.05.056
127046050 140178 None 0 Human Functional pIC50 = 6.5 6.5 -45 3
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 335 4 1 7 3.0 COc1cccc(Cn2cc3nc(-c4ccc(C)o4)nc(N)c3n2)c1 10.1016/j.bmc.2016.04.048
CHEMBL3800587 140178 None 0 Human Functional pIC50 = 6.5 6.5 -45 3
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 335 4 1 7 3.0 COc1cccc(Cn2cc3nc(-c4ccc(C)o4)nc(N)c3n2)c1 10.1016/j.bmc.2016.04.048
56964576 74752 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 372 2 0 5 4.4 O=c1c(-c2ccccc2)nnc2n(-c3ccccc3)c3ccc(Cl)cc3n12 10.1021/jm201177b
CHEMBL2030707 74752 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 372 2 0 5 4.4 O=c1c(-c2ccccc2)nnc2n(-c3ccccc3)c3ccc(Cl)cc3n12 10.1021/jm201177b
44186626 184715 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 526 7 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL484900 184715 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 526 7 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
25207803 5687 None 0 Human Functional pIC50 = 8.5 8.5 10 4
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
CHEMBL1077943 5687 None 0 Human Functional pIC50 = 8.5 8.5 10 4
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
44186669 185903 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL486688 185903 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44186581 3205 None 21 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl 10.1021/jm900413e
6561 3205 None 21 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl 10.1021/jm900413e
CHEMBL482436 3205 None 21 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl 10.1021/jm900413e
53248699 63123 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 8 2 6 6.0 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NCc4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760897 63123 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 8 2 6 6.0 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NCc4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1789197 63123 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 8 2 6 6.0 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NCc4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
4355631 193878 None 1 Human Functional pIC50 = 5.5 5.5 1 3
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 320 2 0 6 2.2 COC(=O)C1=C2C=CN(C)C=C2c2nc(-c3ccccc3)nn2C1 10.1021/jm990499b
CHEMBL52735 193878 None 1 Human Functional pIC50 = 5.5 5.5 1 3
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 320 2 0 6 2.2 COC(=O)C1=C2C=CN(C)C=C2c2nc(-c3ccccc3)nn2C1 10.1021/jm990499b
25230180 5960 None 0 Human Functional pIC50 = 5.5 5.5 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 C[C@@H](Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
CHEMBL1079893 5960 None 0 Human Functional pIC50 = 5.5 5.5 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 C[C@@H](Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
25231170 5517 None 0 Human Functional pIC50 = 6.5 6.5 8 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 327 5 2 6 2.8 CC(C)NC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1076504 5517 None 0 Human Functional pIC50 = 6.5 6.5 8 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 327 5 2 6 2.8 CC(C)NC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
57396935 69807 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 255 1 1 8 0.9 Cn1ncc2nc(N)n3nc(-c4ccco4)nc3c21 10.1016/j.bmc.2011.11.037
CHEMBL1935752 69807 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 255 1 1 8 0.9 Cn1ncc2nc(N)n3nc(-c4ccco4)nc3c21 10.1016/j.bmc.2011.11.037
132991405 151152 None 3 Human Functional pIC50 = 6.5 6.5 -6165 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1ccccc1CNc1nc(N)c2nc(-c3ccco3)sc2n1 10.1021/acs.jmedchem.6b01068
CHEMBL3958838 151152 None 3 Human Functional pIC50 = 6.5 6.5 -6165 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1ccccc1CNc1nc(N)c2nc(-c3ccco3)sc2n1 10.1021/acs.jmedchem.6b01068
118708239 113432 None 0 Human Functional pIC50 = 6.5 6.5 -109 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 345 5 2 6 3.3 Nc1nc(CCCc2cccc(O)c2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
CHEMBL3317579 113432 None 0 Human Functional pIC50 = 6.5 6.5 -109 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 345 5 2 6 3.3 Nc1nc(CCCc2cccc(O)c2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
57391694 69809 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 345 4 1 8 2.6 Nc1nc2cnn(CCc3ccccc3)c2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
CHEMBL1935754 69809 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 345 4 1 8 2.6 Nc1nc2cnn(CCc3ccccc3)c2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
57403904 69812 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 432 6 2 9 3.8 CCCn1ncc2nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc3c21 10.1016/j.bmc.2011.11.037
CHEMBL1935757 69812 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 432 6 2 9 3.8 CCCn1ncc2nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc3c21 10.1016/j.bmc.2011.11.037
57398676 69818 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 359 5 1 8 2.9 Nc1nc2cn(CCCc3ccccc3)nc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
CHEMBL1935763 69818 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 359 5 1 8 2.9 Nc1nc2cn(CCCc3ccccc3)nc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
25230949 6007 None 0 Human Functional pIC50 = 7.5 7.5 15 4
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 5 2 8 3.6 Nc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
CHEMBL1080241 6007 None 0 Human Functional pIC50 = 7.5 7.5 15 4
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 5 2 8 3.6 Nc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
136042333 71184 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 514 8 2 9 3.4 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)c(F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955909 71184 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 514 8 2 9 3.4 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)c(F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
134147788 150079 None 0 Human Functional pIC50 = 7.5 7.5 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 323 4 2 7 3.5 Nc1nc(NCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3950142 150079 None 0 Human Functional pIC50 = 7.5 7.5 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 323 4 2 7 3.5 Nc1nc(NCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
71601630 86956 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting methodAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting method
ChEMBL 225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1016/j.ejmech.2015.11.015
CHEMBL2322916 86956 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting methodAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting method
ChEMBL 225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1016/j.ejmech.2015.11.015
71601630 86956 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1016/j.bmc.2016.04.048
CHEMBL2322916 86956 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1016/j.bmc.2016.04.048
71601630 86956 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1016/j.ejmech.2014.07.060
CHEMBL2322916 86956 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1016/j.ejmech.2014.07.060
44408316 75431 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 391 3 2 9 1.5 Cn1cc2c(nc(NC(=O)Nc3cccc[n+]3[O-])n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
CHEMBL203998 75431 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 391 3 2 9 1.5 Cn1cc2c(nc(NC(=O)Nc3cccc[n+]3[O-])n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
10687707 110413 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 328 2 0 6 3.3 O=c1c(-c2ccco2)nnc2n(-c3ccccc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL324100 110413 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 328 2 0 6 3.3 O=c1c(-c2ccco2)nnc2n(-c3ccccc3)c3ccccc3n12 10.1021/jm201177b
11716665 2281 None 30 Human Functional pIC50 = 6.5 6.5 1 2
Activity at human A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISAActivity at human A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
5617 2281 None 30 Human Functional pIC50 = 6.5 6.5 1 2
Activity at human A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISAActivity at human A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
CHEMBL375293 2281 None 30 Human Functional pIC50 = 6.5 6.5 1 2
Activity at human A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISAActivity at human A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
135522362 100075 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 472 8 1 10 0.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)N4CCN(C)CC4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL286838 100075 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 472 8 1 10 0.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)N4CCN(C)CC4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
134151346 151660 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 275 4 2 7 2.8 CCCNc1nc(N)c2nc(-c3ccco3)sc2n1 10.1021/acs.jmedchem.6b01068
CHEMBL3963278 151660 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 275 4 2 7 2.8 CCCNc1nc(N)c2nc(-c3ccco3)sc2n1 10.1021/acs.jmedchem.6b01068
60154742 77200 None 0 Human Functional pIC50 = 5.5 5.5 -39 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 501 4 3 10 2.5 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)Nc4ccncc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2071050 77200 None 0 Human Functional pIC50 = 5.5 5.5 -39 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 501 4 3 10 2.5 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)Nc4ccncc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2078766 77200 None 0 Human Functional pIC50 = 5.5 5.5 -39 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 501 4 3 10 2.5 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)Nc4ccncc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
60154740 77017 None 0 Human Functional pIC50 = 5.5 5.5 -95 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 544 6 3 10 2.8 COc1ccc(CNC(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)cc1 10.1021/jm300323t
CHEMBL2071049 77017 None 0 Human Functional pIC50 = 5.5 5.5 -95 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 544 6 3 10 2.8 COc1ccc(CNC(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)cc1 10.1021/jm300323t
57402161 69815 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 255 1 1 8 0.9 Cn1cc2nc(N)n3nc(-c4ccco4)nc3c2n1 10.1016/j.bmc.2011.11.037
CHEMBL1935760 69815 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 255 1 1 8 0.9 Cn1cc2nc(N)n3nc(-c4ccco4)nc3c2n1 10.1016/j.bmc.2011.11.037
10126989 10770 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 417 7 1 6 3.7 COCCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171526 10770 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 417 7 1 6 3.7 COCCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
145971923 163113 None 0 Human Functional pIC50 = 7.5 7.5 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2ccncc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4175676 163113 None 0 Human Functional pIC50 = 7.5 7.5 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2ccncc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
118708236 113429 None 0 Human Functional pIC50 = 6.5 6.5 -138 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 359 6 1 6 3.6 COc1cccc(CCCc2nc(N)c3nn(-c4ccccc4)cc3n2)c1 10.1016/j.ejmech.2014.07.060
CHEMBL3317576 113429 None 0 Human Functional pIC50 = 6.5 6.5 -138 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 359 6 1 6 3.6 COc1cccc(CCCc2nc(N)c3nn(-c4ccccc4)cc3n2)c1 10.1016/j.ejmech.2014.07.060
156017042 177863 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 450 5 1 10 3.4 CCOC(=O)c1ccc(N2CCN(c3nc(N)c4nc(-c5ccco5)sc4n3)CC2)cc1 10.1016/j.bmcl.2020.127067
CHEMBL4642713 177863 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 450 5 1 10 3.4 CCOC(=O)c1ccc(N2CCN(c3nc(N)c4nc(-c5ccco5)sc4n3)CC2)cc1 10.1016/j.bmcl.2020.127067
156010442 177148 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP productionInhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP production
ChEMBL 416 6 3 9 2.2 Nc1nc(NCCc2ccc(S(N)(=O)=O)cc2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
CHEMBL4632532 177148 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP productionInhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP production
ChEMBL 416 6 3 9 2.2 Nc1nc(NCCc2ccc(S(N)(=O)=O)cc2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
11716665 2281 None 30 Mouse Functional pIC50 = 6.5 6.5 -1 2
Activity at mouse A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISAActivity at mouse A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
5617 2281 None 30 Mouse Functional pIC50 = 6.5 6.5 -1 2
Activity at mouse A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISAActivity at mouse A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
CHEMBL375293 2281 None 30 Mouse Functional pIC50 = 6.5 6.5 -1 2
Activity at mouse A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISAActivity at mouse A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
49797793 10858 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 427 6 1 7 3.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)OC)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172274 10858 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 427 6 1 7 3.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)OC)cc3)sc12 10.1016/j.bmcl.2010.05.056
136042329 71179 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 534 10 2 11 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(=O)OCC)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955904 71179 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 534 10 2 11 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(=O)OCC)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
22283414 10666 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 359 4 2 5 3.7 COc1ccc(NC(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170518 10666 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 359 4 2 5 3.7 COc1ccc(NC(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
49797825 10669 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 430 6 2 6 2.8 CNC(=O)CN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170525 10669 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 430 6 2 6 2.8 CNC(=O)CN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
22283414 10666 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 359 4 2 5 3.7 COc1ccc(NC(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2011.02.053
CHEMBL1170518 10666 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 359 4 2 5 3.7 COc1ccc(NC(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2011.02.053
145961997 161649 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 301 4 2 7 2.6 COc1cccc(CNc2nc(N)c3nc(C)sc3n2)c1 10.1016/j.bmc.2018.05.048
CHEMBL4128787 161649 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 301 4 2 7 2.6 COc1cccc(CNc2nc(N)c3nc(C)sc3n2)c1 10.1016/j.bmc.2018.05.048
127045699 139722 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 323 3 1 6 3.2 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4F)cc3n2)o1 10.1016/j.bmc.2016.04.048
CHEMBL3797666 139722 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 323 3 1 6 3.2 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4F)cc3n2)o1 10.1016/j.bmc.2016.04.048
145963230 161601 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 333 4 2 6 3.9 Nc1nc(NCc2ccccc2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
CHEMBL4128138 161601 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 333 4 2 6 3.9 Nc1nc(NCc2ccccc2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
49797795 10619 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 447 6 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(S(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170129 10619 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 447 6 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(S(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
25230951 150387 None 0 Human Functional pIC50 = 7.4 7.4 5 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 380 6 1 7 4.6 CCc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL3952824 150387 None 0 Human Functional pIC50 = 7.4 7.4 5 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 380 6 1 7 4.6 CCc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
45481750 201020 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 449 5 1 8 4.0 Cn1cc2c(nc(NC(=O)C(c3ccccc3)c3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL578224 201020 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 449 5 1 8 4.0 Cn1cc2c(nc(NC(=O)C(c3ccccc3)c3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
46882996 5641 None 0 Human Functional pIC50 = 5.4 5.4 1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 288 3 0 5 3.9 CCc1nc(C(=O)c2ccc(C)s2)c2sccc2n1 10.1016/j.bmcl.2009.08.040
CHEMBL1077750 5641 None 0 Human Functional pIC50 = 5.4 5.4 1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 288 3 0 5 3.9 CCc1nc(C(=O)c2ccc(C)s2)c2sccc2n1 10.1016/j.bmcl.2009.08.040
49797774 10625 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 462 7 2 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(NS(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170137 10625 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 462 7 2 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(NS(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
145961339 161659 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 257 2 2 6 2.7 Cc1nc2c(N)nc(Nc3ccccc3)nc2s1 10.1016/j.bmc.2018.05.048
CHEMBL4128862 161659 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 257 2 2 6 2.7 Cc1nc2c(N)nc(Nc3ccccc3)nc2s1 10.1016/j.bmc.2018.05.048
49798139 10675 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 495 6 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCN(C)CC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170583 10675 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 495 6 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCN(C)CC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
135484064 2616 None 3 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm201292w
390 2616 None 3 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm201292w
CHEMBL260331 2616 None 3 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm201292w
136042353 71177 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 530 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(F)(F)F)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955902 71177 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 530 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(F)(F)F)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
135484064 2616 None 3 Human Functional pIC50 = 7.4 7.4 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm0309654
390 2616 None 3 Human Functional pIC50 = 7.4 7.4 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm0309654
CHEMBL260331 2616 None 3 Human Functional pIC50 = 7.4 7.4 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm0309654
118708235 113428 None 0 Human Functional pIC50 = 6.4 6.4 -32 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 359 6 1 6 3.6 COc1ccccc1CCCc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1016/j.ejmech.2014.07.060
CHEMBL3317575 113428 None 0 Human Functional pIC50 = 6.4 6.4 -32 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 359 6 1 6 3.6 COc1ccccc1CCCc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1016/j.ejmech.2014.07.060
134149255 148252 None 0 Human Functional pIC50 = 6.4 6.4 -16 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 2 7 3.6 Nc1nc(NCCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3935610 148252 None 0 Human Functional pIC50 = 6.4 6.4 -16 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 2 7 3.6 Nc1nc(NCCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
145954398 162690 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 5 2 8 3.9 COc1ccccc1CNc1nc(N)c2nc(-c3ccc(C)o3)sc2n1 10.1016/j.ejmech.2018.06.020
CHEMBL4168980 162690 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 5 2 8 3.9 COc1ccccc1CNc1nc(N)c2nc(-c3ccc(C)o3)sc2n1 10.1016/j.ejmech.2018.06.020
25230881 6179 None 0 Human Functional pIC50 = 7.4 7.4 1 4
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 395 6 1 8 4.1 CN(C)c1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
CHEMBL1081160 6179 None 0 Human Functional pIC50 = 7.4 7.4 1 4
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 395 6 1 8 4.1 CN(C)c1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
127045909 140075 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 321 3 2 7 2.7 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4O)cc3n2)o1 10.1016/j.bmc.2016.04.048
CHEMBL3799921 140075 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 321 3 2 7 2.7 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4O)cc3n2)o1 10.1016/j.bmc.2016.04.048
156821369 185729 None 2 Human Functional pIC50 = 8.4 8.4 -14 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 447 4 2 7 3.5 Nc1nc(-c2ccccc2)c(-c2ccc(=O)[nH]c2)c2nc(Cc3ncc(F)cc3Cl)nn12 10.1021/acsmedchemlett.1c00620
CHEMBL4864129 185729 None 2 Human Functional pIC50 = 8.4 8.4 -14 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 447 4 2 7 3.5 Nc1nc(-c2ccccc2)c(-c2ccc(=O)[nH]c2)c2nc(Cc3ncc(F)cc3Cl)nn12 10.1021/acsmedchemlett.1c00620
145436763 162291 None 0 Human Functional pIC50 = 8.4 8.4 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 338 5 2 8 3.0 Nc1nc(NCCc2cccnc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4162638 162291 None 0 Human Functional pIC50 = 8.4 8.4 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 338 5 2 8 3.0 Nc1nc(NCCc2cccnc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
44186579 191893 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 494 6 2 7 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL519813 191893 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 494 6 2 7 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
57400352 69808 None 0 Human Functional pIC50 = 7.4 7.4 12 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 283 3 1 8 1.7 CCCn1ncc2nc(N)n3nc(-c4ccco4)nc3c21 10.1016/j.bmc.2011.11.037
CHEMBL1935753 69808 None 0 Human Functional pIC50 = 7.4 7.4 12 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 283 3 1 8 1.7 CCCn1ncc2nc(N)n3nc(-c4ccco4)nc3c21 10.1016/j.bmc.2011.11.037
49797855 10854 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 441 5 1 5 4.6 COc1ccc(N(CC(F)(F)F)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172269 10854 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 441 5 1 5 4.6 COc1ccc(N(CC(F)(F)F)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
135522368 492 None 1 Human Functional pIC50 = 7.4 7.4 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 493 9 2 9 2.7 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)C)C 10.1021/jm0309654
383 492 None 1 Human Functional pIC50 = 7.4 7.4 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 493 9 2 9 2.7 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)C)C 10.1021/jm0309654
CHEMBL33491 492 None 1 Human Functional pIC50 = 7.4 7.4 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 493 9 2 9 2.7 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)C)C 10.1021/jm0309654
11371101 67588 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human cloned adenosine A2B cells expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP productionAntagonist activity at human cloned adenosine A2B cells expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production
ChEMBL 336 4 0 6 2.2 CCCn1c(=O)c2c(nc3n2CC(C)=C3)n(Cc2ccccc2)c1=O 10.1016/j.bmc.2008.10.049
CHEMBL189904 67588 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human cloned adenosine A2B cells expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP productionAntagonist activity at human cloned adenosine A2B cells expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production
ChEMBL 336 4 0 6 2.2 CCCn1c(=O)c2c(nc3n2CC(C)=C3)n(Cc2ccccc2)c1=O 10.1016/j.bmc.2008.10.049
11371101 67588 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of 100 nM NECA-stimulated cAMP production in CHO cells expressing human adenosine A2B receptorInhibition of 100 nM NECA-stimulated cAMP production in CHO cells expressing human adenosine A2B receptor
ChEMBL 336 4 0 6 2.2 CCCn1c(=O)c2c(nc3n2CC(C)=C3)n(Cc2ccccc2)c1=O 10.1021/jm058008c
CHEMBL189904 67588 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of 100 nM NECA-stimulated cAMP production in CHO cells expressing human adenosine A2B receptorInhibition of 100 nM NECA-stimulated cAMP production in CHO cells expressing human adenosine A2B receptor
ChEMBL 336 4 0 6 2.2 CCCn1c(=O)c2c(nc3n2CC(C)=C3)n(Cc2ccccc2)c1=O 10.1021/jm058008c
145961748 161605 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 365 5 2 9 2.7 COc1ccccc1CNc1nc(N)c2nc(-c3cnccn3)sc2n1 10.1016/j.bmc.2018.05.048
CHEMBL4128190 161605 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 365 5 2 9 2.7 COc1ccccc1CNc1nc(N)c2nc(-c3cnccn3)sc2n1 10.1016/j.bmc.2018.05.048
54586036 60744 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 6 1 6 4.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CCN(C(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760887 60744 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 6 1 6 4.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CCN(C(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
10761800 188325 None 0 Rat Functional pIC50 = 6.4 6.4 -5 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 372 1 2 7 2.5 Cn1c(-c2cccc(C#N)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL49925 188325 None 0 Rat Functional pIC50 = 6.4 6.4 -5 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 372 1 2 7 2.5 Cn1c(-c2cccc(C#N)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
46883041 5735 None 0 Human Functional pIC50 = 6.4 6.4 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 379 5 1 6 5.5 Cc1ccc(C(=O)c2nc(NC(C)c3ccccc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078347 5735 None 0 Human Functional pIC50 = 6.4 6.4 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 379 5 1 6 5.5 Cc1ccc(C(=O)c2nc(NC(C)c3ccccc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
46883074 5707 None 0 Human Functional pIC50 = 5.4 5.4 -1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 0 7 4.3 Cc1ccc(C(=O)c2nc(N(C)Cc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078087 5707 None 0 Human Functional pIC50 = 5.4 5.4 -1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 0 7 4.3 Cc1ccc(C(=O)c2nc(N(C)Cc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
57402117 69797 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 254 1 1 7 1.5 Cn1cc2nc(N)n3nc(-c4ccco4)nc3c2c1 10.1016/j.bmc.2011.11.037
CHEMBL1935743 69797 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 254 1 1 7 1.5 Cn1cc2nc(N)n3nc(-c4ccco4)nc3c2c1 10.1016/j.bmc.2011.11.037
49797852 10768 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 417 7 2 6 3.4 COc1ccc(N(CCCO)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171524 10768 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 417 7 2 6 3.4 COc1ccc(N(CCCO)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
54587015 60742 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 570 7 1 7 4.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CCN(S(=O)(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760885 60742 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 570 7 1 7 4.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CCN(S(=O)(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
71601632 86958 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting methodAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting method
ChEMBL 301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2015.11.015
CHEMBL2322918 86958 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting methodAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting method
ChEMBL 301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2015.11.015
71601632 86958 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.bmc.2016.04.048
CHEMBL2322918 86958 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.bmc.2016.04.048
71601632 86958 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
CHEMBL2322918 86958 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
9841364 101512 None 1 Rat Functional pIC50 = 6.4 6.4 -6 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 351 1 2 6 2.4 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCC3)nc21 10.1021/jm990499b
CHEMBL297685 101512 None 1 Rat Functional pIC50 = 6.4 6.4 -6 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 351 1 2 6 2.4 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCC3)nc21 10.1021/jm990499b
127045700 139809 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 323 3 1 6 3.2 Cc1ccc(-c2nc(N)c3nn(Cc4cccc(F)c4)cc3n2)o1 10.1016/j.bmc.2016.04.048
CHEMBL3798214 139809 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 323 3 1 6 3.2 Cc1ccc(-c2nc(N)c3nn(Cc4cccc(F)c4)cc3n2)o1 10.1016/j.bmc.2016.04.048
1329 1472 None 53 Human Functional pIC50 = 7.4 7.4 -9 8
Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assayAntagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.9b00106
386 1472 None 53 Human Functional pIC50 = 7.4 7.4 -9 8
Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assayAntagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.9b00106
CHEMBL183 1472 None 53 Human Functional pIC50 = 7.4 7.4 -9 8
Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assayAntagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.9b00106
DB12946 1472 None 53 Human Functional pIC50 = 7.4 7.4 -9 8
Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assayAntagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.9b00106
135678052 95830 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 483 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Cl)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL258571 95830 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 483 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Cl)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
46883042 5736 None 0 Human Functional pIC50 = 7.4 7.4 4 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 366 5 1 7 4.3 Cc1ccc(C(=O)c2nc(NCc3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078348 5736 None 0 Human Functional pIC50 = 7.4 7.4 4 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 366 5 1 7 4.3 Cc1ccc(C(=O)c2nc(NCc3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
136042347 71199 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 482 9 2 8 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955925 71199 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 482 9 2 8 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
118708234 113427 None 0 Human Functional pIC50 = 6.4 6.4 -10 3
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 329 5 1 5 3.6 Nc1nc(CCCc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
CHEMBL3317574 113427 None 0 Human Functional pIC50 = 6.4 6.4 -10 3
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 329 5 1 5 3.6 Nc1nc(CCCc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
127035626 137405 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 426 6 3 8 4.0 O=C(Nc1ccccc1)Nc1nc(NCc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2015.12.019
CHEMBL3752621 137405 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 426 6 3 8 4.0 O=C(Nc1ccccc1)Nc1nc(NCc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2015.12.019
145960873 161538 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 347 5 2 6 4.0 Nc1nc(NCCc2ccccc2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
CHEMBL4127351 161538 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 347 5 2 6 4.0 Nc1nc(NCCc2ccccc2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
54580150 60750 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 7 1 6 5.5 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)C3CCN(Cc4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760894 60750 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 7 1 6 5.5 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)C3CCN(Cc4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
71601631 86957 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting methodAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting method
ChEMBL 287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2015.11.015
CHEMBL2322917 86957 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting methodAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting method
ChEMBL 287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2015.11.015
71601631 86957 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.bmc.2016.04.048
CHEMBL2322917 86957 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.bmc.2016.04.048
71601631 86957 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
CHEMBL2322917 86957 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
10691124 101335 None 0 Rat Functional pIC50 = 6.4 6.4 -8 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 379 1 2 6 3.2 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCCC3)nc21 10.1021/jm990499b
CHEMBL296389 101335 None 0 Rat Functional pIC50 = 6.4 6.4 -8 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 379 1 2 6 3.2 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCCC3)nc21 10.1021/jm990499b
10618828 102043 None 0 Rat Functional pIC50 = 6.4 6.4 -5 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 365 1 2 6 2.8 Cn1c(-c2ccccc2F)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL301512 102043 None 0 Rat Functional pIC50 = 6.4 6.4 -5 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 365 1 2 6 2.8 Cn1c(-c2ccccc2F)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
10754589 193429 None 0 Rat Functional pIC50 = 5.4 5.4 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 271 0 2 6 1.0 Cn1cnc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL52432 193429 None 0 Rat Functional pIC50 = 5.4 5.4 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 271 0 2 6 1.0 Cn1cnc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
57396936 69816 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 283 3 1 8 1.7 CCCn1cc2nc(N)n3nc(-c4ccco4)nc3c2n1 10.1016/j.bmc.2011.11.037
CHEMBL1935761 69816 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 283 3 1 8 1.7 CCCn1cc2nc(N)n3nc(-c4ccco4)nc3c2n1 10.1016/j.bmc.2011.11.037
136042354 71178 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 476 8 2 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955903 71178 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 476 8 2 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
46883073 5706 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 6 1 7 4.3 Cc1ccc(C(=O)c2nc(NCCc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078086 5706 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 6 1 7 4.3 Cc1ccc(C(=O)c2nc(NCCc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
132991406 144301 None 0 Human Functional pIC50 = 6.3 6.3 -4786 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1cccc(CNc2nc(N)c3nc(-c4ccco4)sc3n2)c1 10.1021/acs.jmedchem.6b01068
CHEMBL3904408 144301 None 0 Human Functional pIC50 = 6.3 6.3 -4786 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1cccc(CNc2nc(N)c3nc(-c4ccco4)sc3n2)c1 10.1021/acs.jmedchem.6b01068
145958464 162253 None 0 Human Functional pIC50 = 5.3 5.3 -1174 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 369 5 2 8 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3cccs3)sc2n1 10.1016/j.ejmech.2018.06.020
CHEMBL4162037 162253 None 0 Human Functional pIC50 = 5.3 5.3 -1174 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 369 5 2 8 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3cccs3)sc2n1 10.1016/j.ejmech.2018.06.020
57396888 69799 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 344 4 1 7 3.2 Nc1nc2cn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
CHEMBL1935745 69799 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 344 4 1 7 3.2 Nc1nc2cn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
135522375 114321 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 525 11 2 11 2.1 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(OC)c(OC)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL33305 114321 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 525 11 2 11 2.1 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(OC)c(OC)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
46883109 5836 None 0 Human Functional pIC50 = 6.3 6.3 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 350 5 1 7 3.8 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)o1 10.1016/j.bmcl.2009.08.040
CHEMBL1079117 5836 None 0 Human Functional pIC50 = 6.3 6.3 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 350 5 1 7 3.8 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)o1 10.1016/j.bmcl.2009.08.040
134132667 144671 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 6 2 8 3.6 COc1cccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)c1 10.1021/acs.jmedchem.6b01068
CHEMBL3907658 144671 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 6 2 8 3.6 COc1cccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)c1 10.1021/acs.jmedchem.6b01068
10175278 170487 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 588 9 2 8 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)nc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL444787 170487 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 588 9 2 8 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)nc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL5075422 216860 None 4 Human Functional pIC50 = 6.3 6.3 -83 4
Antagonist activity at human recombinant adenosine A2B receptor transfected in HEK293 cells co-transfected with Galpha15/16 assessed as intracellular calcium change incubated for 10 mins by microplate reader methodAntagonist activity at human recombinant adenosine A2B receptor transfected in HEK293 cells co-transfected with Galpha15/16 assessed as intracellular calcium change incubated for 10 mins by microplate reader method
ChEMBL None None None Cn1cc(-c2cnc(N)n3nc(-c4ccco4)nc23)ccc1=O 10.1021/acsmedchemlett.1c00599
176407 4148 None 56 Human Functional pIC50 = 7.3 7.3 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.6b01068
405 4148 None 56 Human Functional pIC50 = 7.3 7.3 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.6b01068
CHEMBL113142 4148 None 56 Human Functional pIC50 = 7.3 7.3 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.6b01068
DB08770 4148 None 56 Human Functional pIC50 = 7.3 7.3 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.6b01068
134132684 144808 None 0 Human Functional pIC50 = 6.3 6.3 -20 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 3 8 3.3 Nc1nc(NCCc2ccc(O)cc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3908770 144808 None 0 Human Functional pIC50 = 6.3 6.3 -20 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 3 8 3.3 Nc1nc(NCCc2ccc(O)cc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
46883108 5835 None 0 Human Functional pIC50 = 6.3 6.3 3 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 386 5 1 7 4.6 O=C(c1ccc(Cl)s1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079116 5835 None 0 Human Functional pIC50 = 6.3 6.3 3 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 386 5 1 7 4.6 O=C(c1ccc(Cl)s1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
54584125 60749 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 584 7 1 7 4.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)C3CCN(S(=O)(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760893 60749 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 584 7 1 7 4.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)C3CCN(S(=O)(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
10691124 101335 None 0 Human Functional pIC50 = 7.3 7.3 8 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 379 1 2 6 3.2 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCCC3)nc21 10.1021/jm990499b
CHEMBL296389 101335 None 0 Human Functional pIC50 = 7.3 7.3 8 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 379 1 2 6 3.2 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCCC3)nc21 10.1021/jm990499b
46237928 8811 None 0 Human Functional pIC50 = 7.3 7.3 -42 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 329 3 1 5 3.3 Cn1cc2c(NC(=O)c3ccccc3)nc(-c3ccccc3)nc2n1 10.1021/jm901785w
CHEMBL1096754 8811 None 0 Human Functional pIC50 = 7.3 7.3 -42 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 329 3 1 5 3.3 Cn1cc2c(NC(=O)c3ccccc3)nc(-c3ccccc3)nc2n1 10.1021/jm901785w
10762430 189269 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 381 1 2 6 3.3 Cn1c(-c2cccc(Cl)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL51107 189269 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 381 1 2 6 3.3 Cn1c(-c2cccc(Cl)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
45481754 200607 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 477 7 1 8 4.9 CCCn1cc2c(nc(NC(=O)C(c3ccccc3)c3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL574775 200607 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 477 7 1 8 4.9 CCCn1cc2c(nc(NC(=O)C(c3ccccc3)c3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
25230098 6218 None 0 Human Functional pIC50 = 6.3 6.3 14 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 299 4 2 6 2.1 CNC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1081334 6218 None 0 Human Functional pIC50 = 6.3 6.3 14 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 299 4 2 6 2.1 CNC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
156010442 177148 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 416 6 3 9 2.2 Nc1nc(NCCc2ccc(S(N)(=O)=O)cc2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
CHEMBL4632532 177148 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 416 6 3 9 2.2 Nc1nc(NCCc2ccc(S(N)(=O)=O)cc2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
44186716 184220 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 524 7 2 8 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL482648 184220 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 524 7 2 8 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44186718 184279 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 538 6 2 9 1.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL483065 184279 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 538 6 2 9 1.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
57325914 74751 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 356 4 0 6 3.5 O=c1c(-c2ccco2)nnc2n(CCc3ccccc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL2030706 74751 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 356 4 0 6 3.5 O=c1c(-c2ccco2)nnc2n(CCc3ccccc3)c3ccccc3n12 10.1021/jm201177b
10714900 189559 None 0 Human Functional pIC50 = 6.3 6.3 12 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 381 1 2 6 3.3 Cn1c(-c2ccc(Cl)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL51353 189559 None 0 Human Functional pIC50 = 6.3 6.3 12 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 381 1 2 6 3.3 Cn1c(-c2ccc(Cl)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
45482074 200758 None 0 Human Functional pIC50 = 4.3 4.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 511 8 1 8 5.2 O=C(Cc1cccc(Cl)c1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2009.05.038
CHEMBL576017 200758 None 0 Human Functional pIC50 = 4.3 4.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 511 8 1 8 5.2 O=C(Cc1cccc(Cl)c1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2009.05.038
145960746 161698 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 365 5 2 9 2.7 COc1cccc(CNc2nc(N)c3nc(-c4cnccn4)sc3n2)c1 10.1016/j.bmc.2018.05.048
CHEMBL4129565 161698 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 365 5 2 9 2.7 COc1cccc(CNc2nc(N)c3nc(-c4cnccn4)sc3n2)c1 10.1016/j.bmc.2018.05.048
60154738 77015 None 0 Human Functional pIC50 = 6.3 6.3 -5 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 548 5 3 9 3.4 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccc(Cl)cc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2071047 77015 None 0 Human Functional pIC50 = 6.3 6.3 -5 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 548 5 3 9 3.4 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccc(Cl)cc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
45482464 200988 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 447 7 1 8 4.1 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL578005 200988 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 447 7 1 8 4.1 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
136042341 71191 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 517 8 2 9 3.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(F)(F)F)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955917 71191 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 517 8 2 9 3.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(F)(F)F)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
176407 4148 None 56 Human Functional pIC50 = 7.3 7.3 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2018.06.020
405 4148 None 56 Human Functional pIC50 = 7.3 7.3 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2018.06.020
CHEMBL113142 4148 None 56 Human Functional pIC50 = 7.3 7.3 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2018.06.020
DB08770 4148 None 56 Human Functional pIC50 = 7.3 7.3 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2018.06.020
10616023 101917 None 0 Rat Functional pIC50 = 6.3 6.3 -3 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 325 1 2 6 1.9 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC(C)(C)O)nc21 10.1021/jm990499b
CHEMBL300624 101917 None 0 Rat Functional pIC50 = 6.3 6.3 -3 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 325 1 2 6 1.9 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC(C)(C)O)nc21 10.1021/jm990499b
46883158 5840 None 0 Human Functional pIC50 = 6.3 6.3 3 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 346 5 1 6 3.9 O=C(c1ccccc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079141 5840 None 0 Human Functional pIC50 = 6.3 6.3 3 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 346 5 1 6 3.9 O=C(c1ccccc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
127046493 139884 None 0 Human Functional pIC50 = 6.3 6.3 -83 3
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 321 4 1 7 2.7 COc1ccccc1Cn1cc2nc(-c3ccco3)nc(N)c2n1 10.1016/j.bmc.2016.04.048
CHEMBL3798766 139884 None 0 Human Functional pIC50 = 6.3 6.3 -83 3
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 321 4 1 7 2.7 COc1ccccc1Cn1cc2nc(-c3ccco3)nc(N)c2n1 10.1016/j.bmc.2016.04.048
16071896 58042 None 39 Mouse Functional pIC50 = 6.3 6.3 -4 2
Antagonist activity at mouse adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISAAntagonist activity at mouse adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISA
ChEMBL 335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2cccnc2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672627 58042 None 39 Mouse Functional pIC50 = 6.3 6.3 -4 2
Antagonist activity at mouse adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISAAntagonist activity at mouse adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISA
ChEMBL 335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2cccnc2)n1)C1CC1 10.1021/ml100249e
25230950 152834 None 0 Human Functional pIC50 = 7.3 7.3 3 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 378 6 1 7 4.6 C=Cc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL3973260 152834 None 0 Human Functional pIC50 = 7.3 7.3 3 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 378 6 1 7 4.6 C=Cc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
136042334 71185 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 490 8 2 9 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C)c(C)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955910 71185 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 490 8 2 9 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C)c(C)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
46237929 8958 None 0 Human Functional pIC50 = 7.3 7.3 -138 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 359 4 1 6 3.3 COc1ccc(C(=O)Nc2nc(-c3ccccc3)nc3nn(C)cc23)cc1 10.1021/jm901785w
CHEMBL1098108 8958 None 0 Human Functional pIC50 = 7.3 7.3 -138 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 359 4 1 6 3.3 COc1ccc(C(=O)Nc2nc(-c3ccccc3)nc3nn(C)cc23)cc1 10.1021/jm901785w
10633978 185983 None 0 Rat Functional pIC50 = 5.3 5.3 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 243 1 1 5 1.8 Cn1c(-c2cccc(F)c2)nc2c(N)ncnc21 10.1021/jm990499b
CHEMBL48682 185983 None 0 Rat Functional pIC50 = 5.3 5.3 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 243 1 1 5 1.8 Cn1c(-c2cccc(F)c2)nc2c(N)ncnc21 10.1021/jm990499b
45482080 200881 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 451 6 1 8 4.5 CCCn1cc2c(nc(NC(=O)Cc3ccc4ccccc4c3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL577135 200881 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 451 6 1 8 4.5 CCCn1cc2c(nc(NC(=O)Cc3ccc4ccccc4c3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
46882994 5827 None 0 Human Functional pIC50 = 5.3 5.3 1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 260 2 0 5 3.3 Cc1ccc(C(=O)c2ncnc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1079059 5827 None 0 Human Functional pIC50 = 5.3 5.3 1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 260 2 0 5 3.3 Cc1ccc(C(=O)c2ncnc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
136042351 71175 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 492 9 2 10 2.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(OC)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955900 71175 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 492 9 2 10 2.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(OC)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
386674 111384 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 352 3 0 5 3.8 O=c1c(-c2ccccc2)nnc2n(Cc3ccccc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL326752 111384 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 352 3 0 5 3.8 O=c1c(-c2ccccc2)nnc2n(Cc3ccccc3)c3ccccc3n12 10.1021/jm201177b
10665761 189385 None 0 Rat Functional pIC50 = 6.3 6.3 -3 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 353 3 2 6 2.7 CCC(O)(C#Cc1nc(N)c2nc(-c3cccc(F)c3)n(C)c2n1)CC 10.1021/jm990499b
CHEMBL51192 189385 None 0 Rat Functional pIC50 = 6.3 6.3 -3 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 353 3 2 6 2.7 CCC(O)(C#Cc1nc(N)c2nc(-c3cccc(F)c3)n(C)c2n1)CC 10.1021/jm990499b
145954098 162634 None 0 Human Functional pIC50 = 6.3 6.3 -35 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 345 4 2 8 4.1 Nc1nc(NCc2cccs2)nc2sc(-c3cccs3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4168016 162634 None 0 Human Functional pIC50 = 6.3 6.3 -35 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 345 4 2 8 4.1 Nc1nc(NCc2cccs2)nc2sc(-c3cccs3)nc12 10.1016/j.ejmech.2018.06.020
57402162 69821 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 494 7 2 9 4.6 COc1ccc(NC(=O)Nc2nc3cn(CCc4ccccc4)nc3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
CHEMBL1935766 69821 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 494 7 2 9 4.6 COc1ccc(NC(=O)Nc2nc3cn(CCc4ccccc4)nc3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
44537897 200532 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 497 7 1 8 5.0 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(C(F)(F)F)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL574263 200532 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 497 7 1 8 5.0 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(C(F)(F)F)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
46883043 5737 None 0 Human Functional pIC50 = 7.3 7.3 18 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 366 5 1 7 4.3 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078349 5737 None 0 Human Functional pIC50 = 7.3 7.3 18 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 366 5 1 7 4.3 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
134138322 148127 None 0 Human Functional pIC50 = 6.3 6.3 -15 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 6 2 8 3.6 COc1ccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1 10.1021/acs.jmedchem.6b01068
CHEMBL3934626 148127 None 0 Human Functional pIC50 = 6.3 6.3 -15 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 6 2 8 3.6 COc1ccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1 10.1021/acs.jmedchem.6b01068
145963661 161636 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 301 4 2 7 2.6 COc1ccccc1CNc1nc(N)c2nc(C)sc2n1 10.1016/j.bmc.2018.05.048
CHEMBL4128638 161636 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 301 4 2 7 2.6 COc1ccccc1CNc1nc(N)c2nc(C)sc2n1 10.1016/j.bmc.2018.05.048
46883040 5689 None 0 Human Functional pIC50 = 5.3 5.3 1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 365 5 1 6 4.9 Cc1ccc(C(=O)c2nc(NCc3ccccc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1077985 5689 None 0 Human Functional pIC50 = 5.3 5.3 1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 365 5 1 6 4.9 Cc1ccc(C(=O)c2nc(NCc3ccccc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
10621771 193228 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 415 1 2 6 3.7 Cn1c(-c2cccc(C(F)(F)F)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL52276 193228 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 415 1 2 6 3.7 Cn1c(-c2cccc(C(F)(F)F)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
25230100 6354 None 0 Human Functional pIC50 = 6.2 6.2 5 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 5 2 6 3.8 O=C(NC1CCCCC1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1082063 6354 None 0 Human Functional pIC50 = 6.2 6.2 5 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 5 2 6 3.8 O=C(NC1CCCCC1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
9970667 207739 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 276 1 0 5 2.2 Cn1c2ccccc2n2c(=O)c(-c3ccccc3)nnc12 10.1021/jm201177b
CHEMBL7909 207739 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 276 1 0 5 2.2 Cn1c2ccccc2n2c(=O)c(-c3ccccc3)nnc12 10.1021/jm201177b
135874413 96443 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 449 8 2 8 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccccc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL261810 96443 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 449 8 2 8 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccccc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
156018440 177957 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 457 4 2 10 1.9 Nc1nc(N2CCN(c3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
CHEMBL4644153 177957 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 457 4 2 10 1.9 Nc1nc(N2CCN(c3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
57395164 69819 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3cn(C)nc3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
CHEMBL1935764 69819 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3cn(C)nc3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
45481760 200464 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 539 8 1 8 5.7 O=C(Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.05.038
CHEMBL573780 200464 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 539 8 1 8 5.7 O=C(Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.05.038
57395162 69810 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 359 5 1 8 2.9 Nc1nc2cnn(CCCc3ccccc3)c2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
CHEMBL1935755 69810 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 359 5 1 8 2.9 Nc1nc2cnn(CCCc3ccccc3)c2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
49797905 10747 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 517 7 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(C(F)(F)F)c4)c3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171164 10747 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 517 7 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(C(F)(F)F)c4)c3)sc12 10.1016/j.bmcl.2010.05.056
49797905 10747 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 517 7 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(C(F)(F)F)c4)c3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1171164 10747 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 517 7 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(C(F)(F)F)c4)c3)sc12 10.1016/j.bmcl.2011.02.053
136042339 71189 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 483 8 2 9 3.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955915 71189 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 483 8 2 9 3.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
25230881 6179 None 0 Human Functional pIC50 = 8.2 8.2 1 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 395 6 1 8 4.1 CN(C)c1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL1081160 6179 None 0 Human Functional pIC50 = 8.2 8.2 1 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 395 6 1 8 4.1 CN(C)c1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
25230948 6037 None 0 Human Functional pIC50 = 8.2 8.2 3 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 395 7 2 8 4.4 CCNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL1080421 6037 None 0 Human Functional pIC50 = 8.2 8.2 3 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 395 7 2 8 4.4 CCNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
156821433 186100 None 0 Human Functional pIC50 = 8.2 8.2 -12 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 427 4 1 8 2.9 Cn1cc(-c2c(-c3ccccc3)nc(N)n3nc(Cc4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
CHEMBL4870159 186100 None 0 Human Functional pIC50 = 8.2 8.2 -12 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 427 4 1 8 2.9 Cn1cc(-c2c(-c3ccccc3)nc(N)n3nc(Cc4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
49797826 10670 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 416 6 2 6 2.5 COc1ccc(N(CC(N)=O)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170526 10670 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 416 6 2 6 2.5 COc1ccc(N(CC(N)=O)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
136042331 71181 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 476 8 2 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C)cccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955906 71181 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 476 8 2 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C)cccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
135489238 477 None 2 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 533 9 2 9 3.4 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)Cl)Cl 10.1021/jm0309654
381 477 None 2 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 533 9 2 9 3.4 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)Cl)Cl 10.1021/jm0309654
CHEMBL32802 477 None 2 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 533 9 2 9 3.4 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)Cl)Cl 10.1021/jm0309654
49797797 10621 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 444 6 1 6 3.1 COc1ccc(N(CC(=O)N(C)C)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170131 10621 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 444 6 1 6 3.1 COc1ccc(N(CC(=O)N(C)C)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
49797827 10645 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 417 6 2 6 3.1 COc1ccc(N(CC(=O)O)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170295 10645 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 417 6 2 6 3.1 COc1ccc(N(CC(=O)O)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
135874420 161396 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 479 9 2 9 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(OC)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL412284 161396 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 479 9 2 9 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(OC)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
136042328 71171 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 507 9 2 11 2.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc([N+](=O)[O-])ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955894 71171 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 507 9 2 11 2.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc([N+](=O)[O-])ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
136042352 71176 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 540 8 2 9 3.3 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Br)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955901 71176 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 540 8 2 9 3.3 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Br)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
156821338 185925 None 0 Human Functional pIC50 = 7.2 7.2 -8 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 439 5 1 9 2.7 COc1ccc(Cc2nc3c(-c4ccc(=O)n(C)c4)c(-c4ccccc4)nc(N)n3n2)nc1 10.1021/acsmedchemlett.1c00620
CHEMBL4867286 185925 None 0 Human Functional pIC50 = 7.2 7.2 -8 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 439 5 1 9 2.7 COc1ccc(Cc2nc3c(-c4ccc(=O)n(C)c4)c(-c4ccccc4)nc(N)n3n2)nc1 10.1021/acsmedchemlett.1c00620
9841364 101512 None 1 Human Functional pIC50 = 7.2 7.2 6 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 351 1 2 6 2.4 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCC3)nc21 10.1021/jm990499b
CHEMBL297685 101512 None 1 Human Functional pIC50 = 7.2 7.2 6 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 351 1 2 6 2.4 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCC3)nc21 10.1021/jm990499b
118708214 113416 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 211 1 1 5 1.4 Nc1ncnc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
CHEMBL3317555 113416 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 211 1 1 5 1.4 Nc1ncnc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
10714900 189559 None 0 Rat Functional pIC50 = 5.2 5.2 -12 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 381 1 2 6 3.3 Cn1c(-c2ccc(Cl)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL51353 189559 None 0 Rat Functional pIC50 = 5.2 5.2 -12 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 381 1 2 6 3.3 Cn1c(-c2ccc(Cl)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
134139825 146585 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 309 3 2 7 3.7 Nc1nc(Nc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3922410 146585 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 309 3 2 7 3.7 Nc1nc(Nc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
127045910 140126 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 321 3 2 7 2.7 Cc1ccc(-c2nc(N)c3nn(Cc4cccc(O)c4)cc3n2)o1 10.1016/j.bmc.2016.04.048
CHEMBL3800254 140126 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 321 3 2 7 2.7 Cc1ccc(-c2nc(N)c3nn(Cc4cccc(O)c4)cc3n2)o1 10.1016/j.bmc.2016.04.048
136042344 71194 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 551 8 2 9 4.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(Cl)cc(C(F)(F)F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955920 71194 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 551 8 2 9 4.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(Cl)cc(C(F)(F)F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
11716665 2281 None 30 Mouse Functional pIC50 = 6.2 6.2 -1 2
Inhibition of NECA-induced IL6 production in Swiss mouse fibroblasts after 24 hrs by ELISAInhibition of NECA-induced IL6 production in Swiss mouse fibroblasts after 24 hrs by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
5617 2281 None 30 Mouse Functional pIC50 = 6.2 6.2 -1 2
Inhibition of NECA-induced IL6 production in Swiss mouse fibroblasts after 24 hrs by ELISAInhibition of NECA-induced IL6 production in Swiss mouse fibroblasts after 24 hrs by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
CHEMBL375293 2281 None 30 Mouse Functional pIC50 = 6.2 6.2 -1 2
Inhibition of NECA-induced IL6 production in Swiss mouse fibroblasts after 24 hrs by ELISAInhibition of NECA-induced IL6 production in Swiss mouse fibroblasts after 24 hrs by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
45482087 200562 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 441 4 1 8 3.8 Cn1cc2c(nc(NC(=O)Cc3c(Cl)cccc3Cl)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL574490 200562 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 441 4 1 8 3.8 Cn1cc2c(nc(NC(=O)Cc3c(Cl)cccc3Cl)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
136042355 71172 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 462 8 2 9 2.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955897 71172 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 462 8 2 9 2.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
135443367 487 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
382 487 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
CHEMBL33455 487 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
135874416 96441 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 467 8 2 8 2.7 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(F)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL261809 96441 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 467 8 2 8 2.7 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(F)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
25230952 146640 None 0 Human Functional pIC50 = 7.2 7.2 3 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 458 8 2 9 5.0 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2cc(NCc3cccnc3)sc12 nan
CHEMBL3922797 146640 None 0 Human Functional pIC50 = 7.2 7.2 3 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 458 8 2 9 5.0 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2cc(NCc3cccnc3)sc12 nan
49797879 10667 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 358 5 2 5 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cc[nH]c3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170519 10667 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 358 5 2 5 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cc[nH]c3)sc12 10.1016/j.bmcl.2010.05.056
25230949 6007 None 0 Human Functional pIC50 = 8.2 8.2 15 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 367 5 2 8 3.6 Nc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL1080241 6007 None 0 Human Functional pIC50 = 8.2 8.2 15 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 367 5 2 8 3.6 Nc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
136042332 71183 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 598 8 2 9 4.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C(F)(F)F)cc(C(F)(F)F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955908 71183 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 598 8 2 9 4.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C(F)(F)F)cc(C(F)(F)F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
135443367 487 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
382 487 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
CHEMBL33455 487 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
51051251 69311 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 321 3 2 8 1.6 Nc1nc(NC(=O)c2ccccc2)n2nc(-c3ccco3)nc2n1 10.1021/jm101349u
CHEMBL1927634 69311 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 321 3 2 8 1.6 Nc1nc(NC(=O)c2ccccc2)n2nc(-c3ccco3)nc2n1 10.1021/jm101349u
51050844 69284 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 442 6 3 10 3.1 CC(C)(C)OC(=O)NCC1CCC(CNc2nc(N)n3nc(-c4ccco4)nc3n2)CC1 10.1021/jm101349u
CHEMBL1927427 69284 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 442 6 3 10 3.1 CC(C)(C)OC(=O)NCC1CCC(CNc2nc(N)n3nc(-c4ccco4)nc3n2)CC1 10.1021/jm101349u
145960813 161444 None 0 Human Functional pIC50 = 7.1 7.1 -1 3
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 339 4 2 7 4.0 Nc1nc(NCc2cccs2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
CHEMBL4125975 161444 None 0 Human Functional pIC50 = 7.1 7.1 -1 3
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 339 4 2 7 4.0 Nc1nc(NCc2cccs2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
54587016 60747 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 520 7 1 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CCN(Cc4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760890 60747 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 520 7 1 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CCN(Cc4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
10761800 188325 None 0 Human Functional pIC50 = 7.1 7.1 5 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 372 1 2 7 2.5 Cn1c(-c2cccc(C#N)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL49925 188325 None 0 Human Functional pIC50 = 7.1 7.1 5 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 372 1 2 7 2.5 Cn1c(-c2cccc(C#N)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
10688203 101780 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 335 1 1 5 3.3 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3CCCC3)nc21 10.1021/jm990499b
CHEMBL299548 101780 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 335 1 1 5 3.3 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3CCCC3)nc21 10.1021/jm990499b
45482082 200679 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 465 7 1 8 4.9 CCCCn1cc2c(nc(NC(=O)Cc3cccc4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL575386 200679 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 465 7 1 8 4.9 CCCCn1cc2c(nc(NC(=O)Cc3cccc4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
136042338 71188 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 449 8 2 9 2.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955914 71188 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 449 8 2 9 2.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
57402118 69803 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 493 7 2 8 5.2 COc1ccc(NC(=O)Nc2nc3cn(CCc4ccccc4)cc3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
CHEMBL1935749 69803 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 493 7 2 8 5.2 COc1ccc(NC(=O)Nc2nc3cn(CCc4ccccc4)cc3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
135546649 116700 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 479 9 2 9 2.4 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(C)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL33695 116700 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 479 9 2 9 2.4 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(C)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
145436760 162236 None 0 Human Functional pIC50 = 7.1 7.1 -2089 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 329 4 2 8 3.6 Nc1nc(NCc2cccs2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4161758 162236 None 0 Human Functional pIC50 = 7.1 7.1 -2089 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 329 4 2 8 3.6 Nc1nc(NCc2cccs2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
10570068 185990 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 353 1 2 7 2.7 Cn1c(-c2cccs2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL48683 185990 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 353 1 2 7 2.7 Cn1c(-c2cccs2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
145962310 161462 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 3 7 3.7 Nc1nc(NCCc2ccc(O)cc2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
CHEMBL4126116 161462 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 3 7 3.7 Nc1nc(NCCc2ccc(O)cc2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
46882997 5642 None 0 Human Functional pIC50 = 6.1 6.1 -3 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 275 2 1 6 2.9 Cc1ccc(C(=O)c2nc(N)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1077751 5642 None 0 Human Functional pIC50 = 6.1 6.1 -3 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 275 2 1 6 2.9 Cc1ccc(C(=O)c2nc(N)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
10807613 189605 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 347 1 2 6 2.7 Cn1c(-c2ccccc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL51394 189605 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 347 1 2 6 2.7 Cn1c(-c2ccccc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
127035806 137461 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 425 7 2 8 3.6 O=C(Cc1ccccc1)Nc1nc(NCc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2015.12.019
CHEMBL3753079 137461 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 425 7 2 8 3.6 O=C(Cc1ccccc1)Nc1nc(NCc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2015.12.019
49797853 10852 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 403 6 2 6 3.0 COc1ccc(N(CCO)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172267 10852 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 403 6 2 6 3.0 COc1ccc(N(CCO)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
10618828 102043 None 0 Human Functional pIC50 = 7.1 7.1 5 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 365 1 2 6 2.8 Cn1c(-c2ccccc2F)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL301512 102043 None 0 Human Functional pIC50 = 7.1 7.1 5 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 365 1 2 6 2.8 Cn1c(-c2ccccc2F)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
57393433 69813 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 494 7 2 9 4.6 COc1ccc(NC(=O)Nc2nc3cnn(CCc4ccccc4)c3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
CHEMBL1935758 69813 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 494 7 2 9 4.6 COc1ccc(NC(=O)Nc2nc3cnn(CCc4ccccc4)c3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
45481621 200365 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 491 8 1 8 5.3 CCCCn1cc2c(nc(NC(=O)C(c3ccccc3)c3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL572906 200365 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 491 8 1 8 5.3 CCCCn1cc2c(nc(NC(=O)C(c3ccccc3)c3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
145961937 161550 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 341 4 2 9 2.8 Nc1nc(NCc2cccs2)nc2sc(-c3cnccn3)nc12 10.1016/j.bmc.2018.05.048
CHEMBL4127472 161550 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 341 4 2 9 2.8 Nc1nc(NCc2cccs2)nc2sc(-c3cnccn3)nc12 10.1016/j.bmc.2018.05.048
57325915 74753 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 362 2 0 6 3.9 O=c1c(-c2ccco2)nnc2n(-c3ccccc3)c3ccc(Cl)cc3n12 10.1021/jm201177b
CHEMBL2030708 74753 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 362 2 0 6 3.9 O=c1c(-c2ccco2)nnc2n(-c3ccccc3)c3ccc(Cl)cc3n12 10.1021/jm201177b
49797828 10769 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 431 6 1 7 3.2 COC(=O)CN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171525 10769 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 431 6 1 7 3.2 COC(=O)CN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
136042343 71193 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 501 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)c(F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955919 71193 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 501 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)c(F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
54582166 60745 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 7 2 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CC[C@H](NC(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760888 60745 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 7 2 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CC[C@H](NC(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
54581143 60746 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 7 2 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CC[C@@H](NC(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760889 60746 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 7 2 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CC[C@@H](NC(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
53248700 60754 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 536 5 2 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)N3CCC(O)(c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760899 60754 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 536 5 2 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)N3CCC(O)(c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
156821421 186325 None 0 Human Functional pIC50 = 8.1 8.1 -16 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 443 4 2 9 2.4 Cn1cc(-c2c(-c3ccccc3)nc(N)n3nc([C@H](O)c4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
CHEMBL4873266 186325 None 0 Human Functional pIC50 = 8.1 8.1 -16 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 443 4 2 9 2.4 Cn1cc(-c2c(-c3ccccc3)nc(N)n3nc([C@H](O)c4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
145436764 162081 None 0 Human Functional pIC50 = 8.1 8.1 -22 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 329 4 2 8 3.6 Nc1nc(NCc2ccsc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4159215 162081 None 0 Human Functional pIC50 = 8.1 8.1 -22 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 329 4 2 8 3.6 Nc1nc(NCc2ccsc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
135874424 95901 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 469 8 2 8 2.9 CCCn1c(=O)c2[nH]c(-c3ccn(CC(=O)Nc4ccc(Cl)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL258987 95901 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 469 8 2 8 2.9 CCCn1c(=O)c2[nH]c(-c3ccn(CC(=O)Nc4ccc(Cl)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
136042327 71170 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 512 8 2 9 3.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc6ccccc6cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955893 71170 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 512 8 2 9 3.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc6ccccc6cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
135416058 491 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 530 8 1 11 -0.5 C=CCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)N3CCN(CC3)c3ccccc3)/N=c2c(=O)n(c1=O)CC=C 10.1021/jm0309654
442 491 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 530 8 1 11 -0.5 C=CCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)N3CCN(CC3)c3ccccc3)/N=c2c(=O)n(c1=O)CC=C 10.1021/jm0309654
CHEMBL2113342 491 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 530 8 1 11 -0.5 C=CCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)N3CCN(CC3)c3ccccc3)/N=c2c(=O)n(c1=O)CC=C 10.1021/jm0309654
5606 1644 None 20 Rat Functional pIC50 = 5.1 5.1 -316 7
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 375 5 1 4 3.8 OCC[C@H]1CCCCN1C(=O)/C=C/c1c(nn2c1cccc2)c1ccccc1 10.1021/jm990499b
6439091 1644 None 20 Rat Functional pIC50 = 5.1 5.1 -316 7
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 375 5 1 4 3.8 OCC[C@H]1CCCCN1C(=O)/C=C/c1c(nn2c1cccc2)c1ccccc1 10.1021/jm990499b
CHEMBL440115 1644 None 20 Rat Functional pIC50 = 5.1 5.1 -316 7
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 375 5 1 4 3.8 OCC[C@H]1CCCCN1C(=O)/C=C/c1c(nn2c1cccc2)c1ccccc1 10.1021/jm990499b
145436769 162899 None 0 Human Functional pIC50 = 7.1 7.1 -2041 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 313 4 2 8 3.1 Nc1nc(NCc2ccco2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4172399 162899 None 0 Human Functional pIC50 = 7.1 7.1 -2041 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 313 4 2 8 3.1 Nc1nc(NCc2ccco2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
56950235 69801 None 0 Human Functional pIC50 = 6.1 6.1 -10 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 403 4 2 8 3.5 COc1ccc(NC(=O)Nc2nc3cn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
CHEMBL1935747 69801 None 0 Human Functional pIC50 = 6.1 6.1 -10 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 403 4 2 8 3.5 COc1ccc(NC(=O)Nc2nc3cn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
57400353 69820 None 0 Human Functional pIC50 = 6.1 6.1 -3 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 432 6 2 9 3.8 CCCn1cc2nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc3c2n1 10.1016/j.bmc.2011.11.037
CHEMBL1935765 69820 None 0 Human Functional pIC50 = 6.1 6.1 -3 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 432 6 2 9 3.8 CCCn1cc2nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc3c2n1 10.1016/j.bmc.2011.11.037
45481771 200417 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 491 8 1 8 5.4 CCCCn1cc2c(nc(NC(=O)Cc3ccc(-c4ccccc4)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL573360 200417 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 491 8 1 8 5.4 CCCCn1cc2c(nc(NC(=O)Cc3ccc(-c4ccccc4)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
46883207 5981 None 0 Human Functional pIC50 = 6.1 6.1 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 347 5 1 7 3.3 O=C(c1ccncc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1080067 5981 None 0 Human Functional pIC50 = 6.1 6.1 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 347 5 1 7 3.3 O=C(c1ccncc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
135493279 100436 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 483 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm201292w
CHEMBL289903 100436 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 483 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm201292w
135493279 100436 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 483 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL289903 100436 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 483 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
45481759 200799 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 505 8 1 8 5.6 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(-c4ccccc4)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL576351 200799 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 505 8 1 8 5.6 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(-c4ccccc4)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
45481753 201319 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 407 4 1 8 3.1 Cn1cc2c(nc(NC(=O)Cc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL583960 201319 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 407 4 1 8 3.1 Cn1cc2c(nc(NC(=O)Cc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
56951623 71197 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 331 5 2 6 1.0 CCCn1c(=O)c2[nH]c(-c3cc(=O)[nH]n3C)cc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955923 71197 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 331 5 2 6 1.0 CCCn1c(=O)c2[nH]c(-c3cc(=O)[nH]n3C)cc2n(CCC)c1=O 10.1021/jm201292w
156821390 185342 None 0 Human Functional pIC50 = 8.0 8.0 -30 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 431 4 2 7 3.0 Nc1nc(-c2ccc(F)cc2)c(-c2ccc(=O)[nH]c2)c2nc(Cc3ccc(F)cn3)nn12 10.1021/acsmedchemlett.1c00620
CHEMBL4858144 185342 None 0 Human Functional pIC50 = 8.0 8.0 -30 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 431 4 2 7 3.0 Nc1nc(-c2ccc(F)cc2)c(-c2ccc(=O)[nH]c2)c2nc(Cc3ccc(F)cn3)nn12 10.1021/acsmedchemlett.1c00620
57398641 69798 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 282 3 1 7 2.3 CCCn1cc2nc(N)n3nc(-c4ccco4)nc3c2c1 10.1016/j.bmc.2011.11.037
CHEMBL1935744 69798 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 282 3 1 7 2.3 CCCn1cc2nc(N)n3nc(-c4ccco4)nc3c2c1 10.1016/j.bmc.2011.11.037
156821411 185805 None 0 Human Functional pIC50 = 7.0 7.0 -1 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 373 4 1 8 2.6 Nc1nc(-c2ccccc2)c(-c2ccnnc2)c2nc(CC3CCCO3)nn12 10.1021/acsmedchemlett.1c00620
CHEMBL4865474 185805 None 0 Human Functional pIC50 = 7.0 7.0 -1 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 373 4 1 8 2.6 Nc1nc(-c2ccccc2)c(-c2ccnnc2)c2nc(CC3CCCO3)nn12 10.1021/acsmedchemlett.1c00620
45482086 200322 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 421 7 1 9 3.8 CCCCn1cc2c(nc(NC(=O)Cc3ccsc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL572601 200322 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 421 7 1 9 3.8 CCCCn1cc2c(nc(NC(=O)Cc3ccsc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
57395120 69802 None 0 Human Functional pIC50 = 6.0 6.0 -18 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 431 6 2 8 4.4 CCCn1cc2nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc3c2c1 10.1016/j.bmc.2011.11.037
CHEMBL1935748 69802 None 0 Human Functional pIC50 = 6.0 6.0 -18 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 431 6 2 8 4.4 CCCn1cc2nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc3c2c1 10.1016/j.bmc.2011.11.037
145949481 162925 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 343 4 2 8 3.9 Cc1ccc(-c2nc3c(N)nc(NCc4cccs4)nc3s2)o1 10.1016/j.ejmech.2018.06.020
CHEMBL4172715 162925 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 343 4 2 8 3.9 Cc1ccc(-c2nc3c(N)nc(NCc4cccs4)nc3s2)o1 10.1016/j.ejmech.2018.06.020
45482094 200295 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 497 7 1 8 4.8 O=C(Cc1cccc(Cl)c1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2009.05.038
CHEMBL572386 200295 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 497 7 1 8 4.8 O=C(Cc1cccc(Cl)c1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2009.05.038
57391695 69823 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 337 3 1 8 3.0 Cn1ncc2nc(NC3CCCCC3)n3nc(-c4ccco4)nc3c21 10.1016/j.bmc.2011.11.037
CHEMBL1935768 69823 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 337 3 1 8 3.0 Cn1ncc2nc(NC3CCCCC3)n3nc(-c4ccco4)nc3c21 10.1016/j.bmc.2011.11.037
46883070 5682 None 0 Human Functional pIC50 = 7.0 7.0 1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 5 1 8 3.7 Cc1ccc(C(=O)c2nc(NCc3ccncn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1077902 5682 None 0 Human Functional pIC50 = 7.0 7.0 1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 5 1 8 3.7 Cc1ccc(C(=O)c2nc(NCc3ccncn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
135443378 109693 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 623 11 2 9 4.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(OCc5ccccc5C(F)(F)F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32229 109693 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 623 11 2 9 4.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(OCc5ccccc5C(F)(F)F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
45481756 200664 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 393 5 1 9 3.0 CCn1cc2c(nc(NC(=O)Cc3ccsc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL575198 200664 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 393 5 1 9 3.0 CCn1cc2c(nc(NC(=O)Cc3ccsc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
46883072 5705 None 0 Human Functional pIC50 = 6.0 6.0 -2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 6 1 7 4.3 Cc1ccc(C(=O)c2nc(NCCc3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078085 5705 None 0 Human Functional pIC50 = 6.0 6.0 -2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 6 1 7 4.3 Cc1ccc(C(=O)c2nc(NCCc3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
136042349 71173 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 480 8 2 9 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(F)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955898 71173 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 480 8 2 9 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(F)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
135522367 110726 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 493 8 2 10 2.0 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc5c(c4)OCO5)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32591 110726 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 493 8 2 10 2.0 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc5c(c4)OCO5)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
134133787 143575 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 397 7 2 9 3.6 COc1ccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1OC 10.1021/acs.jmedchem.6b01068
CHEMBL3898647 143575 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 397 7 2 9 3.6 COc1ccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1OC 10.1021/acs.jmedchem.6b01068
145436766 162622 None 0 Human Functional pIC50 = 7.0 7.0 -102 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2ccccn2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4167813 162622 None 0 Human Functional pIC50 = 7.0 7.0 -102 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2ccccn2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
155516071 170152 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 389 5 3 8 1.4 NCCC(=O)Nc1ccc(-c2cn3c(=O)n(-c4ccccc4)nc3c(N)n2)cc1 10.1021/acs.jmedchem.9b00778
CHEMBL4442908 170152 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 389 5 3 8 1.4 NCCC(=O)Nc1ccc(-c2cn3c(=O)n(-c4ccccc4)nc3c(N)n2)cc1 10.1021/acs.jmedchem.9b00778
10570586 189161 None 0 Rat Functional pIC50 = 6.0 6.0 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 361 1 2 6 3.0 Cc1cccc(-c2nc3c(N)nc(C#CC4(O)CCCCC4)nc3n2C)c1 10.1021/jm990499b
CHEMBL50950 189161 None 0 Rat Functional pIC50 = 6.0 6.0 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 361 1 2 6 3.0 Cc1cccc(-c2nc3c(N)nc(C#CC4(O)CCCCC4)nc3n2C)c1 10.1021/jm990499b
5606 1644 None 20 Human Functional pIC50 = 6.0 6.0 -38 7
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 375 5 1 4 3.8 OCC[C@H]1CCCCN1C(=O)/C=C/c1c(nn2c1cccc2)c1ccccc1 10.1021/jm990499b
6439091 1644 None 20 Human Functional pIC50 = 6.0 6.0 -38 7
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 375 5 1 4 3.8 OCC[C@H]1CCCCN1C(=O)/C=C/c1c(nn2c1cccc2)c1ccccc1 10.1021/jm990499b
CHEMBL440115 1644 None 20 Human Functional pIC50 = 6.0 6.0 -38 7
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 375 5 1 4 3.8 OCC[C@H]1CCCCN1C(=O)/C=C/c1c(nn2c1cccc2)c1ccccc1 10.1021/jm990499b
44587956 174876 None 0 Rat Functional pKd = 9.3 9.3 - 0
Antagonist activity at adenosine A2B receptor in Wistar-Kyoto rat distal colon assessed as inhibition of bethanecol-induced contractionAntagonist activity at adenosine A2B receptor in Wistar-Kyoto rat distal colon assessed as inhibition of bethanecol-induced contraction
ChEMBL 554 9 3 7 4.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL456125 174876 None 0 Rat Functional pKd = 9.3 9.3 - 0
Antagonist activity at adenosine A2B receptor in Wistar-Kyoto rat distal colon assessed as inhibition of bethanecol-induced contractionAntagonist activity at adenosine A2B receptor in Wistar-Kyoto rat distal colon assessed as inhibition of bethanecol-induced contraction
ChEMBL 554 9 3 7 4.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
11632785 73561 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 404 5 2 6 2.3 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL201721 73561 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 404 5 2 6 2.3 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
136 3292 None 26 Rat Functional pKd = 7.9 7.9 - 2
In vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidineIn vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidine
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00360a008
223 3292 None 26 Rat Functional pKd = 7.9 7.9 - 2
In vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidineIn vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidine
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00360a008
643606 3292 None 26 Rat Functional pKd = 7.9 7.9 - 2
In vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidineIn vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidine
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00360a008
CHEMBL10347 3292 None 26 Rat Functional pKd = 7.9 7.9 - 2
In vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidineIn vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidine
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00360a008
44574165 189576 None 0 Rat Functional pKd = 8.7 8.7 - 0
Antagonist activity at adenosine A2B receptor in Wistar-Kyoto rat colon assessed as inhibition of bethanecol-induced contraction after 30 minsAntagonist activity at adenosine A2B receptor in Wistar-Kyoto rat colon assessed as inhibition of bethanecol-induced contraction after 30 mins
ChEMBL 410 4 2 7 3.0 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccsc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL513681 189576 None 0 Rat Functional pKd = 8.7 8.7 - 0
Antagonist activity at adenosine A2B receptor in Wistar-Kyoto rat colon assessed as inhibition of bethanecol-induced contraction after 30 minsAntagonist activity at adenosine A2B receptor in Wistar-Kyoto rat colon assessed as inhibition of bethanecol-induced contraction after 30 mins
ChEMBL 410 4 2 7 3.0 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccsc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
11684443 133227 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL370378 133227 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11568001 72655 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 422 5 2 6 2.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL199446 72655 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 422 5 2 6 2.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
21874557 3996 None 45 Human Functional pKd = 7.5 7.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm800961g
5612 3996 None 45 Human Functional pKd = 7.5 7.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm800961g
CHEMBL447664 3996 None 45 Human Functional pKd = 7.5 7.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm800961g
DB06625 3996 None 45 Human Functional pKd = 7.5 7.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm800961g
11642035 73570 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 512 6 2 7 3.0 COc1cc(OCC(=O)Nc2ccc(Br)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
CHEMBL201750 73570 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 512 6 2 7 3.0 COc1cc(OCC(=O)Nc2ccc(Br)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
11642035 73570 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 512 6 2 7 3.0 COc1cc(OCC(=O)Nc2ccc(Br)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
CHEMBL201750 73570 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 512 6 2 7 3.0 COc1cc(OCC(=O)Nc2ccc(Br)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
11568001 72655 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 422 5 2 6 2.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL199446 72655 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 422 5 2 6 2.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11632785 73561 None 0 Human Functional pKd = 7.3 7.3 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 404 5 2 6 2.3 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL201721 73561 None 0 Human Functional pKd = 7.3 7.3 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 404 5 2 6 2.3 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11649145 135273 None 0 Human Functional pKd = 8.2 8.2 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 508 8 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(-c5ccccc5)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL372148 135273 None 0 Human Functional pKd = 8.2 8.2 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 508 8 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(-c5ccccc5)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11640539 140986 None 0 Human Functional pKd = 8.2 8.2 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 429 5 2 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL382135 140986 None 0 Human Functional pKd = 8.2 8.2 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 429 5 2 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11640539 140986 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 429 5 2 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL382135 140986 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 429 5 2 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11649145 135273 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 508 8 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(-c5ccccc5)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL372148 135273 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 508 8 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(-c5ccccc5)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11684443 133227 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL370378 133227 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
52950040 19167 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 523 10 2 5 6.1 CC[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289569 19167 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 523 10 2 5 6.1 CC[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
52945195 19186 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 525 10 3 6 4.7 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)N[C@@H](CO)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289676 19186 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 525 10 3 6 4.7 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)N[C@@H](CO)c1ccccc1 10.1016/j.bmcl.2010.10.030
450 2970 None 7 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1016/j.ejmech.2010.04.039
454 2970 None 7 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1016/j.ejmech.2010.04.039
5311041 2970 None 7 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1016/j.ejmech.2010.04.039
CHEMBL485862 2970 None 7 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1016/j.ejmech.2010.04.039
44574165 189576 None 0 Human Functional pKi = 9.1 9.1 - 0
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 410 4 2 7 3.0 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccsc4)cc3)cc2n(C)c1=O 10.1016/j.ejmech.2017.05.035
CHEMBL513681 189576 None 0 Human Functional pKi = 9.1 9.1 - 0
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 410 4 2 7 3.0 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccsc4)cc3)cc2n(C)c1=O 10.1016/j.ejmech.2017.05.035
66894241 157905 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP productionAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP production
ChEMBL 543 8 1 8 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
CHEMBL4083317 157905 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP productionAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP production
ChEMBL 543 8 1 8 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
66894241 157905 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 543 8 1 8 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4083317 157905 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 543 8 1 8 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
52946453 19230 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 521 9 2 5 5.6 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NC1(c2ccccc2)CC1 10.1016/j.bmcl.2010.10.030
CHEMBL1290001 19230 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 521 9 2 5 5.6 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NC1(c2ccccc2)CC1 10.1016/j.bmcl.2010.10.030
145958145 162171 None 0 Human Functional pKi = 9.0 9.0 - 0
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 606 7 1 9 4.5 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(O[C@@H](C)C(=O)N4CCN(c5nc6ccc(Cl)cc6s5)CC4)cc3)cc21 10.1016/j.ejmech.2017.05.035
CHEMBL4160732 162171 None 0 Human Functional pKi = 9.0 9.0 - 0
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 606 7 1 9 4.5 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(O[C@@H](C)C(=O)N4CCN(c5nc6ccc(Cl)cc6s5)CC4)cc3)cc21 10.1016/j.ejmech.2017.05.035
50925499 19243 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 523 9 2 5 5.9 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290101 19243 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 523 9 2 5 5.9 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
3284 3216 None 29 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02169
44185871 3216 None 29 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02169
5728 3216 None 29 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02169
CHEMBL483688 3216 None 29 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02169
145971695 163123 None 0 Human Functional pKi = 8.9 8.9 - 0
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 496 5 2 6 3.4 C[C@H](Oc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)C(=O)Nc1ccc(Br)cc1 10.1016/j.ejmech.2017.05.035
CHEMBL4175851 163123 None 0 Human Functional pKi = 8.9 8.9 - 0
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 496 5 2 6 3.4 C[C@H](Oc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)C(=O)Nc1ccc(Br)cc1 10.1016/j.ejmech.2017.05.035
3287 2642 None 33 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1021/jm990421v
5139184 2642 None 33 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1021/jm990421v
CHEMBL17002 2642 None 33 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1021/jm990421v
3287 2642 None 33 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1016/j.ejmech.2010.04.039
5139184 2642 None 33 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1016/j.ejmech.2010.04.039
CHEMBL17002 2642 None 33 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1016/j.ejmech.2010.04.039
9825550 57609 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 461 9 2 7 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16677 57609 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 461 9 2 7 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
10839296 58160 None 1 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 506 10 2 9 3.3 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc([N+](=O)[O-])cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16787 58160 None 1 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 506 10 2 9 3.3 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc([N+](=O)[O-])cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
52943652 19259 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 509 9 2 5 5.7 C[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290210 19259 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 509 9 2 5 5.7 C[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
9846447 58778 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 447 7 2 7 2.9 CCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C)cc4)cc3)[nH]c2n(CC)c1=O 10.1021/jm990421v
CHEMBL16866 58778 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 447 7 2 7 2.9 CCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C)cc4)cc3)[nH]c2n(CC)c1=O 10.1021/jm990421v
44236539 156884 None 0 Human Functional pKi = 8.7 8.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 460 7 2 8 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C(=O)O)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4070936 156884 None 0 Human Functional pKi = 8.7 8.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 460 7 2 8 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C(=O)O)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
145952391 163094 None 0 Human Functional pKi = 8.7 8.7 - 0
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 501 5 1 7 2.7 Cc1ccc(N2CCN(C(=O)[C@H](C)Oc3ccc(-c4cc5c([nH]4)c(=O)n(C)c(=O)n5C)cc3)CC2)cc1 10.1016/j.ejmech.2017.05.035
CHEMBL4175454 163094 None 0 Human Functional pKi = 8.7 8.7 - 0
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 501 5 1 7 2.7 Cc1ccc(N2CCN(C(=O)[C@H](C)Oc3ccc(-c4cc5c([nH]4)c(=O)n(C)c(=O)n5C)cc3)CC2)cc1 10.1016/j.ejmech.2017.05.035
44276476 168197 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 475 9 2 7 3.7 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL432664 168197 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 475 9 2 7 3.7 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
449 2643 None 38 Human Functional pKi = 8.7 8.7 1 4
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm990421v
453 2643 None 38 Human Functional pKi = 8.7 8.7 1 4
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm990421v
6603931 2643 None 38 Human Functional pKi = 8.7 8.7 1 4
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm990421v
CHEMBL273807 2643 None 38 Human Functional pKi = 8.7 8.7 1 4
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm990421v
449 2643 None 38 Human Functional pKi = 8.7 8.7 1 4
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
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.2010.04.039
453 2643 None 38 Human Functional pKi = 8.7 8.7 1 4
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
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.2010.04.039
6603931 2643 None 38 Human Functional pKi = 8.7 8.7 1 4
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
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.2010.04.039
CHEMBL273807 2643 None 38 Human Functional pKi = 8.7 8.7 1 4
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
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.2010.04.039
52948915 19302 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 541 9 2 5 6.0 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccc(F)cc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290437 19302 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 541 9 2 5 6.0 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccc(F)cc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
145982075 166578 None 0 Human Functional pKi = 6 6.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 379 6 1 9 2.8 CNc1ncc(C(=O)OCc2cccc(OC)c2)c2nc(-c3ccco3)nn12 10.1016/j.ejmech.2018.08.042
CHEMBL4278340 166578 None 0 Human Functional pKi = 6 6.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 379 6 1 9 2.8 CNc1ncc(C(=O)OCc2cccc(OC)c2)c2nc(-c3ccco3)nn12 10.1016/j.ejmech.2018.08.042
1329 1472 None 53 Human Functional pKi = 6 6.0 -9 8
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 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.bmc.2009.02.030
386 1472 None 53 Human Functional pKi = 6 6.0 -9 8
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 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.bmc.2009.02.030
CHEMBL183 1472 None 53 Human Functional pKi = 6 6.0 -9 8
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 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.bmc.2009.02.030
DB12946 1472 None 53 Human Functional pKi = 6 6.0 -9 8
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 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.bmc.2009.02.030
137661874 159396 None 0 Human Functional pKi = 6 6.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 405 4 2 7 3.0 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(O)CC3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4099688 159396 None 0 Human Functional pKi = 6 6.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 405 4 2 7 3.0 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(O)CC3)nc12 10.1021/acs.jmedchem.6b01584
145980971 166630 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 383 5 1 8 3.4 CNc1ncc(C(=O)OCc2cccc(Cl)c2)c2nc(-c3ccco3)nn12 10.1016/j.ejmech.2018.08.042
CHEMBL4279340 166630 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 383 5 1 8 3.4 CNc1ncc(C(=O)OCc2cccc(Cl)c2)c2nc(-c3ccco3)nn12 10.1016/j.ejmech.2018.08.042
145994259 167423 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 424 6 2 7 3.9 CNc1ncc(C(=O)NC(c2ccccc2)c2ccccc2)c2nc(-c3ccco3)nn12 10.1016/j.ejmech.2018.08.042
CHEMBL4294246 167423 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 424 6 2 7 3.9 CNc1ncc(C(=O)NC(c2ccccc2)c2ccccc2)c2nc(-c3ccco3)nn12 10.1016/j.ejmech.2018.08.042
118707857 113298 None 0 Human Functional pKi = 5 5.0 - 0
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 315 5 1 8 2.4 CCOC(=O)c1cnc(NC(C)C)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314890 113298 None 0 Human Functional pKi = 5 5.0 - 0
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 315 5 1 8 2.4 CCOC(=O)c1cnc(NC(C)C)n2nc(-c3ccco3)nc12 10.1021/jm500752h
118707863 113304 None 0 Human Functional pKi = 5 5.0 - 0
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 377 6 1 8 3.5 CCOC(=O)c1cnc(NCc2ccc(C)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314896 113304 None 0 Human Functional pKi = 5 5.0 - 0
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 377 6 1 8 3.5 CCOC(=O)c1cnc(NCc2ccc(C)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
155532918 171905 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based methodAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based method
ChEMBL 480 6 2 10 4.0 Cn1cc2c(nc(NCC3CCC(CNC(=O)OC(C)(C)C)CC3)n3nc(-c4ccco4)nc23)n1 10.1039/C9MD00014C
CHEMBL4468152 171905 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based methodAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based method
ChEMBL 480 6 2 10 4.0 Cn1cc2c(nc(NCC3CCC(CNC(=O)OC(C)(C)C)CC3)n3nc(-c4ccco4)nc23)n1 10.1039/C9MD00014C
52949999 19132 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 572 9 1 5 5.1 CN(Cc1ccc(Cl)c(Cl)c1)C(=O)COc1ccc2[nH]c(=O)c(S(C)(=O)=O)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
CHEMBL1289343 19132 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 572 9 1 5 5.1 CN(Cc1ccc(Cl)c(Cl)c1)C(=O)COc1ccc2[nH]c(=O)c(S(C)(=O)=O)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
11687483 163110 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 253 3 1 5 2.5 CCCn1c(-c2ccccc2)nc2c(N)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4175631 163110 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 253 3 1 5 2.5 CCCn1c(-c2ccccc2)nc2c(N)ncnc21 10.1016/j.ejmech.2018.03.067
2519 779 None 49 Human Functional pKi = 5.0 5.0 -17378 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2010.04.039
2519.0 779 None 49 Human Functional pKi = 5.0 5.0 -17378 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2010.04.039
407 779 None 49 Human Functional pKi = 5.0 5.0 -17378 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2010.04.039
463 779 None 49 Human Functional pKi = 5.0 5.0 -17378 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2010.04.039
CHEMBL113 779 None 49 Human Functional pKi = 5.0 5.0 -17378 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2010.04.039
DB00201 779 None 49 Human Functional pKi = 5.0 5.0 -17378 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2010.04.039
44572292 171515 None 0 Human Functional pKi = 6.0 6.0 - 0
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 255 1 1 5 1.8 CC(C)n1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL446264 171515 None 0 Human Functional pKi = 6.0 6.0 - 0
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 255 1 1 5 1.8 CC(C)n1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
123683 3121 None 46 Human Functional pKi = 5.0 5.0 -1258 5
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.ejmech.2018.08.042
422 3121 None 46 Human Functional pKi = 5.0 5.0 -1258 5
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.ejmech.2018.08.042
CHEMBL119709 3121 None 46 Human Functional pKi = 5.0 5.0 -1258 5
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.ejmech.2018.08.042
DB05511 3121 None 46 Human Functional pKi = 5.0 5.0 -1258 5
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.ejmech.2018.08.042
71455624 82985 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 309 3 1 8 2.2 Cn1cc2c(nc(NC3CCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181159 82985 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 309 3 1 8 2.2 Cn1cc2c(nc(NC3CCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
22002449 113284 None 0 Human Functional pKi = 6.0 6.0 - 0
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 273 3 1 8 1.1 CCOC(=O)c1cnc(N)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314876 113284 None 0 Human Functional pKi = 6.0 6.0 - 0
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 273 3 1 8 1.1 CCOC(=O)c1cnc(N)n2nc(-c3ccco3)nc12 10.1021/jm500752h
823558 15250 None 7 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 271 2 2 6 0.8 COc1ccc2c(C)nc(NC3=NCC(=O)N3)nc2c1 10.1016/j.ejmech.2010.04.039
CHEMBL1210817 15250 None 7 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 271 2 2 6 0.8 COc1ccc2c(C)nc(NC3=NCC(=O)N3)nc2c1 10.1016/j.ejmech.2010.04.039
10475082 74 None 23 Human Functional pKi = 5.9 5.9 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 383 4 4 9 0.8 OC[C@H]1O[C@H]([C@]([C@@H]1O)(C)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1016/j.bmc.2007.09.035
5591 74 None 23 Human Functional pKi = 5.9 5.9 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 383 4 4 9 0.8 OC[C@H]1O[C@H]([C@]([C@@H]1O)(C)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1016/j.bmc.2007.09.035
CHEMBL251997 74 None 23 Human Functional pKi = 5.9 5.9 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 383 4 4 9 0.8 OC[C@H]1O[C@H]([C@]([C@@H]1O)(C)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1016/j.bmc.2007.09.035
155562044 175874 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based methodAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based method
ChEMBL 426 7 2 10 3.0 Cn1cc2c(nc(NCCCCNC(=O)OC(C)(C)C)n3nc(-c4ccco4)nc23)n1 10.1039/C9MD00014C
CHEMBL4583657 175874 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based methodAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based method
ChEMBL 426 7 2 10 3.0 Cn1cc2c(nc(NCCCCNC(=O)OC(C)(C)C)n3nc(-c4ccco4)nc23)n1 10.1039/C9MD00014C
11681113 162352 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 309 4 1 6 2.7 CCn1c(-c2ccccc2)nc2c(NC3CCOC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4163630 162352 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 309 4 1 6 2.7 CCn1c(-c2ccccc2)nc2c(NC3CCOC3)ncnc21 10.1016/j.ejmech.2018.03.067
118707845 113285 None 0 Human Functional pKi = 5.9 5.9 - 0
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 377 4 3 7 2.4 CNC(=O)c1cnc(NC(=O)Nc2ccccc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314877 113285 None 0 Human Functional pKi = 5.9 5.9 - 0
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 377 4 3 7 2.4 CNC(=O)c1cnc(NC(=O)Nc2ccccc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
44572295 189150 None 0 Human Functional pKi = 5.9 5.9 - 0
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 269 2 1 5 2.1 CCC(C)n1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL509367 189150 None 0 Human Functional pKi = 5.9 5.9 - 0
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 269 2 1 5 2.1 CCC(C)n1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
44447535 95059 None 0 Human Functional pKi = 4.9 4.9 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 458 5 4 11 0.2 CNC(=S)OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCOC4)nc(Cl)nc32)[C@](C)(O)[C@@H]1O 10.1016/j.bmc.2007.09.035
CHEMBL254896 95059 None 0 Human Functional pKi = 4.9 4.9 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 458 5 4 11 0.2 CNC(=S)OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCOC4)nc(Cl)nc32)[C@](C)(O)[C@@H]1O 10.1016/j.bmc.2007.09.035
71457390 82955 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 359 4 1 8 3.4 C[C@@H](Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12)c1ccccc1 10.1021/jm300899q
CHEMBL2180932 82955 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 359 4 1 8 3.4 C[C@@H](Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12)c1ccccc1 10.1021/jm300899q
49863226 15224 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 311 3 1 9 0.6 Nc1nc(-n2cncn2)c2nnn(Cc3ccccc3F)c2n1 10.1016/j.ejmech.2010.04.039
CHEMBL1210734 15224 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 311 3 1 9 0.6 Nc1nc(-n2cncn2)c2nnn(Cc3ccccc3F)c2n1 10.1016/j.ejmech.2010.04.039
22002364 113279 None 0 Human Functional pKi = 4.9 4.9 - 0
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 423 8 1 10 3.2 CCOC(=O)c1cnc(NCc2ccc(OC)c(OC)c2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314871 113279 None 0 Human Functional pKi = 4.9 4.9 - 0
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 423 8 1 10 3.2 CCOC(=O)c1cnc(NCc2ccc(OC)c(OC)c2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
11659363 162813 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 295 3 1 6 2.2 Cn1c(-c2ccccc2)nc2c(NC3CCOC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4170873 162813 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 295 3 1 6 2.2 Cn1c(-c2ccccc2)nc2c(NC3CCOC3)ncnc21 10.1016/j.ejmech.2018.03.067
11568203 96297 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 432 5 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(C)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL260975 96297 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 432 5 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(C)c1=O 10.1016/j.ejmech.2010.04.039
66892244 159024 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 491 8 1 9 2.2 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(OC)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4095686 159024 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 491 8 1 9 2.2 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(OC)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
71412032 138359 None 3 Human Functional pKi = 6.9 6.9 - 0
Agonist activity at recombinant human adenosine A2B receptor assessed as cAMP accumulation preincubated for 45 mins followed by forskolin addition measured after 15 mins by protein kinase A-based assay in presence of [3H]cyclic AMP, rolipram, adenosine deaminaseAgonist activity at recombinant human adenosine A2B receptor assessed as cAMP accumulation preincubated for 45 mins followed by forskolin addition measured after 15 mins by protein kinase A-based assay in presence of [3H]cyclic AMP, rolipram, adenosine deaminase
ChEMBL 294 4 4 9 -1.4 CCNC[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00828
CHEMBL3770601 138359 None 3 Human Functional pKi = 6.9 6.9 - 0
Agonist activity at recombinant human adenosine A2B receptor assessed as cAMP accumulation preincubated for 45 mins followed by forskolin addition measured after 15 mins by protein kinase A-based assay in presence of [3H]cyclic AMP, rolipram, adenosine deaminaseAgonist activity at recombinant human adenosine A2B receptor assessed as cAMP accumulation preincubated for 45 mins followed by forskolin addition measured after 15 mins by protein kinase A-based assay in presence of [3H]cyclic AMP, rolipram, adenosine deaminase
ChEMBL 294 4 4 9 -1.4 CCNC[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00828
541903 57964 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 382 8 2 7 1.4 C=CCn1c(=O)c2nc(-c3ccc(OCC(=O)O)cc3)[nH]c2n(CC=C)c1=O 10.1021/jm990421v
CHEMBL16724 57964 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 382 8 2 7 1.4 C=CCn1c(=O)c2nc(-c3ccc(OCC(=O)O)cc3)[nH]c2n(CC=C)c1=O 10.1021/jm990421v
11529450 162872 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 293 4 1 5 3.5 CCn1c(-c2ccccc2)nc2c(NC3CCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4171919 162872 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 293 4 1 5 3.5 CCn1c(-c2ccccc2)nc2c(NC3CCC3)ncnc21 10.1016/j.ejmech.2018.03.067
18440405 136706 None 0 Human Functional pKi = 5.8 5.8 - 0
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 374 6 2 6 3.2 CCCn1c(Br)nc2c(N)nc(NCCc3ccccc3)nc21 10.1039/C5MD00034C
CHEMBL3739795 136706 None 0 Human Functional pKi = 5.8 5.8 - 0
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 374 6 2 6 3.2 CCCn1c(Br)nc2c(N)nc(NCCc3ccccc3)nc21 10.1039/C5MD00034C
52943652 19259 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 509 9 2 5 5.7 C[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290210 19259 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 509 9 2 5 5.7 C[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
9871761 59501 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 533 11 4 9 1.2 CCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(CC(=O)NCCN)cc4)cc3)[nH]c2n(CC)c1=O 10.1021/jm990421v
CHEMBL17141 59501 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 533 11 4 9 1.2 CCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(CC(=O)NCCN)cc4)cc3)[nH]c2n(CC)c1=O 10.1021/jm990421v
11610869 80287 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 393 5 3 8 -1.0 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)NCC(=O)O)cc3)[nH]c2n(C)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL213878 80287 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 393 5 3 8 -1.0 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)NCC(=O)O)cc3)[nH]c2n(C)c1=O 10.1016/j.ejmech.2010.04.039
9935943 59042 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 505 10 3 8 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16931 59042 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 505 10 3 8 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
541615 97578 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 385 8 2 7 1.2 CCCn1c(=O)c2nc(-c3ccc(OCC(N)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL27043 97578 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 385 8 2 7 1.2 CCCn1c(=O)c2nc(-c3ccc(OCC(N)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
10839228 59885 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 504 8 2 8 2.1 CCCn1c(=O)c2nc(-c3ccc(/C=C/C(=O)NN4C(=O)C(C)=C(C)C4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17294 59885 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 504 8 2 8 2.1 CCCn1c(=O)c2nc(-c3ccc(/C=C/C(=O)NN4C(=O)C(C)=C(C)C4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
414707 206098 None 10 Human Functional pKi = 4.8 4.8 - 0
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 177 1 1 5 1.0 CC(C)n1cnc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL67199 206098 None 10 Human Functional pKi = 4.8 4.8 - 0
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 177 1 1 5 1.0 CC(C)n1cnc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
118707866 113307 None 0 Human Functional pKi = 5.8 5.8 - 0
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 397 6 1 8 3.8 CCOC(=O)c1cnc(NCc2ccc(Cl)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314899 113307 None 0 Human Functional pKi = 5.8 5.8 - 0
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 397 6 1 8 3.8 CCOC(=O)c1cnc(NCc2ccc(Cl)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
317946 15223 None 2 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 272 1 1 7 0.3 Cn1c(=O)c2c(nc(-c3ccccc3)n2O)n(C)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL1210733 15223 None 2 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 272 1 1 7 0.3 Cn1c(=O)c2c(nc(-c3ccccc3)n2O)n(C)c1=O 10.1016/j.ejmech.2010.04.039
52950206 19118 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 476 8 2 5 3.7 CS(=O)(=O)c1c(CCc2ccccc2)c2cc(OCC(=O)Nc3ccccc3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
CHEMBL1289228 19118 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 476 8 2 5 3.7 CS(=O)(=O)c1c(CCc2ccccc2)c2cc(OCC(=O)Nc3ccccc3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
52946113 19278 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 522 8 3 4 6.2 CC(C)(NC(=O)NCc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290323 19278 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 522 8 3 4 6.2 CC(C)(NC(=O)NCc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL5080823 217195 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCn1c(=O)c2nc(C34CCC(C(=O)NCCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
247436 180353 None 26 Human Functional pKi = 5.8 5.8 - 0
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 177 2 1 5 0.8 CCCn1cnc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
247436 180353 None 26 Human Functional pKi = 5.8 5.8 - 0
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 177 2 1 5 0.8 CCCn1cnc2c(N)ncnc21 10.1039/C5MD00034C
CHEMBL475023 180353 None 26 Human Functional pKi = 5.8 5.8 - 0
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 177 2 1 5 0.8 CCCn1cnc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL475023 180353 None 26 Human Functional pKi = 5.8 5.8 - 0
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 177 2 1 5 0.8 CCCn1cnc2c(N)ncnc21 10.1039/C5MD00034C
452612 174607 None 11 Human Functional pKi = 4.8 4.8 - 0
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 189 1 1 5 1.1 Nc1ncnc2c1ncn2C1CCC1 10.1016/j.bmc.2009.02.030
CHEMBL455493 174607 None 11 Human Functional pKi = 4.8 4.8 - 0
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 189 1 1 5 1.1 Nc1ncnc2c1ncn2C1CCC1 10.1016/j.bmc.2009.02.030
52947452 19319 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 558 9 2 5 4.7 CS(=O)(=O)c1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
CHEMBL1290543 19319 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 558 9 2 5 4.7 CS(=O)(=O)c1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
1892 206503 None 56 Human Functional pKi = 4.8 4.8 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 224 2 1 7 -1.6 Cn1c(=O)c2c(ncn2CCO)n(C)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL699 206503 None 56 Human Functional pKi = 4.8 4.8 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 224 2 1 7 -1.6 Cn1c(=O)c2c(ncn2CCO)n(C)c1=O 10.1016/j.ejmech.2010.04.039
127038356 136797 None 0 Human Functional pKi = 5.8 5.8 - 0
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 360 5 2 6 3.2 CCCn1c(Br)nc2c(N)nc(NCc3ccccc3)nc21 10.1039/C5MD00034C
CHEMBL3740631 136797 None 0 Human Functional pKi = 5.8 5.8 - 0
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 360 5 2 6 3.2 CCCn1c(Br)nc2c(N)nc(NCc3ccccc3)nc21 10.1039/C5MD00034C
71462774 82984 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 295 3 1 8 1.8 Cn1cc2c(nc(NC3CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181158 82984 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 295 3 1 8 1.8 Cn1cc2c(nc(NC3CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
10624626 163232 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 482 8 2 7 3.1 O=C(O)COc1ccc(-c2nc3c(=O)n(Cc4ccccc4)c(=O)n(Cc4ccccc4)c3[nH]2)cc1 10.1021/jm990421v
CHEMBL417812 163232 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 482 8 2 7 3.1 O=C(O)COc1ccc(-c2nc3c(=O)n(Cc4ccccc4)c(=O)n(Cc4ccccc4)c3[nH]2)cc1 10.1021/jm990421v
127042993 136718 None 0 Human Functional pKi = 5.8 5.8 - 0
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 333 6 1 6 4.1 CCCn1c(-c2ccco2)nc2c(NCc3ccccc3)ncnc21 10.1039/C5MD00034C
CHEMBL3739903 136718 None 0 Human Functional pKi = 5.8 5.8 - 0
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 333 6 1 6 4.1 CCCn1c(-c2ccco2)nc2c(NCc3ccccc3)ncnc21 10.1039/C5MD00034C
127042996 136841 None 0 Human Functional pKi = 5.8 5.8 - 0
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 373 7 1 5 4.0 CCCn1c(Br)nc2c(NCCCc3ccccc3)ncnc21 10.1039/C5MD00034C
CHEMBL3741012 136841 None 0 Human Functional pKi = 5.8 5.8 - 0
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 373 7 1 5 4.0 CCCn1c(Br)nc2c(NCCCc3ccccc3)ncnc21 10.1039/C5MD00034C
2840092 203506 None 34 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 245 3 3 4 1.6 CCOc1cccc2c(C)nc(NC(=N)N)nc12 10.1016/j.ejmech.2010.04.039
CHEMBL602578 203506 None 34 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 245 3 3 4 1.6 CCOc1cccc2c(C)nc(NC(=N)N)nc12 10.1016/j.ejmech.2010.04.039
135438480 163013 None 0 Human Functional pKi = 4.8 4.8 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 309 3 2 6 3.1 Cn1c(-c2ccc(O)cc2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4174108 163013 None 0 Human Functional pKi = 4.8 4.8 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 309 3 2 6 3.1 Cn1c(-c2ccc(O)cc2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
135610070 72325 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 377 8 2 9 0.8 CCCn1c(=O)c2nc(-c3cc(OCC(=O)O)no3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
CHEMBL198326 72325 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 377 8 2 9 0.8 CCCn1c(=O)c2nc(-c3cc(OCC(=O)O)no3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
52947301 18986 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 517 9 2 4 5.8 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3cccnc3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1287832 18986 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 517 9 2 4 5.8 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3cccnc3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
127042997 136968 None 0 Human Functional pKi = 5.7 5.7 - 0
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 361 8 1 6 4.5 CCCn1c(-c2ccco2)nc2c(NCCCc3ccccc3)ncnc21 10.1039/C5MD00034C
CHEMBL3742158 136968 None 0 Human Functional pKi = 5.7 5.7 - 0
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 361 8 1 6 4.5 CCCn1c(-c2ccco2)nc2c(NCCCc3ccccc3)ncnc21 10.1039/C5MD00034C
118707851 113291 None 0 Human Functional pKi = 5.7 5.7 - 0
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 392 5 2 8 3.2 CCOC(=O)c1cnc(NC(=O)Nc2ccccc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314883 113291 None 0 Human Functional pKi = 5.7 5.7 - 0
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 392 5 2 8 3.2 CCOC(=O)c1cnc(NC(=O)Nc2ccccc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
44572293 178535 None 1 Human Functional pKi = 4.7 4.7 - 0
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 191 2 1 5 1.4 CCC(C)n1cnc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL466044 178535 None 1 Human Functional pKi = 4.7 4.7 - 0
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 191 2 1 5 1.4 CCC(C)n1cnc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
66892382 159245 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 559 9 1 9 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5ccc(OC(F)(F)F)cc5)C4=O)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4098127 159245 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 559 9 1 9 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5ccc(OC(F)(F)F)cc5)C4=O)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
52946159 19300 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 493 9 2 4 5.7 O=C(CCc1ccccc1)NCc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
CHEMBL1290435 19300 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 493 9 2 4 5.7 O=C(CCc1ccccc1)NCc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
52949755 19245 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 468 6 2 5 3.2 Cc1c(S(C)(=O)=O)c(=O)[nH]c2ccc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)cc12 10.1016/j.bmcl.2010.10.030
CHEMBL1290103 19245 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 468 6 2 5 3.2 Cc1c(S(C)(=O)=O)c(=O)[nH]c2ccc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)cc12 10.1016/j.bmcl.2010.10.030
118707865 113306 None 0 Human Functional pKi = 5.7 5.7 - 0
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 6 1 8 3.3 CCOC(=O)c1cnc(NCc2ccc(F)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314898 113306 None 0 Human Functional pKi = 5.7 5.7 - 0
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 6 1 8 3.3 CCOC(=O)c1cnc(NCc2ccc(F)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
9957239 59434 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 490 7 2 6 4.8 O=C(O)/C=C/c1ccc(-c2nc3c(=O)n(CC4CCCCC4)c(=O)n(CC4CCCCC4)c3[nH]2)cc1 10.1021/jm990421v
CHEMBL17103 59434 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 490 7 2 6 4.8 O=C(O)/C=C/c1ccc(-c2nc3c(=O)n(CC4CCCCC4)c(=O)n(CC4CCCCC4)c3[nH]2)cc1 10.1021/jm990421v
136086750 8723 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NSCA-induced cAMP accumulation pre-incubated for 15 mins by enzyme immunoassayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NSCA-induced cAMP accumulation pre-incubated for 15 mins by enzyme immunoassay
ChEMBL 349 3 4 6 1.9 N=C1c2c(C(N)=O)nc(-c3ccccc3O)n2CN1c1ccc(O)cc1 10.1016/j.bmc.2010.03.048
CHEMBL1095872 8723 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NSCA-induced cAMP accumulation pre-incubated for 15 mins by enzyme immunoassayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NSCA-induced cAMP accumulation pre-incubated for 15 mins by enzyme immunoassay
ChEMBL 349 3 4 6 1.9 N=C1c2c(C(N)=O)nc(-c3ccccc3O)n2CN1c1ccc(O)cc1 10.1016/j.bmc.2010.03.048
9912816 98487 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 475 10 2 7 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL275605 98487 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 475 10 2 7 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
11801496 98800 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 587 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL278039 98800 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 587 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
11801496 98800 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 587 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL278039 98800 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 587 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.ejmech.2010.04.039
10792296 98719 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 529 9 2 7 4.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(F)(F)F)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL277386 98719 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 529 9 2 7 4.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(F)(F)F)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
10767043 59040 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 479 9 2 7 3.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16929 59040 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 479 9 2 7 3.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
10840167 59196 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 539 9 2 7 4.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17003 59196 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 539 9 2 7 4.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
10720065 98450 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 495 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Cl)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL275427 98450 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 495 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Cl)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
9870718 60006 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 503 10 2 8 3.6 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4C(C)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17341 60006 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 503 10 2 8 3.6 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4C(C)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
72197880 90832 None 0 Human Functional pKi = 8.6 8.6 - 0
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 347 4 1 5 4.7 O=C(Nc1nc(-c2ccccc2)c(-c2ccncc2)s1)c1ccco1 10.1016/j.ejmech.2013.03.020
CHEMBL2391834 90832 None 0 Human Functional pKi = 8.6 8.6 - 0
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 347 4 1 5 4.7 O=C(Nc1nc(-c2ccccc2)c(-c2ccncc2)s1)c1ccco1 10.1016/j.ejmech.2013.03.020
52945195 19186 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 525 10 3 6 4.7 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)N[C@@H](CO)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289676 19186 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 525 10 3 6 4.7 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)N[C@@H](CO)c1ccccc1 10.1016/j.bmcl.2010.10.030
11849871 188937 None 0 Human Functional pKi = 6.7 6.7 - 0
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 255 2 1 5 1.6 CCCn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
11849871 188937 None 0 Human Functional pKi = 6.7 6.7 - 0
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 255 2 1 5 1.6 CCCn1c(Br)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
11849871 188937 None 0 Human Functional pKi = 6.7 6.7 - 0
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 255 2 1 5 1.6 CCCn1c(Br)nc2c(N)ncnc21 10.1039/C5MD00034C
CHEMBL506450 188937 None 0 Human Functional pKi = 6.7 6.7 - 0
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 255 2 1 5 1.6 CCCn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL506450 188937 None 0 Human Functional pKi = 6.7 6.7 - 0
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 255 2 1 5 1.6 CCCn1c(Br)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL506450 188937 None 0 Human Functional pKi = 6.7 6.7 - 0
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 255 2 1 5 1.6 CCCn1c(Br)nc2c(N)ncnc21 10.1039/C5MD00034C
137636304 156292 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 419 4 2 7 3.4 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(C)(O)CC3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4064207 156292 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 419 4 2 7 3.4 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(C)(O)CC3)nc12 10.1021/acs.jmedchem.6b01584
137645935 157668 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 446 6 1 8 3.5 COc1cnc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4080594 157668 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 446 6 1 8 3.5 COc1cnc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3)nc12 10.1021/acs.jmedchem.6b01584
22002375 113283 None 0 Human Functional pKi = 5.7 5.7 - 0
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 258 2 2 7 0.3 CNC(=O)c1cnc(N)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314875 113283 None 0 Human Functional pKi = 5.7 5.7 - 0
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 258 2 2 7 0.3 CNC(=O)c1cnc(N)n2nc(-c3ccco3)nc12 10.1021/jm500752h
18440417 136748 None 0 Human Functional pKi = 5.7 5.7 - 0
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 362 7 2 7 3.7 CCCn1c(-c2ccco2)nc2c(N)nc(NCCc3ccccc3)nc21 10.1039/C5MD00034C
CHEMBL3740141 136748 None 0 Human Functional pKi = 5.7 5.7 - 0
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 362 7 2 7 3.7 CCCn1c(-c2ccco2)nc2c(N)nc(NCCc3ccccc3)nc21 10.1039/C5MD00034C
118707867 113308 None 0 Human Functional pKi = 5.7 5.7 - 0
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 431 6 1 8 4.2 CCOC(=O)c1cnc(NCc2ccc(C(F)(F)F)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314900 113308 None 0 Human Functional pKi = 5.7 5.7 - 0
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 431 6 1 8 4.2 CCOC(=O)c1cnc(NCc2ccc(C(F)(F)F)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
52944930 19301 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 495 9 2 5 5.1 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290436 19301 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 495 9 2 5 5.1 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
459 2618 None 29 Human Functional pKi = 5.7 5.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm300323t
477 2618 None 29 Human Functional pKi = 5.7 5.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm300323t
5310960 2618 None 29 Human Functional pKi = 5.7 5.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm300323t
CHEMBL302765 2618 None 29 Human Functional pKi = 5.7 5.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm300323t
20592013 94658 None 0 Human Functional pKi = 6.7 6.7 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 371 4 4 10 -0.7 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCOC4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.09.035
CHEMBL252198 94658 None 0 Human Functional pKi = 6.7 6.7 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 371 4 4 10 -0.7 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCOC4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.09.035
21874755 176997 None 1 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 336 4 2 8 1.8 Nc1nc(-c2ccco2)c2nnn(Cc3cccc(C(=O)O)c3)c2n1 10.1016/j.ejmech.2010.04.039
CHEMBL461656 176997 None 1 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 336 4 2 8 1.8 Nc1nc(-c2ccco2)c2nnn(Cc3cccc(C(=O)O)c3)c2n1 10.1016/j.ejmech.2010.04.039
71450241 82972 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 269 2 1 8 1.3 CNc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181147 82972 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 269 2 1 8 1.3 CNc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
71453892 82973 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 283 3 1 8 1.7 CCNc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181148 82973 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 283 3 1 8 1.7 CCNc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
24827444 96397 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 365 5 1 8 1.6 CCCn1c(=O)c2[nH]c(-c3cnn(-c4cccnc4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL261526 96397 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 365 5 1 8 1.6 CCCn1c(=O)c2[nH]c(-c3cnn(-c4cccnc4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2010.04.039
9870396 139124 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 494 7 1 7 4.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(C(F)(F)F)ccc4Cl)c3)[nH]c2n(CCC)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL378598 139124 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 494 7 1 7 4.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(C(F)(F)F)ccc4Cl)c3)[nH]c2n(CCC)c1=O 10.1016/j.ejmech.2010.04.039
21916394 160907 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 458 6 1 7 3.2 CCn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc21 10.1016/j.ejmech.2010.04.039
CHEMBL411452 160907 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 458 6 1 7 3.2 CCn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc21 10.1016/j.ejmech.2010.04.039
CHEMBL5074992 216838 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCCn1c(=O)c2nc(C34CCC(C(=O)NCCOCCOCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
9929470 110536 None 0 Human Functional pKi = 6.7 6.7 - 1
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 374 3 2 8 2.9 Cn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm500752h
CHEMBL324735 110536 None 0 Human Functional pKi = 6.7 6.7 - 1
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 374 3 2 8 2.9 Cn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm500752h
118707859 113300 None 0 Human Functional pKi = 5.7 5.7 - 0
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 313 5 1 8 2.1 CCOC(=O)c1cnc(NC2CC2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314892 113300 None 0 Human Functional pKi = 5.7 5.7 - 0
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 313 5 1 8 2.1 CCOC(=O)c1cnc(NC2CC2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
158795 3770 None 33 Human Functional pKi = 6.6 6.6 - 2
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 337 4 4 10 -1.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H]1COCC1 10.1016/j.bmc.2007.09.035
5592 3770 None 33 Human Functional pKi = 6.6 6.6 - 2
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 337 4 4 10 -1.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H]1COCC1 10.1016/j.bmc.2007.09.035
CHEMBL392149 3770 None 33 Human Functional pKi = 6.6 6.6 - 2
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 337 4 4 10 -1.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H]1COCC1 10.1016/j.bmc.2007.09.035
DB04954 3770 None 33 Human Functional pKi = 6.6 6.6 - 2
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 337 4 4 10 -1.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H]1COCC1 10.1016/j.bmc.2007.09.035
99619 205929 None 16 Human Functional pKi = 4.6 4.6 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 223 2 1 7 -1.6 Cn1c(=O)c2c(ncn2CCN)n(C)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL66011 205929 None 16 Human Functional pKi = 4.6 4.6 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 223 2 1 7 -1.6 Cn1c(=O)c2c(ncn2CCN)n(C)c1=O 10.1016/j.ejmech.2010.04.039
101874280 113295 None 0 Human Functional pKi = 5.6 5.6 - 0
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 287 4 1 8 1.6 CCOC(=O)c1cnc(NC)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314887 113295 None 0 Human Functional pKi = 5.6 5.6 - 0
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 287 4 1 8 1.6 CCOC(=O)c1cnc(NC)n2nc(-c3ccco3)nc12 10.1021/jm500752h
22002319 113281 None 0 Human Functional pKi = 5.6 5.6 - 0
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 408 7 2 9 2.4 CNC(=O)c1cnc(NCc2ccc(OC)c(OC)c2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314873 113281 None 0 Human Functional pKi = 5.6 5.6 - 0
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 408 7 2 9 2.4 CNC(=O)c1cnc(NCc2ccc(OC)c(OC)c2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
1330 163313 None 29 Human Functional pKi = 6.6 6.6 - 3
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 392 6 2 7 1.6 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
CHEMBL418333 163313 None 29 Human Functional pKi = 6.6 6.6 - 3
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 392 6 2 7 1.6 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
CHEMBL435575 163313 None 29 Human Functional pKi = 6.6 6.6 - 3
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 392 6 2 7 1.6 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
9887859 113576 None 0 Human Functional pKi = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL118923 113576 None 0 Human Functional pKi = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL332091 113576 None 0 Human Functional pKi = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
76331702 103753 None 0 Human Functional pKi = 6.6 6.6 - 0
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 243 3 1 6 2.1 CCCn1c(-c2ccco2)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL3087706 103753 None 0 Human Functional pKi = 6.6 6.6 - 0
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 243 3 1 6 2.1 CCCn1c(-c2ccco2)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
76335304 103755 None 0 Human Functional pKi = 5.6 5.6 - 0
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 333 4 1 6 2.8 Cn1c(-c2ccco2)nc2c(NC(=O)Cc3ccccc3)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL3087708 103755 None 0 Human Functional pKi = 5.6 5.6 - 0
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 333 4 1 6 2.8 Cn1c(-c2ccco2)nc2c(NC(=O)Cc3ccccc3)ncnc21 10.1016/j.ejmech.2013.10.006
118707862 113303 None 0 Human Functional pKi = 5.6 5.6 - 0
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 363 6 1 8 3.2 CCOC(=O)c1cnc(NCc2ccccc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314895 113303 None 0 Human Functional pKi = 5.6 5.6 - 0
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 363 6 1 8 3.2 CCOC(=O)c1cnc(NCc2ccccc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
76331702 103753 None 0 Human Functional pKi = 6.6 6.6 - 0
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 243 3 1 6 2.1 CCCn1c(-c2ccco2)nc2c(N)ncnc21 10.1039/C5MD00034C
CHEMBL3087706 103753 None 0 Human Functional pKi = 6.6 6.6 - 0
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 243 3 1 6 2.1 CCCn1c(-c2ccco2)nc2c(N)ncnc21 10.1039/C5MD00034C
11587927 162768 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 327 3 1 5 4.0 Cn1c(-c2cccc(Cl)c2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4170180 162768 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 327 3 1 5 4.0 Cn1c(-c2cccc(Cl)c2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL5089483 217699 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCCn1c(=O)c2nc(C34CCC(C(=O)NCCCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
9936058 59577 None 2 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 508 9 2 9 1.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NN4C(=O)C(C)=C(C)C4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17173 59577 None 2 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 508 9 2 9 1.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NN4C(=O)C(C)=C(C)C4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
377 2758 None 42 Rat Functional pKi = 5.6 5.6 - 10
Activity against Adenosine A2B receptor as cAMP production in VA-13 cellsActivity against Adenosine A2B receptor as cAMP production in VA-13 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9802822
425 2758 None 42 Rat Functional pKi = 5.6 5.6 - 10
Activity against Adenosine A2B receptor as cAMP production in VA-13 cellsActivity against Adenosine A2B receptor as cAMP production in VA-13 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9802822
448222 2758 None 42 Rat Functional pKi = 5.6 5.6 - 10
Activity against Adenosine A2B receptor as cAMP production in VA-13 cellsActivity against Adenosine A2B receptor as cAMP production in VA-13 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9802822
CHEMBL464859 2758 None 42 Rat Functional pKi = 5.6 5.6 - 10
Activity against Adenosine A2B receptor as cAMP production in VA-13 cellsActivity against Adenosine A2B receptor as cAMP production in VA-13 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9802822
71462773 82977 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 311 4 1 8 2.5 CC[C@H](C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181151 82977 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 311 4 1 8 2.5 CC[C@H](C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
71457391 82958 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 379 4 1 8 3.5 Cn1cc2c(nc(NCc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2180935 82958 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 379 4 1 8 3.5 Cn1cc2c(nc(NCc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
71457407 82986 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 323 3 1 8 2.6 Cn1cc2c(nc(NC3CCCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181160 82986 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 323 3 1 8 2.6 Cn1cc2c(nc(NC3CCCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
52942475 19261 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 489 9 2 5 5.7 CC(C)CCc1c(-c2nccs2)c(=O)[nH]c2ccc(OCC(=O)NC(C)(C)c3ccccc3)cc12 10.1016/j.bmcl.2010.10.030
CHEMBL1290212 19261 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 489 9 2 5 5.7 CC(C)CCc1c(-c2nccs2)c(=O)[nH]c2ccc(OCC(=O)NC(C)(C)c3ccccc3)cc12 10.1016/j.bmcl.2010.10.030
42636897 172743 None 20 Human Functional pKi = 5.6 5.6 - 0
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 379 4 3 8 1.3 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(NC4CC5CCC4C5)ncnc32)[C@@H]1O 10.1021/jm801456g
CHEMBL449575 172743 None 20 Human Functional pKi = 5.6 5.6 - 0
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 379 4 3 8 1.3 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(NC4CC5CCC4C5)ncnc32)[C@@H]1O 10.1021/jm801456g
76331703 103759 None 0 Human Functional pKi = 5.6 5.6 - 0
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 453 7 1 7 4.7 Cc1ccc(COc2ccc(CC(=O)Nc3ncnc4c3nc(-c3ccco3)n4C)cc2)cc1 10.1016/j.ejmech.2013.10.006
CHEMBL3087712 103759 None 0 Human Functional pKi = 5.6 5.6 - 0
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 453 7 1 7 4.7 Cc1ccc(COc2ccc(CC(=O)Nc3ncnc4c3nc(-c3ccco3)n4C)cc2)cc1 10.1016/j.ejmech.2013.10.006
71462755 82963 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 359 5 1 8 2.9 Cn1cc2c(nc(NCCc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2180940 82963 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 359 5 1 8 2.9 Cn1cc2c(nc(NCCc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
44572469 179557 None 8 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 257 2 2 6 0.2 Nc1ncnc2c1nc(Br)n2CCO 10.1016/j.ejmech.2010.04.039
CHEMBL474058 179557 None 8 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 257 2 2 6 0.2 Nc1ncnc2c1nc(Br)n2CCO 10.1016/j.ejmech.2010.04.039
44572469 179557 None 8 Human Functional pKi = 5.6 5.6 - 0
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 257 2 2 6 0.2 Nc1ncnc2c1nc(Br)n2CCO 10.1016/j.bmc.2009.02.030
44572469 179557 None 8 Human Functional pKi = 5.6 5.6 - 0
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 257 2 2 6 0.2 Nc1ncnc2c1nc(Br)n2CCO 10.1016/j.ejmech.2013.10.006
CHEMBL474058 179557 None 8 Human Functional pKi = 5.6 5.6 - 0
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 257 2 2 6 0.2 Nc1ncnc2c1nc(Br)n2CCO 10.1016/j.bmc.2009.02.030
CHEMBL474058 179557 None 8 Human Functional pKi = 5.6 5.6 - 0
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 257 2 2 6 0.2 Nc1ncnc2c1nc(Br)n2CCO 10.1016/j.ejmech.2013.10.006
24882472 154744 None 0 Human Functional pKi = 5.6 5.6 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 456 5 4 10 1.4 CNC(=S)OC[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@](C)(O)[C@@H]1O 10.1016/j.bmc.2007.09.035
CHEMBL399514 154744 None 0 Human Functional pKi = 5.6 5.6 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 456 5 4 10 1.4 CNC(=S)OC[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@](C)(O)[C@@H]1O 10.1016/j.bmc.2007.09.035
71459268 82966 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 398 5 2 8 3.4 Cn1cc2c(nc(NCCc3c[nH]c4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181141 82966 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 398 5 2 8 3.4 Cn1cc2c(nc(NCCc3c[nH]c4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
9806649 59562 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 518 10 3 8 2.8 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)NC)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17167 59562 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 518 10 3 8 2.8 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)NC)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
11605883 79983 None 3 Human Functional pKi = 8.4 8.4 - 1
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL212625 79983 None 3 Human Functional pKi = 8.4 8.4 - 1
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1016/j.ejmech.2010.04.039
9892149 59644 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 499 9 2 7 4.2 CCCn1c(=O)c2nc(-c3ccc(/C=C/C(=O)Nc4ccccc4C(C)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17202 59644 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 499 9 2 7 4.2 CCCn1c(=O)c2nc(-c3ccc(/C=C/C(=O)Nc4ccccc4C(C)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
541759 170138 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 477 9 3 8 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL444281 170138 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 477 9 3 8 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
9936467 58109 None 1 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 519 10 2 9 3.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)OC)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16741 58109 None 1 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 519 10 2 9 3.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)OC)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
155544096 173410 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based methodAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based method
ChEMBL 440 8 2 10 3.4 Cn1cc2c(nc(NCCCCCNC(=O)OC(C)(C)C)n3nc(-c4ccco4)nc23)n1 10.1039/C9MD00014C
CHEMBL4526138 173410 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based methodAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based method
ChEMBL 440 8 2 10 3.4 Cn1cc2c(nc(NCCCCCNC(=O)OC(C)(C)C)n3nc(-c4ccco4)nc23)n1 10.1039/C9MD00014C
11053743 162973 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 239 2 1 5 2.1 CCn1c(-c2ccccc2)nc2c(N)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4173347 162973 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 239 2 1 5 2.1 CCn1c(-c2ccccc2)nc2c(N)ncnc21 10.1016/j.ejmech.2018.03.067
118707855 113296 None 0 Human Functional pKi = 5.5 5.5 - 0
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 301 5 1 8 2.0 CCNc1ncc(C(=O)OCC)c2nc(-c3ccco3)nn12 10.1021/jm500752h
CHEMBL3314888 113296 None 0 Human Functional pKi = 5.5 5.5 - 0
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 301 5 1 8 2.0 CCNc1ncc(C(=O)OCC)c2nc(-c3ccco3)nn12 10.1021/jm500752h
44447534 95034 None 0 Human Functional pKi = 4.5 4.5 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 442 5 4 11 0.0 CNC(=O)OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCOC4)nc(Cl)nc32)[C@](C)(O)[C@@H]1O 10.1016/j.bmc.2007.09.035
CHEMBL254693 95034 None 0 Human Functional pKi = 4.5 4.5 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 442 5 4 11 0.0 CNC(=O)OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCOC4)nc(Cl)nc32)[C@](C)(O)[C@@H]1O 10.1016/j.bmc.2007.09.035
136199393 19244 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 521 9 2 5 5.7 Cc1cc(-c2c(CCc3ccccc3)c3cc(OCC(=O)NC(C)(C)c4ccccc4)ccc3[nH]c2=O)on1 10.1016/j.bmcl.2010.10.030
CHEMBL1290102 19244 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 521 9 2 5 5.7 Cc1cc(-c2c(CCc3ccccc3)c3cc(OCC(=O)NC(C)(C)c4ccccc4)ccc3[nH]c2=O)on1 10.1016/j.bmcl.2010.10.030
52947452 19319 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 558 9 2 5 4.7 CS(=O)(=O)c1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
CHEMBL1290543 19319 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 558 9 2 5 4.7 CS(=O)(=O)c1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
71461028 82959 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 363 4 1 8 3.0 Cn1cc2c(nc(NCc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2180936 82959 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 363 4 1 8 3.0 Cn1cc2c(nc(NCc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
127038355 136795 None 0 Human Functional pKi = 5.5 5.5 - 0
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 359 6 1 5 3.7 CCCn1c(Br)nc2c(NCCc3ccccc3)ncnc21 10.1039/C5MD00034C
CHEMBL3740619 136795 None 0 Human Functional pKi = 5.5 5.5 - 0
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 359 6 1 5 3.7 CCCn1c(Br)nc2c(NCCc3ccccc3)ncnc21 10.1039/C5MD00034C
52941244 19258 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 509 9 2 5 5.7 C[C@@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290209 19258 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 509 9 2 5 5.7 C[C@@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
14426726 181743 None 0 Human Functional pKi = 5.5 5.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 353 4 3 8 1.0 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(NC4CCCC4)ncnc32)[C@@H]1O 10.1021/jm801456g
CHEMBL477444 181743 None 0 Human Functional pKi = 5.5 5.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 353 4 3 8 1.0 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(NC4CCCC4)ncnc32)[C@@H]1O 10.1021/jm801456g
9807634 59904 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 551 11 2 7 4.7 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NC(c4ccccc4)c4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17299 59904 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 551 11 2 7 4.7 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NC(c4ccccc4)c4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
52950027 19150 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 478 9 2 4 5.3 O=C(COc1ccc2[nH]c(=O)c(-c3ccco3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289461 19150 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 478 9 2 4 5.3 O=C(COc1ccc2[nH]c(=O)c(-c3ccco3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
71453874 82953 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 345 4 1 8 2.9 Cn1cc2c(nc(NCc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2180930 82953 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 345 4 1 8 2.9 Cn1cc2c(nc(NCc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
2519 779 None 49 Human Functional pKi = 4.5 4.5 -17378 8
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
2519.0 779 None 49 Human Functional pKi = 4.5 4.5 -17378 8
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
407 779 None 49 Human Functional pKi = 4.5 4.5 -17378 8
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
463 779 None 49 Human Functional pKi = 4.5 4.5 -17378 8
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
CHEMBL113 779 None 49 Human Functional pKi = 4.5 4.5 -17378 8
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
DB00201 779 None 49 Human Functional pKi = 4.5 4.5 -17378 8
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
52950028 19151 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 461 7 2 5 4.7 CC(C)(C)NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
CHEMBL1289462 19151 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 461 7 2 5 4.7 CC(C)(C)NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
11623934 162144 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 321 5 1 5 4.3 CCCn1c(-c2ccccc2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4160264 162144 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 321 5 1 5 4.3 CCCn1c(-c2ccccc2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
52941597 19099 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 357 5 1 4 2.7 COc1ccc2[nH]c(=O)c(S(C)(=O)=O)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
CHEMBL1289109 19099 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 357 5 1 4 2.7 COc1ccc2[nH]c(=O)c(S(C)(=O)=O)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
CHEMBL5092788 217879 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None C#CCCCCNC(=O)C12CCC(c3nc4c(=O)n(CCCC)c(=O)n(CCCNC(=O)c5ccc(S(=O)(=O)F)cc5)c4[nH]3)(CC1)CC2 10.1021/acs.jmedchem.0c02169
76335303 103754 None 0 Human Functional pKi = 6.5 6.5 - 0
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 259 4 2 7 1.1 Nc1ncnc2c1nc(-c1ccco1)n2CCCO 10.1016/j.ejmech.2013.10.006
CHEMBL3087707 103754 None 0 Human Functional pKi = 6.5 6.5 - 0
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 259 4 2 7 1.1 Nc1ncnc2c1nc(-c1ccco1)n2CCCO 10.1016/j.ejmech.2013.10.006
52945098 19360 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 504 9 1 6 3.4 Cn1c(=O)c(S(C)(=O)=O)c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccccc3)ccc21 10.1016/j.bmcl.2010.10.030
CHEMBL1290782 19360 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 504 9 1 6 3.4 Cn1c(=O)c(S(C)(=O)=O)c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccccc3)ccc21 10.1016/j.bmcl.2010.10.030
145987819 167250 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 363 5 1 8 3.3 CNc1ncc(C(=O)OC(C)c2ccccc2)c2nc(-c3ccco3)nn12 10.1016/j.ejmech.2018.08.042
CHEMBL4290842 167250 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 363 5 1 8 3.3 CNc1ncc(C(=O)OC(C)c2ccccc2)c2nc(-c3ccco3)nn12 10.1016/j.ejmech.2018.08.042
11492857 162445 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 279 3 1 5 3.0 Cn1c(-c2ccccc2)nc2c(NC3CCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4165013 162445 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 279 3 1 5 3.0 Cn1c(-c2ccccc2)nc2c(NC3CCC3)ncnc21 10.1016/j.ejmech.2018.03.067
11229946 103762 None 0 Human Functional pKi = 6.4 6.4 - 0
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 229 2 1 6 1.7 CCn1c(-c2ccco2)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL3087715 103762 None 0 Human Functional pKi = 6.4 6.4 - 0
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 229 2 1 6 1.7 CCn1c(-c2ccco2)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
71457405 82976 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 311 4 1 8 2.5 CCC(C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181150 82976 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 311 4 1 8 2.5 CCC(C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
71455619 82964 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 419 7 1 10 2.9 COc1ccc(CCNc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1OC 10.1021/jm300899q
CHEMBL2181139 82964 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 419 7 1 10 2.9 COc1ccc(CCNc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1OC 10.1021/jm300899q
10085373 10431 None 4 Human Functional pKi = 6.4 6.4 - 1
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 286 2 1 6 0.6 COc1ccc(-c2nc3c(=O)n(C)c(=O)n(C)c3[nH]2)cc1 10.1016/j.ejmech.2010.04.039
CHEMBL11635 10431 None 4 Human Functional pKi = 6.4 6.4 - 1
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 286 2 1 6 0.6 COc1ccc(-c2nc3c(=O)n(C)c(=O)n(C)c3[nH]2)cc1 10.1016/j.ejmech.2010.04.039
71455603 82956 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 359 4 1 8 3.2 Cc1ccc(CNc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm300899q
CHEMBL2180933 82956 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 359 4 1 8 3.2 Cc1ccc(CNc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm300899q
71455622 82979 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 325 6 1 8 2.9 CCCCCNc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181153 82979 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 325 6 1 8 2.9 CCCCCNc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
57429649 159034 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP productionAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP production
ChEMBL 572 8 1 9 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5cccc(C(F)(F)F)c5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
CHEMBL4095843 159034 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP productionAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP production
ChEMBL 572 8 1 9 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5cccc(C(F)(F)F)c5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
66892867 156410 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 479 7 1 8 2.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(F)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4065629 156410 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 479 7 1 8 2.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(F)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
57429649 159034 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 572 8 1 9 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5cccc(C(F)(F)F)c5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4095843 159034 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 572 8 1 9 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5cccc(C(F)(F)F)c5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
11690712 77821 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 439 7 3 6 2.0 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)NCc4ccccc4)cc3)nc2c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL209230 77821 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 439 7 3 6 2.0 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)NCc4ccccc4)cc3)nc2c1=O 10.1016/j.ejmech.2010.04.039
52946453 19230 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 521 9 2 5 5.6 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NC1(c2ccccc2)CC1 10.1016/j.bmcl.2010.10.030
CHEMBL1290001 19230 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 521 9 2 5 5.6 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NC1(c2ccccc2)CC1 10.1016/j.bmcl.2010.10.030
44404010 72602 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 480 9 2 8 2.9 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(F)cc4)nc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
CHEMBL199249 72602 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 480 9 2 8 2.9 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(F)cc4)nc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
135528632 72588 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 329 5 2 7 1.5 CCCn1c(=O)c2nc(-c3ccc(O)nc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
CHEMBL199196 72588 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 329 5 2 7 1.5 CCCn1c(=O)c2nc(-c3ccc(O)nc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
9870719 57434 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 503 10 2 8 3.6 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4cccc(C(C)=O)c4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16534 57434 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 503 10 2 8 3.6 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4cccc(C(C)=O)c4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
126079 4100 None 29 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 10.1021/jm990421v
451 4100 None 29 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 10.1021/jm990421v
CHEMBL27041 4100 None 29 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 10.1021/jm990421v
52950027 19150 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 478 9 2 4 5.3 O=C(COc1ccc2[nH]c(=O)c(-c3ccco3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289461 19150 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 478 9 2 4 5.3 O=C(COc1ccc2[nH]c(=O)c(-c3ccco3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
52950000 19133 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 505 8 2 4 5.2 N#Cc1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
CHEMBL1289344 19133 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 505 8 2 4 5.2 N#Cc1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
52948915 19302 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 541 9 2 5 6.0 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccc(F)cc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290437 19302 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 541 9 2 5 6.0 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccc(F)cc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
44572409 189800 None 0 Human Functional pKi = 5.4 5.4 - 0
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 267 1 1 5 1.9 Nc1ncnc2c1nc(Br)n2C1CCC1 10.1016/j.bmc.2009.02.030
CHEMBL515419 189800 None 0 Human Functional pKi = 5.4 5.4 - 0
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 267 1 1 5 1.9 Nc1ncnc2c1nc(Br)n2C1CCC1 10.1016/j.bmc.2009.02.030
123807 871 None 35 Human Functional pKi = 7.4 7.4 -12022 7
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1016/j.bmc.2007.09.035
374 871 None 35 Human Functional pKi = 7.4 7.4 -12022 7
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1016/j.bmc.2007.09.035
379 871 None 35 Human Functional pKi = 7.4 7.4 -12022 7
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1016/j.bmc.2007.09.035
CHEMBL284969 871 None 35 Human Functional pKi = 7.4 7.4 -12022 7
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1016/j.bmc.2007.09.035
176407 4148 None 56 Human Functional pKi = 7.4 7.4 -13 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation countingAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation counting
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm900718w
405 4148 None 56 Human Functional pKi = 7.4 7.4 -13 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation countingAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation counting
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm900718w
CHEMBL113142 4148 None 56 Human Functional pKi = 7.4 7.4 -13 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation countingAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation counting
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm900718w
DB08770 4148 None 56 Human Functional pKi = 7.4 7.4 -13 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation countingAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation counting
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm900718w
44572355 179690 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 269 2 1 5 1.8 CC(C)Cn1c(Br)nc2c(N)ncnc21 10.1016/j.ejmech.2010.04.039
CHEMBL474207 179690 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 269 2 1 5 1.8 CC(C)Cn1c(Br)nc2c(N)ncnc21 10.1016/j.ejmech.2010.04.039
44572355 179690 None 0 Human Functional pKi = 5.4 5.4 - 0
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 269 2 1 5 1.8 CC(C)Cn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL474207 179690 None 0 Human Functional pKi = 5.4 5.4 - 0
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 269 2 1 5 1.8 CC(C)Cn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
380 1287 None 37 Human Functional pKi = 7.4 7.4 - 5
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1016/j.bmc.2007.09.035
657378 1287 None 37 Human Functional pKi = 7.4 7.4 - 5
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1016/j.bmc.2007.09.035
CHEMBL68738 1287 None 37 Human Functional pKi = 7.4 7.4 - 5
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1016/j.bmc.2007.09.035
9915751 59146 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 557 14 1 11 1.7 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(CC(=O)OCC)CC(=O)OCC)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16984 59146 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 557 14 1 11 1.7 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(CC(=O)OCC)CC(=O)OCC)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
44447542 154880 None 0 Human Functional pKi = 5.4 5.4 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 351 4 4 10 -1.0 C[C@@]1(O)[C@H](O)[C@@H](CO)O[C@H]1n1cnc2c(N[C@@H]3CCOC3)ncnc21 10.1016/j.bmc.2007.09.035
CHEMBL400190 154880 None 0 Human Functional pKi = 5.4 5.4 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 351 4 4 10 -1.0 C[C@@]1(O)[C@H](O)[C@@H](CO)O[C@H]1n1cnc2c(N[C@@H]3CCOC3)ncnc21 10.1016/j.bmc.2007.09.035
44447548 154976 None 0 Human Functional pKi = 5.4 5.4 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 385 4 4 10 -0.3 C[C@@]1(O)[C@H](O)[C@@H](CO)O[C@H]1n1cnc2c(N[C@@H]3CCOC3)nc(Cl)nc21 10.1016/j.bmc.2007.09.035
CHEMBL400782 154976 None 0 Human Functional pKi = 5.4 5.4 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 385 4 4 10 -0.3 C[C@@]1(O)[C@H](O)[C@@H](CO)O[C@H]1n1cnc2c(N[C@@H]3CCOC3)nc(Cl)nc21 10.1016/j.bmc.2007.09.035
44572408 188968 None 0 Human Functional pKi = 5.3 5.3 - 0
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 253 2 1 5 1.4 C=CCn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL506888 188968 None 0 Human Functional pKi = 5.3 5.3 - 0
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 253 2 1 5 1.4 C=CCn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
127042409 136861 None 0 Human Functional pKi = 5.3 5.3 - 0
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 348 6 2 7 3.7 CCCn1c(-c2ccco2)nc2c(N)nc(NCc3ccccc3)nc21 10.1039/C5MD00034C
CHEMBL3741217 136861 None 0 Human Functional pKi = 5.3 5.3 - 0
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 348 6 2 7 3.7 CCCn1c(-c2ccco2)nc2c(N)nc(NCc3ccccc3)nc21 10.1039/C5MD00034C
118707860 113301 None 0 Human Functional pKi = 5.3 5.3 - 0
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 341 5 1 8 2.9 CCOC(=O)c1cnc(NC2CCCC2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314893 113301 None 0 Human Functional pKi = 5.3 5.3 - 0
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 341 5 1 8 2.9 CCOC(=O)c1cnc(NC2CCCC2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
9912946 59019 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 478 7 2 6 3.7 O=C(O)/C=C/c1ccc(-c2nc3c(=O)n(Cc4ccccc4)c(=O)n(Cc4ccccc4)c3[nH]2)cc1 10.1021/jm990421v
CHEMBL16908 59019 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 478 7 2 6 3.7 O=C(O)/C=C/c1ccc(-c2nc3c(=O)n(Cc4ccccc4)c(=O)n(Cc4ccccc4)c3[nH]2)cc1 10.1021/jm990421v
76335305 103764 None 0 Human Functional pKi = 6.3 6.3 - 0
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 3 2 7 0.7 Nc1ncnc2c1nc(-c1ccco1)n2CCO 10.1016/j.ejmech.2013.10.006
CHEMBL3087717 103764 None 0 Human Functional pKi = 6.3 6.3 - 0
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 3 2 7 0.7 Nc1ncnc2c1nc(-c1ccco1)n2CCO 10.1016/j.ejmech.2013.10.006
10387088 59474 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 414 10 2 7 2.6 CCCCn1c(=O)c2nc(-c3ccc(OCC(=O)O)cc3)[nH]c2n(CCCC)c1=O 10.1021/jm990421v
CHEMBL17123 59474 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 414 10 2 7 2.6 CCCCn1c(=O)c2nc(-c3ccc(OCC(=O)O)cc3)[nH]c2n(CCCC)c1=O 10.1021/jm990421v
71455621 82978 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 311 4 1 8 2.5 CC[C@@H](C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181152 82978 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 311 4 1 8 2.5 CC[C@@H](C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
118707864 113305 None 0 Human Functional pKi = 5.3 5.3 - 0
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 393 7 1 9 3.2 CCOC(=O)c1cnc(NCc2ccc(OC)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314897 113305 None 0 Human Functional pKi = 5.3 5.3 - 0
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 393 7 1 9 3.2 CCOC(=O)c1cnc(NCc2ccc(OC)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
44582613 181744 None 0 Human Functional pKi = 5.3 5.3 - 0
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 387 4 3 8 1.7 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@@H]1O 10.1021/jm801456g
CHEMBL477445 181744 None 0 Human Functional pKi = 5.3 5.3 - 0
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 387 4 3 8 1.7 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@@H]1O 10.1021/jm801456g
118707847 113287 None 0 Human Functional pKi = 5.3 5.3 - 0
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 376 5 2 7 1.9 CNC(=O)c1cnc(NC(=O)Cc2ccccc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314879 113287 None 0 Human Functional pKi = 5.3 5.3 - 0
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 376 5 2 7 1.9 CNC(=O)c1cnc(NC(=O)Cc2ccccc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
21958762 155870 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 288 4 2 6 0.7 CCCn1c(=O)c2[nH]c(-c3cn[nH]c3)nc2n(CC)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL405901 155870 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 288 4 2 6 0.7 CCCn1c(=O)c2[nH]c(-c3cn[nH]c3)nc2n(CC)c1=O 10.1016/j.ejmech.2010.04.039
10021483 186989 None 0 Human Functional pKi = 5.3 5.3 - 0
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 361 4 4 9 0.0 OC[C@H]1O[C@@H](n2cnc3c(NC4CC5CCC4C5)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm801456g
CHEMBL489640 186989 None 0 Human Functional pKi = 5.3 5.3 - 0
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 361 4 4 9 0.0 OC[C@H]1O[C@@H](n2cnc3c(NC4CC5CCC4C5)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm801456g
50925499 19243 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 523 9 2 5 5.9 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290101 19243 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 523 9 2 5 5.9 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
10648228 98488 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 475 9 1 7 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(C)c4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL275606 98488 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 475 9 1 7 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(C)c4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
135484064 2616 None 3 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm049418o
390 2616 None 3 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm049418o
CHEMBL260331 2616 None 3 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm049418o
135484064 2616 None 3 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2010.04.039
390 2616 None 3 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2010.04.039
CHEMBL260331 2616 None 3 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2010.04.039
52942359 19201 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 517 9 2 4 5.8 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3ccccn3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289778 19201 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 517 9 2 4 5.8 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3ccccn3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
76313600 103758 None 0 Human Functional pKi = 5.3 5.3 - 0
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 439 7 1 7 4.4 Cn1c(-c2ccco2)nc2c(NC(=O)Cc3ccc(OCc4ccccc4)cc3)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL3087711 103758 None 0 Human Functional pKi = 5.3 5.3 - 0
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 439 7 1 7 4.4 Cn1c(-c2ccco2)nc2c(NC(=O)Cc3ccc(OCc4ccccc4)cc3)ncnc21 10.1016/j.ejmech.2013.10.006
44572471 180713 None 0 Human Functional pKi = 5.3 5.3 - 0
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 271 3 2 6 0.6 Nc1ncnc2c1nc(Br)n2CCCO 10.1016/j.bmc.2009.02.030
44572471 180713 None 0 Human Functional pKi = 5.3 5.3 - 0
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 271 3 2 6 0.6 Nc1ncnc2c1nc(Br)n2CCCO 10.1016/j.ejmech.2013.10.006
CHEMBL475455 180713 None 0 Human Functional pKi = 5.3 5.3 - 0
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 271 3 2 6 0.6 Nc1ncnc2c1nc(Br)n2CCCO 10.1016/j.bmc.2009.02.030
CHEMBL475455 180713 None 0 Human Functional pKi = 5.3 5.3 - 0
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 271 3 2 6 0.6 Nc1ncnc2c1nc(Br)n2CCCO 10.1016/j.ejmech.2013.10.006
52942501 19279 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 515 8 2 5 5.6 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCC(F)(F)F)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290324 19279 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 515 8 2 5 5.6 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCC(F)(F)F)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
71455620 82965 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 387 6 1 8 3.7 CC(CCc1ccccc1)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181140 82965 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 387 6 1 8 3.7 CC(CCc1ccccc1)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
71452056 82954 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATPAntagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATP
ChEMBL 359 4 1 8 3.4 C[C@H](Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12)c1ccccc1 10.1039/d0md00380h
CHEMBL2180931 82954 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATPAntagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATP
ChEMBL 359 4 1 8 3.4 C[C@H](Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12)c1ccccc1 10.1039/d0md00380h
71452056 82954 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 359 4 1 8 3.4 C[C@H](Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12)c1ccccc1 10.1021/jm300899q
CHEMBL2180931 82954 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 359 4 1 8 3.4 C[C@H](Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12)c1ccccc1 10.1021/jm300899q
11602451 162347 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 335 5 1 5 4.6 CCCn1c(-c2ccccc2)nc2c(NC3CCCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4163601 162347 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 335 5 1 5 4.6 CCCn1c(-c2ccccc2)nc2c(NC3CCCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
118707844 113166 None 0 Human Functional pKi = 5.3 5.3 - 0
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 348 5 2 7 1.9 Nc1ncc(C(=O)NCCc2ccccc2)c2nc(-c3ccco3)nn12 10.1021/jm500752h
CHEMBL3313941 113166 None 0 Human Functional pKi = 5.3 5.3 - 0
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 348 5 2 7 1.9 Nc1ncc(C(=O)NCCc2ccccc2)c2nc(-c3ccco3)nn12 10.1021/jm500752h
136414902 159808 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 560 9 1 9 3.8 CCCn1c(=O)c2[nH]c(-c3cc(OCC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)no3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4104450 159808 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 560 9 1 9 3.8 CCCn1c(=O)c2[nH]c(-c3cc(OCC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)no3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
1329 1472 None 53 Human Functional pKi = 7.3 7.3 -9 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.ejmech.2010.04.039
386 1472 None 53 Human Functional pKi = 7.3 7.3 -9 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.ejmech.2010.04.039
CHEMBL183 1472 None 53 Human Functional pKi = 7.3 7.3 -9 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.ejmech.2010.04.039
DB12946 1472 None 53 Human Functional pKi = 7.3 7.3 -9 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.ejmech.2010.04.039
52933926 156273 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as reduction in NECA-induced increase in cAMP level preincubated for 15 mins followed by NECA addition measured after 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as reduction in NECA-induced increase in cAMP level preincubated for 15 mins followed by NECA addition measured after 15 mins by HTRF assay
ChEMBL 353 5 1 6 3.7 CCCn1c(Oc2cccnc2C)nc2nc(C3CCCC3)[nH]c2c1=O 10.1016/j.bmc.2017.02.029
CHEMBL4063997 156273 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as reduction in NECA-induced increase in cAMP level preincubated for 15 mins followed by NECA addition measured after 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as reduction in NECA-induced increase in cAMP level preincubated for 15 mins followed by NECA addition measured after 15 mins by HTRF assay
ChEMBL 353 5 1 6 3.7 CCCn1c(Oc2cccnc2C)nc2nc(C3CCCC3)[nH]c2c1=O 10.1016/j.bmc.2017.02.029
11608719 188850 None 22 Human Functional pKi = 5.3 5.3 - 0
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 269 3 1 5 2.0 CCCCn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL505089 188850 None 22 Human Functional pKi = 5.3 5.3 - 0
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 269 3 1 5 2.0 CCCCn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
11623708 162598 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 307 4 1 5 3.9 CCn1c(-c2ccccc2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4167491 162598 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 307 4 1 5 3.9 CCn1c(-c2ccccc2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
11774068 94617 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 404 4 2 6 2.4 CCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL251876 94617 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 404 4 2 6 2.4 CCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.ejmech.2010.04.039
10158974 155596 None 0 Human Functional pKi = 8.2 8.2 - 0
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 418 5 2 6 2.8 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.05.035
CHEMBL404168 155596 None 0 Human Functional pKi = 8.2 8.2 - 0
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 418 5 2 6 2.8 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.05.035
CHEMBL5076192 216907 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCCn1c(=O)c2nc(C34CCC(C(=O)NCCCCCCCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
443 755 None 9 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 382 7 2 6 2.5 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)/C=C/C(=O)O 10.1021/jm990421v
6439089 755 None 9 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 382 7 2 6 2.5 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)/C=C/C(=O)O 10.1021/jm990421v
CHEMBL16997 755 None 9 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 382 7 2 6 2.5 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)/C=C/C(=O)O 10.1021/jm990421v
52941244 19258 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 509 9 2 5 5.7 C[C@@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290209 19258 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 509 9 2 5 5.7 C[C@@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
118732285 118429 None 0 Human Functional pKi = 4.2 4.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 311 5 1 7 1.8 CCOC(=O)c1nc(N)nc2nn(CCc3ccccc3)cc12 10.1016/j.ejmech.2015.01.046
CHEMBL3410301 118429 None 0 Human Functional pKi = 4.2 4.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 311 5 1 7 1.8 CCOC(=O)c1nc(N)nc2nn(CCc3ccccc3)cc12 10.1016/j.ejmech.2015.01.046
11681092 162806 None 0 Human Functional pKi = 5.2 5.2 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 307 3 1 5 3.7 Cc1cccc(-c2nc3c(NC4CCCC4)ncnc3n2C)c1 10.1016/j.ejmech.2018.03.067
CHEMBL4170850 162806 None 0 Human Functional pKi = 5.2 5.2 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 307 3 1 5 3.7 Cc1cccc(-c2nc3c(NC4CCCC4)ncnc3n2C)c1 10.1016/j.ejmech.2018.03.067
145991283 166942 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 364 6 2 9 3.0 CCOC(=O)c1cnc(NNc2ccccc2)n2nc(-c3ccco3)nc12 10.1016/j.ejmech.2018.08.042
CHEMBL4285374 166942 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 364 6 2 9 3.0 CCOC(=O)c1cnc(NNc2ccccc2)n2nc(-c3ccco3)nc12 10.1016/j.ejmech.2018.08.042
52944930 19301 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 495 9 2 5 5.1 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290436 19301 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 495 9 2 5 5.1 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
76324475 103760 None 0 Human Functional pKi = 5.2 5.2 - 0
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 334 3 2 6 3.3 Cn1c(-c2ccco2)nc2c(NC(=O)Nc3ccccc3)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL3087713 103760 None 0 Human Functional pKi = 5.2 5.2 - 0
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 334 3 2 6 3.3 Cn1c(-c2ccco2)nc2c(NC(=O)Nc3ccccc3)ncnc21 10.1016/j.ejmech.2013.10.006
18440528 136719 None 0 Human Functional pKi = 5.2 5.2 - 0
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 388 7 2 6 3.6 CCCn1c(Br)nc2c(N)nc(NCCCc3ccccc3)nc21 10.1039/C5MD00034C
CHEMBL3739922 136719 None 0 Human Functional pKi = 5.2 5.2 - 0
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 388 7 2 6 3.6 CCCn1c(Br)nc2c(N)nc(NCCCc3ccccc3)nc21 10.1039/C5MD00034C
71453894 82987 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 337 3 1 8 3.0 Cn1cc2c(nc(NC3CCCCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181161 82987 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 337 3 1 8 3.0 Cn1cc2c(nc(NC3CCCCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
52948671 19320 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 520 11 1 5 4.8 COCCCNC(=O)COc1ccc2c(c1)c(CCc1ccccc1)c(-c1ccc(F)cc1F)c(=O)n2C 10.1016/j.bmcl.2010.10.030
CHEMBL1290544 19320 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 520 11 1 5 4.8 COCCCNC(=O)COc1ccc2c(c1)c(CCc1ccccc1)c(-c1ccc(F)cc1F)c(=O)n2C 10.1016/j.bmcl.2010.10.030
44572473 180869 None 0 Human Functional pKi = 6.2 6.2 - 0
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 271 2 2 6 0.6 CC(O)Cn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL475617 180869 None 0 Human Functional pKi = 6.2 6.2 - 0
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 271 2 2 6 0.6 CC(O)Cn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
132941757 158991 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 460 7 1 7 4.4 CCN(CC)C1CCC(C)(C(=O)Nc2nc3c(OC)ccc(N4CCOCC4)c3s2)CC1 10.1021/acs.jmedchem.6b01584
CHEMBL4095355 158991 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 460 7 1 7 4.4 CCN(CC)C1CCC(C)(C(=O)Nc2nc3c(OC)ccc(N4CCOCC4)c3s2)CC1 10.1021/acs.jmedchem.6b01584
137631671 156424 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as reduction in NECA-induced increase in cAMP level preincubated for 15 mins followed by NECA addition measured after 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as reduction in NECA-induced increase in cAMP level preincubated for 15 mins followed by NECA addition measured after 15 mins by HTRF assay
ChEMBL 352 5 1 5 3.9 CCCn1c(-c2cccc(OC)c2)nc2nc(C3CCCC3)[nH]c2c1=O 10.1016/j.bmc.2017.02.029
CHEMBL4065762 156424 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as reduction in NECA-induced increase in cAMP level preincubated for 15 mins followed by NECA addition measured after 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as reduction in NECA-induced increase in cAMP level preincubated for 15 mins followed by NECA addition measured after 15 mins by HTRF assay
ChEMBL 352 5 1 5 3.9 CCCn1c(-c2cccc(OC)c2)nc2nc(C3CCCC3)[nH]c2c1=O 10.1016/j.bmc.2017.02.029
71450242 82988 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 351 3 1 8 3.4 Cn1cc2c(nc(NC3CCCCCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181162 82988 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 351 3 1 8 3.4 Cn1cc2c(nc(NC3CCCCCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
52950000 19133 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 505 8 2 4 5.2 N#Cc1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
CHEMBL1289344 19133 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 505 8 2 4 5.2 N#Cc1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
52949755 19245 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 468 6 2 5 3.2 Cc1c(S(C)(=O)=O)c(=O)[nH]c2ccc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)cc12 10.1016/j.bmcl.2010.10.030
CHEMBL1290103 19245 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 468 6 2 5 3.2 Cc1c(S(C)(=O)=O)c(=O)[nH]c2ccc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)cc12 10.1016/j.bmcl.2010.10.030
52948949 19277 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 494 8 3 4 5.4 O=C(NCc1ccccc1)NCc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
CHEMBL1290322 19277 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 494 8 3 4 5.4 O=C(NCc1ccccc1)NCc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
10226014 94644 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 452 6 2 9 2.4 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)[nH]c2c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL252048 94644 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 452 6 2 9 2.4 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)[nH]c2c1=O 10.1016/j.ejmech.2010.04.039
52950040 19167 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 523 10 2 5 6.1 CC[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289569 19167 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 523 10 2 5 6.1 CC[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
404 4098 None 26 Human Functional pKi = 8.1 8.1 1318 2
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1021/jm990421v
432 4098 None 26 Human Functional pKi = 8.1 8.1 1318 2
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1021/jm990421v
5697 4098 None 26 Human Functional pKi = 8.1 8.1 1318 2
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1021/jm990421v
CHEMBL273094 4098 None 26 Human Functional pKi = 8.1 8.1 1318 2
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1021/jm990421v
9827467 98440 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 504 10 3 8 2.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(N)=O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL275360 98440 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 504 10 3 8 2.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(N)=O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
135921140 11347 None 0 Mouse Functional pKi = 5.2 5.2 - 0
Inhibition against A2B-Adenosine Receptor in mouse NIH 3T3 fibroblast cell membranes (functional antagonist activity)Inhibition against A2B-Adenosine Receptor in mouse NIH 3T3 fibroblast cell membranes (functional antagonist activity)
ChEMBL 267 1 1 4 1.7 Cn1c(-c2ccccc2)nc2c1C1=NCCN1C(=O)N2 10.1021/jm011093d
CHEMBL117962 11347 None 0 Mouse Functional pKi = 5.2 5.2 - 0
Inhibition against A2B-Adenosine Receptor in mouse NIH 3T3 fibroblast cell membranes (functional antagonist activity)Inhibition against A2B-Adenosine Receptor in mouse NIH 3T3 fibroblast cell membranes (functional antagonist activity)
ChEMBL 267 1 1 4 1.7 Cn1c(-c2ccccc2)nc2c1C1=NCCN1C(=O)N2 10.1021/jm011093d
52946114 19280 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 525 9 2 6 5.7 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(COc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290325 19280 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 525 9 2 6 5.7 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(COc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
69029783 156418 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 570 9 1 8 4.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)nc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4065717 156418 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 570 9 1 8 4.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)nc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
2773172 188885 None 5 Human Functional pKi = 5.2 5.2 - 0
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 287 3 3 7 -0.5 Nc1ncnc2c1nc(Br)n2CC(O)CO 10.1016/j.bmc.2009.02.030
CHEMBL505633 188885 None 5 Human Functional pKi = 5.2 5.2 - 0
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 287 3 3 7 -0.5 Nc1ncnc2c1nc(Br)n2CC(O)CO 10.1016/j.bmc.2009.02.030
118707879 113320 None 0 Human Functional pKi = 5.2 5.2 - 0
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 329 6 1 8 2.6 CCOC(=O)c1cnc(NCC(C)C)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314913 113320 None 0 Human Functional pKi = 5.2 5.2 - 0
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 329 6 1 8 2.6 CCOC(=O)c1cnc(NCC(C)C)n2nc(-c3ccco3)nc12 10.1021/jm500752h
822296 189222 None 14 Human Functional pKi = 6.1 6.1 - 0
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 227 0 1 5 0.7 Cn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
822296 189222 None 14 Human Functional pKi = 6.1 6.1 - 0
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 227 0 1 5 0.7 Cn1c(Br)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL510288 189222 None 14 Human Functional pKi = 6.1 6.1 - 0
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 227 0 1 5 0.7 Cn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL510288 189222 None 14 Human Functional pKi = 6.1 6.1 - 0
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 227 0 1 5 0.7 Cn1c(Br)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
71457403 82967 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 299 4 2 9 0.7 Cn1cc2c(nc(NCCO)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181142 82967 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 299 4 2 9 0.7 Cn1cc2c(nc(NCCO)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
127040410 136857 None 0 Human Functional pKi = 5.1 5.1 - 0
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 345 5 1 5 3.6 CCCn1c(Br)nc2c(NCc3ccccc3)ncnc21 10.1039/C5MD00034C
CHEMBL3741167 136857 None 0 Human Functional pKi = 5.1 5.1 - 0
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 345 5 1 5 3.6 CCCn1c(Br)nc2c(NCc3ccccc3)ncnc21 10.1039/C5MD00034C
71455601 82941 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 375 6 1 9 2.8 Cn1cc2c(nc(NCCOc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2180918 82941 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 375 6 1 9 2.8 Cn1cc2c(nc(NCCOc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
71452072 82980 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 353 7 1 8 3.7 CCCCCC(C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181154 82980 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 353 7 1 8 3.7 CCCCCC(C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
11565780 162374 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 307 5 1 5 3.9 CCCn1c(-c2ccccc2)nc2c(NC3CCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4164048 162374 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 307 5 1 5 3.9 CCCn1c(-c2ccccc2)nc2c(NC3CCC3)ncnc21 10.1016/j.ejmech.2018.03.067
308531 165816 None 6 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 225 1 1 5 1.6 Cn1c(-c2ccccc2)nc2c(N)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL424597 165816 None 6 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 225 1 1 5 1.6 Cn1c(-c2ccccc2)nc2c(N)ncnc21 10.1016/j.ejmech.2018.03.067
76324476 103763 None 0 Human Functional pKi = 6.1 6.1 - 0
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 215 1 1 6 1.2 Cn1c(-c2ccco2)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL3087716 103763 None 0 Human Functional pKi = 6.1 6.1 - 0
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 215 1 1 6 1.2 Cn1c(-c2ccco2)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL5073669 216789 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCCn1c(=O)c2nc(C34CCC(C(=O)NCCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
76309882 103757 None 0 Human Functional pKi = 6.1 6.1 - 0
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 409 5 1 6 4.4 Cn1c(-c2ccco2)nc2c(NC(=O)C(c3ccccc3)c3ccccc3)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL3087710 103757 None 0 Human Functional pKi = 6.1 6.1 - 0
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 409 5 1 6 4.4 Cn1c(-c2ccco2)nc2c(NC(=O)C(c3ccccc3)c3ccccc3)ncnc21 10.1016/j.ejmech.2013.10.006
44236568 156561 None 0 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 486 6 1 8 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4067401 156561 None 0 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 486 6 1 8 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
69031481 157169 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP productionAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP production
ChEMBL 529 7 1 8 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2021.113907
CHEMBL4074253 157169 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP productionAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP production
ChEMBL 529 7 1 8 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2021.113907
57429602 157331 None 0 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP productionAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP production
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
CHEMBL4076435 157331 None 0 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP productionAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP production
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
69031481 157169 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 529 7 1 8 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4074253 157169 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 529 7 1 8 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
57429602 157331 None 0 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4076435 157331 None 0 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
72197883 90835 None 0 Human Functional pKi = 5.1 5.1 - 0
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 407 5 2 9 3.2 CN(C)c1nc(N)nc(-c2sc(NC(=O)c3ccco3)nc2-c2ccccc2)n1 10.1016/j.ejmech.2013.03.020
CHEMBL2391837 90835 None 0 Human Functional pKi = 5.1 5.1 - 0
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 407 5 2 9 3.2 CN(C)c1nc(N)nc(-c2sc(NC(=O)c3ccco3)nc2-c2ccccc2)n1 10.1016/j.ejmech.2013.03.020
52946114 19280 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 525 9 2 6 5.7 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(COc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290325 19280 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 525 9 2 6 5.7 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(COc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
439176 98674 None 50 Human Functional pKi = 5.1 5.1 - 2
Binding affinity towards human adenosine A2B receptor in VA13 fibroblasts as inhibition of adenylate cyclase at 10 uM; Less than 10% inhibitionBinding affinity towards human adenosine A2B receptor in VA13 fibroblasts as inhibition of adenylate cyclase at 10 uM; Less than 10% inhibition
ChEMBL 297 3 3 9 -0.6 CSC[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm031092g
CHEMBL277041 98674 None 50 Human Functional pKi = 5.1 5.1 - 2
Binding affinity towards human adenosine A2B receptor in VA13 fibroblasts as inhibition of adenylate cyclase at 10 uM; Less than 10% inhibitionBinding affinity towards human adenosine A2B receptor in VA13 fibroblasts as inhibition of adenylate cyclase at 10 uM; Less than 10% inhibition
ChEMBL 297 3 3 9 -0.6 CSC[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm031092g
127040064 136838 None 0 Human Functional pKi = 5.1 5.1 - 0
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 376 8 2 7 4.1 CCCn1c(-c2ccco2)nc2c(N)nc(NCCCc3ccccc3)nc21 10.1039/C5MD00034C
CHEMBL3740992 136838 None 0 Human Functional pKi = 5.1 5.1 - 0
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 376 8 2 7 4.1 CCCn1c(-c2ccco2)nc2c(N)nc(NCCCc3ccccc3)nc21 10.1039/C5MD00034C
44447519 94939 None 0 Human Functional pKi = 5.1 5.1 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 440 5 4 10 1.2 CNC(=O)OC[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@](C)(O)[C@@H]1O 10.1016/j.bmc.2007.09.035
CHEMBL254064 94939 None 0 Human Functional pKi = 5.1 5.1 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 440 5 4 10 1.2 CNC(=O)OC[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@](C)(O)[C@@H]1O 10.1016/j.bmc.2007.09.035
25188209 178864 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 311 3 1 8 1.6 Nc1nc(-c2ncco2)c2nnn(Cc3ccccc3F)c2n1 10.1016/j.ejmech.2010.04.039
CHEMBL468701 178864 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 311 3 1 8 1.6 Nc1nc(-c2ncco2)c2nnn(Cc3ccccc3F)c2n1 10.1016/j.ejmech.2010.04.039
5248753 178858 None 3 Human Functional pKi = 6.1 6.1 - 0
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 241 1 1 5 1.2 CCn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
5248753 178858 None 3 Human Functional pKi = 6.1 6.1 - 0
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 241 1 1 5 1.2 CCn1c(Br)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL468633 178858 None 3 Human Functional pKi = 6.1 6.1 - 0
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 241 1 1 5 1.2 CCn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL468633 178858 None 3 Human Functional pKi = 6.1 6.1 - 0
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 241 1 1 5 1.2 CCn1c(Br)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
72197703 90831 None 0 Human Functional pKi = 6.1 6.1 - 0
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 347 4 1 5 4.7 O=C(Nc1nc(-c2ccccc2)c(-c2ccccn2)s1)c1ccco1 10.1016/j.ejmech.2013.03.020
CHEMBL2391833 90831 None 0 Human Functional pKi = 6.1 6.1 - 0
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 347 4 1 5 4.7 O=C(Nc1nc(-c2ccccc2)c(-c2ccccn2)s1)c1ccco1 10.1016/j.ejmech.2013.03.020
71457389 82939 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 285 3 1 9 1.2 CONc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2180916 82939 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 285 3 1 9 1.2 CONc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
11587409 163091 None 0 Human Functional pKi = 5.1 5.1 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 293 3 1 5 3.4 Cn1c(-c2ccccc2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4175366 163091 None 0 Human Functional pKi = 5.1 5.1 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 293 3 1 5 3.4 Cn1c(-c2ccccc2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
12016633 172773 None 0 Human Functional pKi = 6.1 6.1 - 0
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 281 1 1 5 2.3 Nc1ncnc2c1nc(Br)n2C1CCCC1 10.1016/j.bmc.2009.02.030
CHEMBL449924 172773 None 0 Human Functional pKi = 6.1 6.1 - 0
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 281 1 1 5 2.3 Nc1ncnc2c1nc(Br)n2C1CCCC1 10.1016/j.bmc.2009.02.030
9946338 154879 None 29 Human Functional pKi = 6.1 6.1 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 349 4 4 9 0.2 C[C@@]1(O)[C@H](O)[C@@H](CO)O[C@H]1n1cnc2c(NC3CCCC3)ncnc21 10.1016/j.bmc.2007.09.035
CHEMBL400189 154879 None 29 Human Functional pKi = 6.1 6.1 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 349 4 4 9 0.2 C[C@@]1(O)[C@H](O)[C@@H](CO)O[C@H]1n1cnc2c(NC3CCCC3)ncnc21 10.1016/j.bmc.2007.09.035
52941201 19231 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 517 9 2 4 5.8 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3ccncc3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290002 19231 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 517 9 2 4 5.8 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3ccncc3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
10267860 176928 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 317 3 1 8 2.0 N#Cc1ccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)cc1 10.1016/j.ejmech.2010.04.039
CHEMBL461007 176928 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 317 3 1 8 2.0 N#Cc1ccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)cc1 10.1016/j.ejmech.2010.04.039
11198201 110740 None 4 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 327 5 2 6 2.0 CCCn1c(=O)c2nc(-c3ccc(N)cc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
CHEMBL32598 110740 None 4 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 327 5 2 6 2.0 CCCn1c(=O)c2nc(-c3ccc(N)cc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
14484978 97645 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 483 9 1 10 1.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)ON4C(=O)CCC4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL27081 97645 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 483 9 1 10 1.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)ON4C(=O)CCC4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
9850900 98404 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 565 12 1 7 5.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(Cc4ccccc4)Cc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL275149 98404 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 565 12 1 7 5.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(Cc4ccccc4)Cc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
9850900 98404 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 565 12 1 7 5.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(Cc4ccccc4)Cc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL275149 98404 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 565 12 1 7 5.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(Cc4ccccc4)Cc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.ejmech.2010.04.039
11508049 162076 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 321 4 1 5 4.3 CCn1c(-c2ccccc2)nc2c(NC3CCCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4159165 162076 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 321 4 1 5 4.3 CCn1c(-c2ccccc2)nc2c(NC3CCCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
2153 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm049418o
2153.0 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm049418o
2620 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm049418o
413 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm049418o
CHEMBL190 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm049418o
DB00277 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm049418o
2153 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2010.04.039
2153.0 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2010.04.039
2620 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2010.04.039
413 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2010.04.039
CHEMBL190 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2010.04.039
DB00277 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2010.04.039
2153 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
2153.0 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
2620 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
413 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
CHEMBL190 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
DB00277 3800 None 72 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
11681354 163031 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 323 5 1 6 3.1 CCCn1c(-c2ccccc2)nc2c(NC3CCOC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4174308 163031 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 323 5 1 6 3.1 CCCn1c(-c2ccccc2)nc2c(NC3CCOC3)ncnc21 10.1016/j.ejmech.2018.03.067
72197701 90829 None 0 Human Functional pKi = 5.0 5.0 - 0
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 375 5 1 6 4.3 O=C(Nc1nc(-c2ccccc2)c(C(=O)c2ccccn2)s1)c1ccco1 10.1016/j.ejmech.2013.03.020
CHEMBL2391831 90829 None 0 Human Functional pKi = 5.0 5.0 - 0
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 375 5 1 6 4.3 O=C(Nc1nc(-c2ccccc2)c(C(=O)c2ccccn2)s1)c1ccco1 10.1016/j.ejmech.2013.03.020
18440431 136731 None 0 Human Functional pKi = 5.0 5.0 - 0
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 296 6 2 6 2.5 CCCn1cnc2c(N)nc(NCCc3ccccc3)nc21 10.1039/C5MD00034C
CHEMBL3739985 136731 None 0 Human Functional pKi = 5.0 5.0 - 0
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 296 6 2 6 2.5 CCCn1cnc2c(N)nc(NCCc3ccccc3)nc21 10.1039/C5MD00034C
127042994 136875 None 0 Human Functional pKi = 5.0 5.0 - 0
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 347 7 1 6 4.2 CCCn1c(-c2ccco2)nc2c(NCCc3ccccc3)ncnc21 10.1039/C5MD00034C
CHEMBL3741337 136875 None 0 Human Functional pKi = 5.0 5.0 - 0
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 347 7 1 6 4.2 CCCn1c(-c2ccco2)nc2c(NCCc3ccccc3)ncnc21 10.1039/C5MD00034C
71453891 82968 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 313 5 2 9 1.1 Cn1cc2c(nc(NCCCO)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181143 82968 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 313 5 2 9 1.1 Cn1cc2c(nc(NCCCO)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL5088372 217645 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCCn1c(=O)c2nc(C34CCC(C(=O)NCCOCCOCCOCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
71462775 82990 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 351 4 1 8 3.3 Cn1cc2c(nc(NCC3CCCCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181164 82990 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 351 4 1 8 3.3 Cn1cc2c(nc(NCC3CCCCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
71457404 82974 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 297 3 1 8 2.1 CC(C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181149 82974 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 297 3 1 8 2.1 CC(C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
71455604 82957 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 375 5 1 9 2.9 COc1ccc(CNc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm300899q
CHEMBL2180934 82957 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 375 5 1 9 2.9 COc1ccc(CNc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm300899q
162657141 181029 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATPAntagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATP
ChEMBL 371 6 2 11 0.6 CCOC(=O)C(CO)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1039/d0md00380h
CHEMBL4757966 181029 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATPAntagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATP
ChEMBL 371 6 2 11 0.6 CCOC(=O)C(CO)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1039/d0md00380h
2690 903 None 44 Human Functional pA2 = 7.8 7.8 -31 5
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 8937736
384 903 None 44 Human Functional pA2 = 7.8 7.8 -31 5
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 8937736
CHEMBL16687 903 None 44 Human Functional pA2 = 7.8 7.8 -31 5
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 8937736
404 4098 None 26 Human Functional pA2 = 7.9 7.9 1318 2
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 8937736
432 4098 None 26 Human Functional pA2 = 7.9 7.9 1318 2
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 8937736
5697 4098 None 26 Human Functional pA2 = 7.9 7.9 1318 2
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 8937736
CHEMBL273094 4098 None 26 Human Functional pA2 = 7.9 7.9 1318 2
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 8937736
2844 283 None 61 Human Functional pEC50 = 8.3 8.3 -16 5
NoneNone
Drug Central 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
60961 283 None 61 Human Functional pEC50 = 8.3 8.3 -16 5
NoneNone
Drug Central 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
60961.0 283 None 61 Human Functional pEC50 = 8.3 8.3 -16 5
NoneNone
Drug Central 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
90 283 None 61 Human Functional pEC50 = 8.3 8.3 -16 5
NoneNone
Drug Central 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
CHEMBL477 283 None 61 Human Functional pEC50 = 8.3 8.3 -16 5
NoneNone
Drug Central 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
DB00640 283 None 61 Human Functional pEC50 = 8.3 8.3 -16 5
NoneNone
Drug Central 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
219024 3300 None 47 Human Functional pEC50 = 8.3 8.3 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
Drug Central 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 None
219024.0 3300 None 47 Human Functional pEC50 = 8.3 8.3 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
Drug Central 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 None
2362 3300 None 47 Human Functional pEC50 = 8.3 8.3 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
Drug Central 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 None
5596 3300 None 47 Human Functional pEC50 = 8.3 8.3 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
Drug Central 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 None
CHEMBL317052 3300 None 47 Human Functional pEC50 = 8.3 8.3 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
Drug Central 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 None
DB06213 3300 None 47 Human Functional pEC50 = 8.3 8.3 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
Drug Central 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 None
11224 582 None 34 Mouse Functional pIC50 = 6.4 6.4 -6 7
UnclassifiedUnclassified
Guide to Pharmacology 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 30576906
118016229 582 None 34 Mouse Functional pIC50 = 6.4 6.4 -6 7
UnclassifiedUnclassified
Guide to Pharmacology 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 30576906
CHEMBL4522981 582 None 34 Mouse Functional pIC50 = 6.4 6.4 -6 7
UnclassifiedUnclassified
Guide to Pharmacology 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 30576906
11224 582 None 34 Rat Functional pIC50 = 6.6 6.6 -4 7
UnclassifiedUnclassified
Guide to Pharmacology 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 30576906
118016229 582 None 34 Rat Functional pIC50 = 6.6 6.6 -4 7
UnclassifiedUnclassified
Guide to Pharmacology 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 30576906
CHEMBL4522981 582 None 34 Rat Functional pIC50 = 6.6 6.6 -4 7
UnclassifiedUnclassified
Guide to Pharmacology 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 30576906


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
10981286 1919 None 24 Human Binding pEC50 = 4 4.0 -28183 5
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 10.1021/jm0109762
5599 1919 None 24 Human Binding pEC50 = 4 4.0 -28183 5
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 10.1021/jm0109762
5736 1919 None 24 Human Binding pEC50 = 4 4.0 -28183 5
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 10.1021/jm0109762
CHEMBL260563 1919 None 24 Human Binding pEC50 = 4 4.0 -28183 5
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 10.1021/jm0109762
11014608 96412 None 0 Human Binding pEC50 = 4 4.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 389 6 4 9 0.8 CCCCC#Cc1nc(NC(C)C)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
CHEMBL261623 96412 None 0 Human Binding pEC50 = 4 4.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 389 6 4 9 0.8 CCCCC#Cc1nc(NC(C)C)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
10020580 108029 None 3 Human Binding pEC50 = 4 4.0 - 5
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 347 4 4 9 -0.4 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
CHEMBL319387 108029 None 3 Human Binding pEC50 = 4 4.0 - 5
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 347 4 4 9 -0.4 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
11112381 159535 None 0 Human Binding pEC50 = 4 4.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL410115 159535 None 0 Human Binding pEC50 = 4 4.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
10970819 168939 None 0 Human Binding pEC50 = 4 4.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 375 6 4 9 0.4 CCCCC#Cc1nc(NCC)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
CHEMBL437842 168939 None 0 Human Binding pEC50 = 4 4.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 375 6 4 9 0.4 CCCCC#Cc1nc(NCC)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
11068963 200577 None 0 Human Binding pEC50 = 4 4.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 381 3 4 9 -0.1 CNc1nc(C#Cc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL574597 200577 None 0 Human Binding pEC50 = 4 4.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 381 3 4 9 -0.1 CNc1nc(C#Cc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
9932840 77927 None 1 Human Binding pEC50 = 6.0 6.0 - 4
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#CC(O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
CHEMBL2094083 77927 None 1 Human Binding pEC50 = 6.0 6.0 - 4
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#CC(O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
377 2758 None 42 Human Binding pEC50 = 6.9 6.9 -1659 15
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b01662
425 2758 None 42 Human Binding pEC50 = 6.9 6.9 -1659 15
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b01662
448222 2758 None 42 Human Binding pEC50 = 6.9 6.9 -1659 15
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b01662
CHEMBL464859 2758 None 42 Human Binding pEC50 = 6.9 6.9 -1659 15
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b01662
377 2758 None 42 Human Binding pEC50 = 4.8 4.8 -1659 15
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
425 2758 None 42 Human Binding pEC50 = 4.8 4.8 -1659 15
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
448222 2758 None 42 Human Binding pEC50 = 4.8 4.8 -1659 15
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
CHEMBL464859 2758 None 42 Human Binding pEC50 = 4.8 4.8 -1659 15
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
70682890 77843 None 4 Human Binding pEC50 = 5.8 5.8 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL2092788 77843 None 4 Human Binding pEC50 = 5.8 5.8 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
23757284 85163 None 0 Human Binding pEC50 = 6.7 6.7 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#C[C@@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
CHEMBL224874 85163 None 0 Human Binding pEC50 = 6.7 6.7 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#C[C@@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
25268841 8663 None 12 Human Binding pEC50 = 6.6 6.6 - 3
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells using [3H]PSB-603 by functional activity assayBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells using [3H]PSB-603 by functional activity assay
ChEMBL 402 5 1 7 2.6 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(OCCN3CCOCC3)ccc1C2=O 10.1021/acs.jmedchem.0c00914
CHEMBL1095488 8663 None 12 Human Binding pEC50 = 6.6 6.6 - 3
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells using [3H]PSB-603 by functional activity assayBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells using [3H]PSB-603 by functional activity assay
ChEMBL 402 5 1 7 2.6 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(OCCN3CCOCC3)ccc1C2=O 10.1021/acs.jmedchem.0c00914
13830108 77864 None 0 Human Binding pEC50 = 5.6 5.6 - 4
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL2092941 77864 None 0 Human Binding pEC50 = 5.6 5.6 - 4
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
23900137 95818 None 0 Human Binding pEC50 = 5.6 5.6 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#C[C@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
CHEMBL258534 95818 None 0 Human Binding pEC50 = 5.6 5.6 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#C[C@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
2844 283 None 61 Human Binding pEC50 = 4.6 4.6 -467 8
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
60961 283 None 61 Human Binding pEC50 = 4.6 4.6 -467 8
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
60961.0 283 None 61 Human Binding pEC50 = 4.6 4.6 -467 8
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
90 283 None 61 Human Binding pEC50 = 4.6 4.6 -467 8
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
CHEMBL477 283 None 61 Human Binding pEC50 = 4.6 4.6 -467 8
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
DB00640 283 None 61 Human Binding pEC50 = 4.6 4.6 -467 8
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
11026001 96380 None 0 Human Binding pEC50 = 5.6 5.6 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL261453 96380 None 0 Human Binding pEC50 = 5.6 5.6 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
69427076 77841 None 0 Human Binding pEC50 = 5.6 5.6 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL2092786 77841 None 0 Human Binding pEC50 = 5.6 5.6 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
377 2758 None 42 Human Binding pEC50 = 6.5 6.5 -1659 15
Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
425 2758 None 42 Human Binding pEC50 = 6.5 6.5 -1659 15
Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
448222 2758 None 42 Human Binding pEC50 = 6.5 6.5 -1659 15
Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
CHEMBL464859 2758 None 42 Human Binding pEC50 = 6.5 6.5 -1659 15
Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
2844 283 None 61 Human Binding pEC50 = 4.3 4.3 -467 8
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
60961 283 None 61 Human Binding pEC50 = 4.3 4.3 -467 8
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
60961.0 283 None 61 Human Binding pEC50 = 4.3 4.3 -467 8
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
90 283 None 61 Human Binding pEC50 = 4.3 4.3 -467 8
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
CHEMBL477 283 None 61 Human Binding pEC50 = 4.3 4.3 -467 8
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
DB00640 283 None 61 Human Binding pEC50 = 4.3 4.3 -467 8
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
70697521 77842 None 0 Human Binding pEC50 = 5.2 5.2 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL2092787 77842 None 0 Human Binding pEC50 = 5.2 5.2 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
118719026 115499 None 0 Human Binding pEC50 = 5.2 5.2 - 5
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 582 13 4 8 2.1 CC(C)(C)OC(=O)C1CCCN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)OCc1ccccc1 10.1021/jm0109762
CHEMBL3350613 115499 None 0 Human Binding pEC50 = 5.2 5.2 - 5
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 582 13 4 8 2.1 CC(C)(C)OC(=O)C1CCCN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)OCc1ccccc1 10.1021/jm0109762
9978117 158412 None 0 Human Binding pEC50 = 5.2 5.2 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL408918 158412 None 0 Human Binding pEC50 = 5.2 5.2 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
123807 871 None 35 Human Binding pEC50 = 4.1 4.1 -13803 13
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/acs.jmedchem.5b01402
374 871 None 35 Human Binding pEC50 = 4.1 4.1 -13803 13
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/acs.jmedchem.5b01402
379 871 None 35 Human Binding pEC50 = 4.1 4.1 -13803 13
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/acs.jmedchem.5b01402
CHEMBL284969 871 None 35 Human Binding pEC50 = 4.1 4.1 -13803 13
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/acs.jmedchem.5b01402
10455080 95819 None 0 Human Binding pEC50 = 6.1 6.1 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL258535 95819 None 0 Human Binding pEC50 = 6.1 6.1 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
11048438 169001 None 0 Human Binding pEC50 = 5.1 5.1 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL438418 169001 None 0 Human Binding pEC50 = 5.1 5.1 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
11112711 159515 None 0 Human Binding pEC50 = 5.0 5.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL410095 159515 None 0 Human Binding pEC50 = 5.0 5.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
44450290 96528 None 0 Human Binding pEC50 = 6.0 6.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL262363 96528 None 0 Human Binding pEC50 = 6.0 6.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
215492 16478 None 1 Human Binding pEC50 = 6.0 6.0 - 3
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based assay
ChEMBL 324 4 5 10 -2.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCO)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.8b01662
CHEMBL1234591 16478 None 1 Human Binding pEC50 = 6.0 6.0 - 3
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based assay
ChEMBL 324 4 5 10 -2.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCO)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.8b01662
10455852 96106 None 0 Human Binding pEC50 = 6.0 6.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL259938 96106 None 0 Human Binding pEC50 = 6.0 6.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
3284 3216 None 29 Human Binding pIC50 = 9.3 9.3 -1 7
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
44185871 3216 None 29 Human Binding pIC50 = 9.3 9.3 -1 7
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
5728 3216 None 29 Human Binding pIC50 = 9.3 9.3 -1 7
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
CHEMBL483688 3216 None 29 Human Binding pIC50 = 9.3 9.3 -1 7
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
3284 3216 None 29 Human Binding pIC50 = 9.1 9.1 -1 7
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
44185871 3216 None 29 Human Binding pIC50 = 9.1 9.1 -1 7
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
5728 3216 None 29 Human Binding pIC50 = 9.1 9.1 -1 7
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
CHEMBL483688 3216 None 29 Human Binding pIC50 = 9.1 9.1 -1 7
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
169151077 196555 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assayBinding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assay
ChEMBL 417 4 2 8 3.5 COc1cccc2c1nc(N)n1nc(C3CCC(c4ccc(C(C)(C)N)cn4)C3)nc21 10.1021/acsmedchemlett.3c00473
CHEMBL5426527 196555 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assayBinding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assay
ChEMBL 417 4 2 8 3.5 COc1cccc2c1nc(N)n1nc(C3CCC(c4ccc(C(C)(C)N)cn4)C3)nc21 10.1021/acsmedchemlett.3c00473
16037920 168865 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 571 5 1 7 2.5 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Br)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL437309 168865 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 571 5 1 7 2.5 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Br)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
74944536 164684 None 1 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 540 7 0 7 2.8 CCCN1C(=O)N=C2N=C(c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)cc5)CC4)cc3)N=C2C1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4215606 164684 None 1 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 540 7 0 7 2.8 CCCN1C(=O)N=C2N=C(c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)cc5)CC4)cc3)N=C2C1=O 10.1021/acs.jmedchem.7b01627
169150773 195918 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assayBinding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assay
ChEMBL 417 4 2 8 3.4 COc1cccc2c1nc(N)n1nc([C@H]3C[C@H](c4ncc(C(C)(C)N)cc4C)C3)nc21 10.1021/acsmedchemlett.3c00473
CHEMBL5413371 195918 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assayBinding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assay
ChEMBL 417 4 2 8 3.4 COc1cccc2c1nc(N)n1nc([C@H]3C[C@H](c4ncc(C(C)(C)N)cc4C)C3)nc21 10.1021/acsmedchemlett.3c00473
44413112 139392 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 511 5 1 7 1.9 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL379217 139392 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 511 5 1 7 1.9 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
134148336 148415 None 0 Human Binding pIC50 = 6 6.0 - 2
Displacement of [3H]PSB603 from recombinant human adenosine A2B receptor expressed in HEK293 cell membranes after 1 hr by beta scintillation counting methodDisplacement of [3H]PSB603 from recombinant human adenosine A2B receptor expressed in HEK293 cell membranes after 1 hr by beta scintillation counting method
ChEMBL 395 4 2 4 5.7 O[C@H]1CC[C@H](Nc2ncc(-c3ccc4ccccc4c3)c(-c3ccccc3)n2)CC1 10.1016/j.ejmech.2016.09.081
CHEMBL3937015 148415 None 0 Human Binding pIC50 = 6 6.0 - 2
Displacement of [3H]PSB603 from recombinant human adenosine A2B receptor expressed in HEK293 cell membranes after 1 hr by beta scintillation counting methodDisplacement of [3H]PSB603 from recombinant human adenosine A2B receptor expressed in HEK293 cell membranes after 1 hr by beta scintillation counting method
ChEMBL 395 4 2 4 5.7 O[C@H]1CC[C@H](Nc2ncc(-c3ccc4ccccc4c3)c(-c3ccccc3)n2)CC1 10.1016/j.ejmech.2016.09.081
2519 779 None 49 Human Binding pIC50 = 5.0 5.0 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
2519.0 779 None 49 Human Binding pIC50 = 5.0 5.0 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
407 779 None 49 Human Binding pIC50 = 5.0 5.0 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
463 779 None 49 Human Binding pIC50 = 5.0 5.0 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
CHEMBL113 779 None 49 Human Binding pIC50 = 5.0 5.0 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
DB00201 779 None 49 Human Binding pIC50 = 5.0 5.0 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
44236568 156561 None 0 Human Binding pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 486 6 1 8 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4067401 156561 None 0 Human Binding pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 486 6 1 8 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
155552077 175532 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 496 6 1 9 2.6 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1nc2cc(S(N)(=O)=O)ccc2o1 10.1016/j.ejmech.2018.11.045
CHEMBL4576194 175532 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 496 6 1 9 2.6 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1nc2cc(S(N)(=O)=O)ccc2o1 10.1016/j.ejmech.2018.11.045
155542641 173257 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 424 8 0 8 2.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cn3ccnc3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4521489 173257 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 424 8 0 8 2.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cn3ccnc3)sc21 10.1016/j.ejmech.2018.11.045
10237847 77488 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 411 4 2 7 1.4 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)Nc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL208705 77488 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 411 4 2 7 1.4 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)Nc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
10196517 78354 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 553 8 2 7 3.3 CCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccc(F)cc5)CC4)cc3)cc2n(CC)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL210969 78354 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 553 8 2 7 3.3 CCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccc(F)cc5)CC4)cc3)cc2n(CC)c1=O 10.1016/j.bmcl.2006.04.074
155568402 176115 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 468 8 1 9 2.4 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(C)(O)c3cncn3C)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4589654 176115 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 468 8 1 9 2.4 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(C)(O)c3cncn3C)sc21 10.1016/j.ejmech.2018.11.045
2690 903 None 44 Human Binding pIC50 = 5.9 5.9 -30 9
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm980094b
384 903 None 44 Human Binding pIC50 = 5.9 5.9 -30 9
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm980094b
CHEMBL16687 903 None 44 Human Binding pIC50 = 5.9 5.9 -30 9
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm980094b
10812045 15528 None 0 Human Binding pIC50 = 6.9 6.9 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2OC)CC1 10.1039/C1MD00213A
CHEMBL121766 15528 None 0 Human Binding pIC50 = 6.9 6.9 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2OC)CC1 10.1039/C1MD00213A
44413202 78424 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 565 7 1 9 2.3 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)cc21 10.1016/j.bmcl.2006.04.074
CHEMBL211071 78424 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 565 7 1 9 2.3 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)cc21 10.1016/j.bmcl.2006.04.074
155527056 171244 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 366 5 1 6 2.5 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1ncc[nH]1 10.1016/j.ejmech.2018.11.045
CHEMBL4458469 171244 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 366 5 1 6 2.5 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1ncc[nH]1 10.1016/j.ejmech.2018.11.045
155550407 174035 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 325 4 0 6 2.3 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CC#N 10.1016/j.ejmech.2018.11.045
CHEMBL4540909 174035 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 325 4 0 6 2.3 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CC#N 10.1016/j.ejmech.2018.11.045
155525648 171196 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 366 5 1 6 2.5 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1cnc[nH]1 10.1016/j.ejmech.2018.11.045
CHEMBL4457584 171196 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 366 5 1 6 2.5 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1cnc[nH]1 10.1016/j.ejmech.2018.11.045
10766773 210578 None 0 Human Binding pIC50 = 4.9 4.9 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 356 4 2 7 2.5 NCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
CHEMBL97961 210578 None 0 Human Binding pIC50 = 4.9 4.9 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 356 4 2 7 2.5 NCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
155515805 170110 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 332 5 0 5 2.7 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CCF 10.1016/j.ejmech.2018.11.045
CHEMBL4442438 170110 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 332 5 0 5 2.7 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CCF 10.1016/j.ejmech.2018.11.045
155526484 171229 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 414 8 1 7 2.9 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(O)C3CC3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4458223 171229 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 414 8 1 7 2.9 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(O)C3CC3)sc21 10.1016/j.ejmech.2018.11.045
10288169 79790 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 439 6 2 7 1.1 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL211762 79790 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 439 6 2 7 1.1 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
155515166 170034 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 380 5 0 7 2.6 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1nccn1C 10.1016/j.ejmech.2018.11.045
CHEMBL4441343 170034 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 380 5 0 7 2.6 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1nccn1C 10.1016/j.ejmech.2018.11.045
44413113 78349 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 539 7 1 7 2.8 CCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)cc2n(CC)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL210931 78349 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 539 7 1 7 2.8 CCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)cc2n(CC)c1=O 10.1016/j.bmcl.2006.04.074
44413192 79964 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 483 8 2 8 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCc4ccc(OC)cn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL212528 79964 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 483 8 2 8 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCc4ccc(OC)cn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
122574772 171190 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 374 7 1 7 1.9 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(CO)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4457476 171190 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 374 7 1 7 1.9 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(CO)sc21 10.1016/j.ejmech.2018.11.045
155548802 173912 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 428 8 1 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(C)(O)C3CC3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4538262 173912 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 428 8 1 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(C)(O)C3CC3)sc21 10.1016/j.ejmech.2018.11.045
155562247 175827 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 370 6 0 6 2.9 COCCn1c(=O)n(CC2(c3ccccc3)CC2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
CHEMBL4582620 175827 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 370 6 0 6 2.9 COCCn1c(=O)n(CC2(c3ccccc3)CC2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
10311222 77772 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 493 5 1 7 1.7 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL209019 77772 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 493 5 1 7 1.7 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
155521875 170711 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 310 4 0 6 2.2 COCCn1c(=O)n(CC(C)(C)C)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
CHEMBL4450782 170711 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 310 4 0 6 2.2 COCCn1c(=O)n(CC(C)(C)C)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
10310578 77818 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 455 7 2 8 1.0 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCOc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL209208 77818 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 455 7 2 8 1.0 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCOc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
10238677 79946 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 467 8 2 7 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL212464 79946 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 467 8 2 7 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
44413193 140219 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 539 7 1 7 2.8 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)cc21 10.1016/j.bmcl.2006.04.074
CHEMBL380177 140219 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 539 7 1 7 2.8 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)cc21 10.1016/j.bmcl.2006.04.074
155523243 170937 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 469 7 1 7 2.7 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CCc1ccc(S(N)(=O)=O)cc1 10.1016/j.ejmech.2018.11.045
CHEMBL4453664 170937 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 469 7 1 7 2.7 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CCc1ccc(S(N)(=O)=O)cc1 10.1016/j.ejmech.2018.11.045
155533818 171999 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 416 8 0 8 2.6 CCOC(=O)c1sc2c(c1C)c(=O)n(CCc1ccccc1)c(=O)n2CCOC 10.1016/j.ejmech.2018.11.045
CHEMBL4469697 171999 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 416 8 0 8 2.6 CCOC(=O)c1sc2c(c1C)c(=O)n(CCc1ccccc1)c(=O)n2CCOC 10.1016/j.ejmech.2018.11.045
10577289 210532 None 0 Human Binding pIC50 = 5.8 5.8 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 384 6 2 7 3.3 NCCCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
CHEMBL97700 210532 None 0 Human Binding pIC50 = 5.8 5.8 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 384 6 2 7 3.3 NCCCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
10153029 78077 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 563 10 2 7 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL209944 78077 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 563 10 2 7 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmcl.2006.04.074
10288197 78203 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 441 5 2 8 1.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)cn1 10.1016/j.bmcl.2006.04.074
CHEMBL210456 78203 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 441 5 2 8 1.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)cn1 10.1016/j.bmcl.2006.04.074
155521508 170807 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 370 5 0 6 3.0 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CC1CCCO1 10.1016/j.ejmech.2018.11.045
CHEMBL4451942 170807 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 370 5 0 6 3.0 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CC1CCCO1 10.1016/j.ejmech.2018.11.045
155555355 174546 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 452 8 0 9 2.4 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)c3cn(C)cn3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4553423 174546 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 452 8 0 9 2.4 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)c3cn(C)cn3)sc21 10.1016/j.ejmech.2018.11.045
155551709 175247 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 438 8 1 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cc3nc[nH]c3C)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4569909 175247 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 438 8 1 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cc3nc[nH]c3C)sc21 10.1016/j.ejmech.2018.11.045
169150840 197070 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assayBinding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assay
ChEMBL 437 4 2 8 3.8 COc1cccc2c1nc(N)n1nc([C@H]3C[C@H](c4ncc(C(C)(C)N)cc4Cl)C3)nc21 10.1021/acsmedchemlett.3c00473
CHEMBL5438060 197070 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assayBinding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assay
ChEMBL 437 4 2 8 3.8 COc1cccc2c1nc(N)n1nc([C@H]3C[C@H](c4ncc(C(C)(C)N)cc4Cl)C3)nc21 10.1021/acsmedchemlett.3c00473
172465064 196700 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assayBinding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assay
ChEMBL 385 3 1 8 3.0 COc1cccc2c1nc(N)n1nc(C3CC3c3nc4ccccc4n3C)nc21 10.1021/acsmedchemlett.3c00473
CHEMBL5430246 196700 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assayBinding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assay
ChEMBL 385 3 1 8 3.0 COc1cccc2c1nc(N)n1nc(C3CC3c3nc4ccccc4n3C)nc21 10.1021/acsmedchemlett.3c00473
44413182 78204 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 455 6 2 8 1.1 COc1ccc(CNS(=O)(=O)c2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)nc1 10.1016/j.bmcl.2006.04.074
CHEMBL210457 78204 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 455 6 2 8 1.1 COc1ccc(CNS(=O)(=O)c2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)nc1 10.1016/j.bmcl.2006.04.074
155521394 170693 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 443 7 1 8 1.2 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)N3CC(O)C3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4450633 170693 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 443 7 1 8 1.2 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)N3CC(O)C3)sc21 10.1016/j.ejmech.2018.11.045
155523200 170858 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 427 8 0 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(CN3CCCC3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4452532 170858 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 427 8 0 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(CN3CCCC3)sc21 10.1016/j.ejmech.2018.11.045
155526352 171316 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 358 6 0 6 2.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4459477 171316 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 358 6 0 6 2.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C)sc21 10.1016/j.ejmech.2018.11.045
155543633 173305 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 405 4 1 7 1.3 CCn1c(=O)c2c(C)c(C(=O)N3CC(O)C3)sc2n(CCC(F)(F)F)c1=O 10.1016/j.ejmech.2018.11.045
CHEMBL4522738 173305 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 405 4 1 7 1.3 CCn1c(=O)c2c(C)c(C(=O)N3CC(O)C3)sc2n(CCC(F)(F)F)c1=O 10.1016/j.ejmech.2018.11.045
44236539 156884 None 0 Human Binding pIC50 = 5.7 5.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 460 7 2 8 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C(=O)O)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4070936 156884 None 0 Human Binding pIC50 = 5.7 5.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 460 7 2 8 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C(=O)O)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
10645984 18824 None 0 Human Binding pIC50 = 5.7 5.7 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cccc(Cl)c2)CC1 10.1039/C1MD00213A
CHEMBL127876 18824 None 0 Human Binding pIC50 = 5.7 5.7 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cccc(Cl)c2)CC1 10.1039/C1MD00213A
155549589 174021 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 362 6 0 6 2.6 COCCn1c(=O)n(CCc2ccccc2F)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
CHEMBL4540558 174021 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 362 6 0 6 2.6 COCCn1c(=O)n(CCc2ccccc2F)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
118016325 170176 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 388 7 1 7 2.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)O)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4443243 170176 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 388 7 1 7 2.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)O)sc21 10.1016/j.ejmech.2018.11.045
155514761 169994 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 294 4 0 6 1.4 CCn1c(=O)c2c3c(sc2n(CCOC)c1=O)CCC3 10.1016/j.ejmech.2018.11.045
CHEMBL4440686 169994 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 294 4 0 6 1.4 CCn1c(=O)c2c3c(sc2n(CCOC)c1=O)CCC3 10.1016/j.ejmech.2018.11.045
45073485 163712 None 7 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 506 7 0 7 2.2 CCCN1C(=O)N=C2N=C(c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)N=C2C1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4203745 163712 None 7 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 506 7 0 7 2.2 CCCN1C(=O)N=C2N=C(c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)N=C2C1=O 10.1021/acs.jmedchem.7b01627
155562338 175951 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 448 8 0 7 3.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)c3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4585480 175951 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 448 8 0 7 3.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)c3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
10474279 107366 None 0 Human Binding pIC50 = 5.6 5.6 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 369 2 1 6 4.2 CC(C)(C)C(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
CHEMBL317310 107366 None 0 Human Binding pIC50 = 5.6 5.6 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 369 2 1 6 4.2 CC(C)(C)C(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
10691504 210240 None 0 Human Binding pIC50 = 5.6 5.6 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 385 2 1 7 4.5 CC(C)(C)OC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
CHEMBL96041 210240 None 0 Human Binding pIC50 = 5.6 5.6 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 385 2 1 7 4.5 CC(C)(C)OC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
10669778 117539 None 0 Human Binding pIC50 = 6.6 6.6 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1ccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1 10.1039/C1MD00213A
CHEMBL339936 117539 None 0 Human Binding pIC50 = 6.6 6.6 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1ccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1 10.1039/C1MD00213A
155522968 170872 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 442 9 0 7 3.9 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(COC3CCCC3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4452799 170872 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 442 9 0 7 3.9 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(COC3CCCC3)sc21 10.1016/j.ejmech.2018.11.045
155558166 174858 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 441 7 0 7 2.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)N3CCCC3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4560841 174858 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 441 7 0 7 2.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)N3CCCC3)sc21 10.1016/j.ejmech.2018.11.045
71600087 154446 None 47 Human Binding pIC50 = 5.6 5.6 - 0
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 459 6 2 5 4.4 CCS(=O)(=O)Nc1ccc(Oc2ccc(F)cc2F)c(-c2cn(C)c(=O)c3[nH]ccc23)c1 10.1021/acs.jmedchem.7b00746
CHEMBL3987016 154446 None 47 Human Binding pIC50 = 5.6 5.6 - 0
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 459 6 2 5 4.4 CCS(=O)(=O)Nc1ccc(Oc2ccc(F)cc2F)c(-c2cn(C)c(=O)c3[nH]ccc23)c1 10.1021/acs.jmedchem.7b00746
10616222 107502 None 0 Human Binding pIC50 = 5.6 5.6 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 327 2 1 6 3.1 CC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
CHEMBL318251 107502 None 0 Human Binding pIC50 = 5.6 5.6 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 327 2 1 6 3.1 CC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
44413130 79989 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 494 5 1 8 1.1 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccncc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL212642 79989 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 494 5 1 8 1.1 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccncc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
10339165 210203 None 0 Human Binding pIC50 = 6.6 6.6 -2 4
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 370 5 2 7 2.9 NCCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
CHEMBL95811 210203 None 0 Human Binding pIC50 = 6.6 6.6 -2 4
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 370 5 2 7 2.9 NCCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
135418256 15576 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.
ChEMBL 326 4 1 5 3.7 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(Cl)cc3)nn12 10.1016/j.bmcl.2004.04.099
CHEMBL122037 15576 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.
ChEMBL 326 4 1 5 3.7 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(Cl)cc3)nn12 10.1016/j.bmcl.2004.04.099
11224 582 None 34 Rat Binding pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant rat A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant rat A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
118016229 582 None 34 Rat Binding pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant rat A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant rat A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
CHEMBL4522981 582 None 34 Rat Binding pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant rat A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant rat A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
155548182 173892 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 345 6 0 7 1.8 COCCn1c(=O)n(CCc2cccnc2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
CHEMBL4537687 173892 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 345 6 0 7 1.8 COCCn1c(=O)n(CCc2cccnc2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
155536243 172283 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 470 8 0 6 4.6 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(F)(F)c3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4473551 172283 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 470 8 0 6 4.6 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(F)(F)c3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
169150931 195916 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assayBinding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assay
ChEMBL 386 3 2 7 2.8 COc1cccc2c1nc(N)n1nc(C3CC3c3ccc4c(c3)CCNC4)nc21 10.1021/acsmedchemlett.3c00473
CHEMBL5413330 195916 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assayBinding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assay
ChEMBL 386 3 2 7 2.8 COc1cccc2c1nc(N)n1nc(C3CC3c3ccc4c(c3)CCNC4)nc21 10.1021/acsmedchemlett.3c00473
169151069 196565 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assayBinding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assay
ChEMBL 404 4 2 8 3.2 COc1cccc2c1nc(N)n1nc([C@H]3C[C@H](c4ccc(C(C)(C)O)cn4)C3)nc21 10.1021/acsmedchemlett.3c00473
CHEMBL5426841 196565 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assayBinding affinity to recombinant human adenosine A2B receptor expressed in HEK293 cell membrane incubated for 15 to 30 mins by Topcount scintillation counter assay
ChEMBL 404 4 2 8 3.2 COc1cccc2c1nc(N)n1nc([C@H]3C[C@H](c4ccc(C(C)(C)O)cn4)C3)nc21 10.1021/acsmedchemlett.3c00473
1329 1472 None 53 Human Binding pIC50 = 8.4 8.4 -1288 14
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.7b01627
386 1472 None 53 Human Binding pIC50 = 8.4 8.4 -1288 14
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.7b01627
CHEMBL183 1472 None 53 Human Binding pIC50 = 8.4 8.4 -1288 14
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.7b01627
DB12946 1472 None 53 Human Binding pIC50 = 8.4 8.4 -1288 14
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.7b01627
155519860 170518 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 450 8 1 7 3.5 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(O)c3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4448231 170518 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 450 8 1 7 3.5 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(O)c3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
155544551 173498 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 344 6 0 6 2.4 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
CHEMBL4528081 173498 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 344 6 0 6 2.4 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
449 2643 None 38 Human Binding pIC50 = 7.5 7.5 -1 9
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N nan
453 2643 None 38 Human Binding pIC50 = 7.5 7.5 -1 9
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N nan
6603931 2643 None 38 Human Binding pIC50 = 7.5 7.5 -1 9
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N nan
CHEMBL273807 2643 None 38 Human Binding pIC50 = 7.5 7.5 -1 9
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N nan
71601630 86956 None 0 Human Binding pIC50 = 6.5 6.5 - 2
Inhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assayInhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assay
ChEMBL 225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1021/jm400068e
CHEMBL2322916 86956 None 0 Human Binding pIC50 = 6.5 6.5 - 2
Inhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assayInhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assay
ChEMBL 225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1021/jm400068e
155517038 170262 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 378 6 0 6 3.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cl)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4444370 170262 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 378 6 0 6 3.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cl)sc21 10.1016/j.ejmech.2018.11.045
155541364 173093 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 380 5 1 6 2.9 Cc1[nH]cnc1Cn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
CHEMBL4517977 173093 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 380 5 1 6 2.9 Cc1[nH]cnc1Cn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
10717193 16789 None 0 Human Binding pIC50 = 5.4 5.4 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccc(Cl)cc2)CC1 10.1039/C1MD00213A
CHEMBL124485 16789 None 0 Human Binding pIC50 = 5.4 5.4 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccc(Cl)cc2)CC1 10.1039/C1MD00213A
155526277 171221 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 449 7 1 7 2.7 CCN(CC(C)(C)O)C(=O)c1sc2c(c1C)c(=O)n(CC)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
CHEMBL4458042 171221 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 449 7 1 7 2.7 CCN(CC(C)(C)O)C(=O)c1sc2c(c1C)c(=O)n(CC)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
155522797 170904 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 308 4 0 6 1.8 CCn1c(=O)c2c3c(sc2n(CCOC)c1=O)CCCC3 10.1016/j.ejmech.2018.11.045
CHEMBL4453228 170904 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 308 4 0 6 1.8 CCn1c(=O)c2c3c(sc2n(CCOC)c1=O)CCCC3 10.1016/j.ejmech.2018.11.045
155548102 173822 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 431 8 0 8 2.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)N(C)OC)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4536104 173822 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 431 8 0 8 2.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)N(C)OC)sc21 10.1016/j.ejmech.2018.11.045
10218183 79797 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 533 5 1 8 2.5 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)s5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL211813 79797 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 533 5 1 8 2.5 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)s5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
11224 582 None 34 Mouse Binding pIC50 = 6.4 6.4 - 1
Antagonist activity at recombinant mouse A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant mouse A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
118016229 582 None 34 Mouse Binding pIC50 = 6.4 6.4 - 1
Antagonist activity at recombinant mouse A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant mouse A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
CHEMBL4522981 582 None 34 Mouse Binding pIC50 = 6.4 6.4 - 1
Antagonist activity at recombinant mouse A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant mouse A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
1922 205276 None 33 Human Binding pIC50 = 6.4 6.4 -26 6
Inhibitory activity against cyclic AMP production in human Adenosine A2B receptor assayInhibitory activity against cyclic AMP production in human Adenosine A2B receptor assay
ChEMBL 256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O 10.1021/jm990499b
CHEMBL62350 205276 None 33 Human Binding pIC50 = 6.4 6.4 -26 6
Inhibitory activity against cyclic AMP production in human Adenosine A2B receptor assayInhibitory activity against cyclic AMP production in human Adenosine A2B receptor assay
ChEMBL 256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O 10.1021/jm990499b
155520492 170585 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 443 9 0 7 2.9 CCN(CC)C(=O)c1sc2c(c1C)c(=O)n(CCc1ccccc1)c(=O)n2CCOC 10.1016/j.ejmech.2018.11.045
CHEMBL4449139 170585 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 443 9 0 7 2.9 CCN(CC)C(=O)c1sc2c(c1C)c(=O)n(CCc1ccccc1)c(=O)n2CCOC 10.1016/j.ejmech.2018.11.045
71601632 86958 None 0 Human Binding pIC50 = 6.4 6.4 - 2
Inhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assayInhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assay
ChEMBL 301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1021/jm400068e
CHEMBL2322918 86958 None 0 Human Binding pIC50 = 6.4 6.4 - 2
Inhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assayInhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assay
ChEMBL 301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1021/jm400068e
44413136 79298 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 507 6 2 7 2.2 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL211347 79298 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 507 6 2 7 2.2 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
155518555 170397 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 387 7 1 7 1.5 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(N)=O)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4446433 170397 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 387 7 1 7 1.5 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(N)=O)sc21 10.1016/j.ejmech.2018.11.045
155537687 172434 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 380 6 0 6 3.0 COCCn1c(=O)n(CC(F)(F)c2ccccc2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
CHEMBL4475483 172434 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 380 6 0 6 3.0 COCCn1c(=O)n(CC(F)(F)c2ccccc2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
155560676 175219 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 282 4 0 6 1.5 CCn1c(=O)c2c(C)c(C)sc2n(CCOC)c1=O 10.1016/j.ejmech.2018.11.045
CHEMBL4569387 175219 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 282 4 0 6 1.5 CCn1c(=O)c2c(C)c(C)sc2n(CCOC)c1=O 10.1016/j.ejmech.2018.11.045
71601631 86957 None 0 Human Binding pIC50 = 6.4 6.4 - 2
Inhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assayInhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assay
ChEMBL 287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12 10.1021/jm400068e
CHEMBL2322917 86957 None 0 Human Binding pIC50 = 6.4 6.4 - 2
Inhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assayInhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assay
ChEMBL 287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12 10.1021/jm400068e
155512463 169738 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 330 6 0 6 2.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2ccsc21 10.1016/j.ejmech.2018.11.045
CHEMBL4437132 169738 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 330 6 0 6 2.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2ccsc21 10.1016/j.ejmech.2018.11.045
59351824 174130 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 286 3 1 4 2.3 Cc1csc2[nH]c(=O)n(CCc3ccccc3)c(=O)c12 10.1016/j.ejmech.2018.11.045
CHEMBL4543255 174130 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 286 3 1 4 2.3 Cc1csc2[nH]c(=O)n(CCc3ccccc3)c(=O)c12 10.1016/j.ejmech.2018.11.045
155537810 172431 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 384 6 0 6 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c3c(sc21)CCCC3 10.1016/j.ejmech.2018.11.045
CHEMBL4475461 172431 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 384 6 0 6 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c3c(sc21)CCCC3 10.1016/j.ejmech.2018.11.045
155520204 170570 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 420 7 0 6 4.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(-c3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4448896 170570 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 420 7 0 6 4.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(-c3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
155559377 174952 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 316 5 0 6 2.0 COCCn1c(=O)n(CC=C(F)F)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
CHEMBL4562969 174952 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 316 5 0 6 2.0 COCCn1c(=O)n(CC=C(F)F)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
11796362 115165 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1cccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)c1 10.1039/C1MD00213A
CHEMBL334325 115165 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1cccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)c1 10.1039/C1MD00213A
155529645 171531 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 421 7 1 7 2.0 CCN(CCO)C(=O)c1sc2c(c1C)c(=O)n(CC)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
CHEMBL4462879 171531 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 421 7 1 7 2.0 CCN(CCO)C(=O)c1sc2c(c1C)c(=O)n(CC)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
155521508 170807 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 370 5 0 6 3.0 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CC1CCCO1 10.1016/j.ejmech.2018.11.045
CHEMBL4451942 170807 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 370 5 0 6 3.0 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CC1CCCO1 10.1016/j.ejmech.2018.11.045
155551418 174067 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 434 8 0 6 4.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cc3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4541543 174067 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 434 8 0 6 4.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cc3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
155569093 176107 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 383 5 0 6 3.1 Cc1csc2c1c(=O)n(CCc1cccnc1)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
CHEMBL4589448 176107 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 383 5 0 6 3.1 Cc1csc2c1c(=O)n(CCc1cccnc1)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
155537122 172368 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 382 5 0 5 3.7 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
CHEMBL4474572 172368 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 382 5 0 5 3.7 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
10550242 17264 None 0 Human Binding pIC50 = 5.2 5.2 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2Cl)CC1 10.1039/C1MD00213A
CHEMBL125670 17264 None 0 Human Binding pIC50 = 5.2 5.2 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2Cl)CC1 10.1039/C1MD00213A
11224 582 None 34 Human Binding pIC50 = 7.2 7.2 - 1
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
118016229 582 None 34 Human Binding pIC50 = 7.2 7.2 - 1
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
CHEMBL4522981 582 None 34 Human Binding pIC50 = 7.2 7.2 - 1
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
44413154 78034 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 479 4 1 7 1.7 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL209742 78034 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 479 4 1 7 1.7 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
44413106 79933 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 546 7 1 8 2.5 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C#N)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL212416 79933 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 546 7 1 8 2.5 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C#N)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
2690 903 None 44 Human Binding pIC50 = 7.2 7.2 -30 9
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/acs.jmedchem.7b01627
384 903 None 44 Human Binding pIC50 = 7.2 7.2 -30 9
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/acs.jmedchem.7b01627
CHEMBL16687 903 None 44 Human Binding pIC50 = 7.2 7.2 -30 9
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/acs.jmedchem.7b01627
122574669 175936 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 268 4 0 6 1.2 CCn1c(=O)c2c(C)csc2n(CCOC)c1=O 10.1016/j.ejmech.2018.11.045
CHEMBL4585015 175936 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 268 4 0 6 1.2 CCn1c(=O)c2c(C)csc2n(CCOC)c1=O 10.1016/j.ejmech.2018.11.045
10645103 164436 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 407 6 1 6 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2F)CC1 10.1039/C1MD00213A
CHEMBL421256 164436 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 407 6 1 6 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2F)CC1 10.1039/C1MD00213A
11224 582 None 34 Human Binding pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant human A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
118016229 582 None 34 Human Binding pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant human A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
CHEMBL4522981 582 None 34 Human Binding pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant human A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
10193 3010 None 42 Human Binding pIC50 = 6.2 6.2 -46 4
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 nan
53466958 3010 None 42 Human Binding pIC50 = 6.2 6.2 -46 4
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 nan
53466958.0 3010 None 42 Human Binding pIC50 = 6.2 6.2 -46 4
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 nan
CHEMBL3638684 3010 None 42 Human Binding pIC50 = 6.2 6.2 -46 4
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 nan
CHEMBL3694769 3010 None 42 Human Binding pIC50 = 6.2 6.2 -46 4
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 nan
44413125 78106 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 529 5 1 7 2.0 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5F)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL210088 78106 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 529 5 1 7 2.0 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5F)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
10196060 78178 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 511 5 1 7 1.9 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL210383 78178 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 511 5 1 7 1.9 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
155259564 185325 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 339 5 3 9 1.2 Nc1nc(NCCc2ccc(O)cc2)nc2nc(C3=CCCO3)nn12 nan
CHEMBL4857871 185325 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 339 5 3 9 1.2 Nc1nc(NCCc2ccc(O)cc2)nc2nc(C3=CCCO3)nn12 nan
155559834 175024 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 400 5 0 5 3.9 Cc1csc2c1c(=O)n(CCc1ccccc1F)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
CHEMBL4564912 175024 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 400 5 0 5 3.9 Cc1csc2c1c(=O)n(CCc1ccccc1F)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
10621961 210539 None 0 Human Binding pIC50 = 5.1 5.1 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 418 4 2 7 4.0 Nc1ccc(CC(=O)Nc2nc3ccc(Cl)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm980094b
CHEMBL97748 210539 None 0 Human Binding pIC50 = 5.1 5.1 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 418 4 2 7 4.0 Nc1ccc(CC(=O)Nc2nc3ccc(Cl)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm980094b
44413096 139057 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 467 8 2 7 2.1 CCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(CC)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL378527 139057 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 467 8 2 7 2.1 CCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(CC)c1=O 10.1016/j.bmcl.2006.04.074
155552481 174161 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 443 8 0 8 2.3 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(CN3CCOCC3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4544040 174161 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 443 8 0 8 2.3 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(CN3CCOCC3)sc21 10.1016/j.ejmech.2018.11.045
155541183 173115 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 412 8 0 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)C3CC3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4518356 173115 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 412 8 0 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)C3CC3)sc21 10.1016/j.ejmech.2018.11.045
155553932 175554 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 438 8 1 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cc3c[nH]c(C)n3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4576817 175554 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 438 8 1 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cc3c[nH]c(C)n3)sc21 10.1016/j.ejmech.2018.11.045
57429602 157331 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4076435 157331 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
44413142 78240 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 521 6 1 7 2.5 CN(C1CCN(Cc2ccccc2)CC1)S(=O)(=O)c1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1016/j.bmcl.2006.04.074
CHEMBL210560 78240 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 521 6 1 7 2.5 CN(C1CCN(Cc2ccccc2)CC1)S(=O)(=O)c1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1016/j.bmcl.2006.04.074
176407 4148 None 56 Human Binding pIC50 = 7.0 7.0 -34 6
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.7b01627
405 4148 None 56 Human Binding pIC50 = 7.0 7.0 -34 6
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.7b01627
CHEMBL113142 4148 None 56 Human Binding pIC50 = 7.0 7.0 -34 6
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.7b01627
DB08770 4148 None 56 Human Binding pIC50 = 7.0 7.0 -34 6
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.7b01627
135515408 117138 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.
ChEMBL 310 4 1 5 3.1 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(F)cc3)nn12 10.1016/j.bmcl.2004.04.099
CHEMBL339218 117138 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.
ChEMBL 310 4 1 5 3.1 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(F)cc3)nn12 10.1016/j.bmcl.2004.04.099
155540197 173005 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 370 6 0 6 2.6 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c3c(sc21)CCC3 10.1016/j.ejmech.2018.11.045
CHEMBL4516075 173005 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 370 6 0 6 2.6 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c3c(sc21)CCC3 10.1016/j.ejmech.2018.11.045
155549654 174010 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 435 8 0 7 2.6 CCN(CC)C(=O)c1sc2c(c1C)c(=O)n(CCOC)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
CHEMBL4540250 174010 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 435 8 0 7 2.6 CCN(CC)C(=O)c1sc2c(c1C)c(=O)n(CCOC)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
450 2970 None 7 Human Binding pKd = 9.8 9.8 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm900413e
454 2970 None 7 Human Binding pKd = 9.8 9.8 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm900413e
5311041 2970 None 7 Human Binding pKd = 9.8 9.8 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm900413e
CHEMBL485862 2970 None 7 Human Binding pKd = 9.8 9.8 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm900413e
3284 3216 None 29 Mouse Binding pKd = 9.5 9.5 1 7
Displacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
44185871 3216 None 29 Mouse Binding pKd = 9.5 9.5 1 7
Displacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
5728 3216 None 29 Mouse Binding pKd = 9.5 9.5 1 7
Displacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
CHEMBL483688 3216 None 29 Mouse Binding pKd = 9.5 9.5 1 7
Displacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
3284 3216 None 29 Human Binding pKd = 9.4 9.4 -1 7
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experimentBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experiment
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
44185871 3216 None 29 Human Binding pKd = 9.4 9.4 -1 7
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experimentBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experiment
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
5728 3216 None 29 Human Binding pKd = 9.4 9.4 -1 7
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experimentBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experiment
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
CHEMBL483688 3216 None 29 Human Binding pKd = 9.4 9.4 -1 7
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experimentBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experiment
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
3284 3216 None 29 Human Binding pKd = 9.2 9.2 -1 7
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experimentBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experiment
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
44185871 3216 None 29 Human Binding pKd = 9.2 9.2 -1 7
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experimentBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experiment
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
5728 3216 None 29 Human Binding pKd = 9.2 9.2 -1 7
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experimentBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experiment
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
CHEMBL483688 3216 None 29 Human Binding pKd = 9.2 9.2 -1 7
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experimentBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experiment
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
449 2643 None 38 Human Binding pKd = 9.0 9.0 -1 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
453 2643 None 38 Human Binding pKd = 9.0 9.0 -1 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
6603931 2643 None 38 Human Binding pKd = 9.0 9.0 -1 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
CHEMBL273807 2643 None 38 Human Binding pKd = 9.0 9.0 -1 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
135484064 2616 None 3 Human Binding pKd = 8.8 8.8 21 4
Binding affinity of [3H]-MRE 2029-F20 towards human adenosine A2b receptor expressed in CHO cellsBinding affinity of [3H]-MRE 2029-F20 towards human adenosine A2b receptor expressed in CHO cells
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.03.110
390 2616 None 3 Human Binding pKd = 8.8 8.8 21 4
Binding affinity of [3H]-MRE 2029-F20 towards human adenosine A2b receptor expressed in CHO cellsBinding affinity of [3H]-MRE 2029-F20 towards human adenosine A2b receptor expressed in CHO cells
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.03.110
CHEMBL260331 2616 None 3 Human Binding pKd = 8.8 8.8 21 4
Binding affinity of [3H]-MRE 2029-F20 towards human adenosine A2b receptor expressed in CHO cellsBinding affinity of [3H]-MRE 2029-F20 towards human adenosine A2b receptor expressed in CHO cells
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.03.110
135484064 2616 None 3 Human Binding pKd = 8.8 8.8 21 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm900413e
390 2616 None 3 Human Binding pKd = 8.8 8.8 21 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm900413e
CHEMBL260331 2616 None 3 Human Binding pKd = 8.8 8.8 21 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm900413e
2690 903 None 44 Human Binding pKd = 8 8.0 -30 9
pA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unitypA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unity
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm980094b
384 903 None 44 Human Binding pKd = 8 8.0 -30 9
pA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unitypA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unity
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm980094b
CHEMBL16687 903 None 44 Human Binding pKd = 8 8.0 -30 9
pA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unitypA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unity
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm980094b
10339165 210203 None 0 Human Binding pKd = 8 8.0 -2 4
pA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unitypA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unity
ChEMBL 370 5 2 7 2.9 NCCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
CHEMBL95811 210203 None 0 Human Binding pKd = 8 8.0 -2 4
pA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unitypA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unity
ChEMBL 370 5 2 7 2.9 NCCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
7064 116778 None 63 Human Binding pKd = 4.0 4.0 -70 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 187 1 2 5 0.7 Nc1nc(N)nc(-c2ccccc2)n1 10.1021/acsmedchemlett.2c00099
CHEMBL337319 116778 None 63 Human Binding pKd = 4.0 4.0 -70 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 187 1 2 5 0.7 Nc1nc(N)nc(-c2ccccc2)n1 10.1021/acsmedchemlett.2c00099
554203 191548 None 47 Human Binding pKd = 4.0 4.0 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 177 1 1 4 1.8 Nc1nsc(-c2ccccc2)n1 10.1021/acsmedchemlett.2c00099
CHEMBL5193006 191548 None 47 Human Binding pKd = 4.0 4.0 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 177 1 1 4 1.8 Nc1nsc(-c2ccccc2)n1 10.1021/acsmedchemlett.2c00099
2727447 150525 None 2 Human Binding pKd = 3.9 3.9 -109 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 211 1 1 5 1.4 Nc1ccc2nnc(-c3ccccc3)n2n1 10.1021/acsmedchemlett.2c00099
CHEMBL3954022 150525 None 2 Human Binding pKd = 3.9 3.9 -109 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 211 1 1 5 1.4 Nc1ccc2nnc(-c3ccccc3)n2n1 10.1021/acsmedchemlett.2c00099
CHEMBL4550896 216469 None 2 Human Binding pKd = 3.9 3.9 -3 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL None None None O=C(Nc1ccc2ccccc2n1)c1ccco1 10.1021/acsmedchemlett.2c00099
2774349 33143 None 21 Human Binding pKd = 3.9 3.9 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 202 2 1 4 0.7 Cc1nn(-c2ccccc2)nc1C(N)=O 10.1021/acsmedchemlett.2c00099
CHEMBL1417210 33143 None 21 Human Binding pKd = 3.9 3.9 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 202 2 1 4 0.7 Cc1nn(-c2ccccc2)nc1C(N)=O 10.1021/acsmedchemlett.2c00099
344385 192318 None 37 Human Binding pKd = 3.8 3.8 -7 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 176 0 1 3 0.2 Cn1c(=O)[nH]c2ccccc2c1=O 10.1021/acsmedchemlett.2c00099
CHEMBL5204663 192318 None 37 Human Binding pKd = 3.8 3.8 -7 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 176 0 1 3 0.2 Cn1c(=O)[nH]c2ccccc2c1=O 10.1021/acsmedchemlett.2c00099
2747546 192523 None 7 Human Binding pKd = 4.7 4.7 -2 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 309 3 1 3 3.0 CS(=O)(=O)c1ccc(C(=O)Nc2cccc(Cl)c2)cc1 10.1021/acsmedchemlett.2c00099
CHEMBL5208068 192523 None 7 Human Binding pKd = 4.7 4.7 -2 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 309 3 1 3 3.0 CS(=O)(=O)c1ccc(C(=O)Nc2cccc(Cl)c2)cc1 10.1021/acsmedchemlett.2c00099
16362023 191553 None 2 Human Binding pKd = 3.7 3.7 -3 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 229 3 2 2 2.2 CC(C)NC(=O)c1cc(-c2ccccc2)[nH]n1 10.1021/acsmedchemlett.2c00099
CHEMBL5193059 191553 None 2 Human Binding pKd = 3.7 3.7 -3 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 229 3 2 2 2.2 CC(C)NC(=O)c1cc(-c2ccccc2)[nH]n1 10.1021/acsmedchemlett.2c00099
2314144 50498 None 2 Human Binding pKd = 3.7 3.7 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 251 3 1 4 2.3 O=c1cc(NCc2ccccc2)nc2ccccn12 10.1021/acsmedchemlett.2c00099
CHEMBL1573515 50498 None 2 Human Binding pKd = 3.7 3.7 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 251 3 1 4 2.3 O=c1cc(NCc2ccccc2)nc2ccccn12 10.1021/acsmedchemlett.2c00099
2823411 191689 None 2 Human Binding pKd = 4.7 4.7 4 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 253 3 1 4 2.2 O=C(NCc1ccccc1)c1ccc2nonc2c1 10.1021/acsmedchemlett.2c00099
CHEMBL5195119 191689 None 2 Human Binding pKd = 4.7 4.7 4 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 253 3 1 4 2.2 O=C(NCc1ccccc1)c1ccc2nonc2c1 10.1021/acsmedchemlett.2c00099
9857146 185294 None 1 Human Binding pKd = 6.6 6.6 2 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 289 2 0 3 4.2 Fc1ccc(-c2nn3ccccc3c2-c2ccncc2)cc1 10.1021/acsmedchemlett.2c00099
CHEMBL485745 185294 None 1 Human Binding pKd = 6.6 6.6 2 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 289 2 0 3 4.2 Fc1ccc(-c2nn3ccccc3c2-c2ccncc2)cc1 10.1021/acsmedchemlett.2c00099
135543624 16316 None 25 Human Binding pKd = 5.5 5.5 -16 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccc(O)cc1 10.1021/acsmedchemlett.2c00099
CHEMBL122622 16316 None 25 Human Binding pKd = 5.5 5.5 -16 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccc(O)cc1 10.1021/acsmedchemlett.2c00099
221427 35342 None 23 Human Binding pKd = 4.4 4.4 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 213 2 2 2 2.7 O=C(Nc1ccccc1)Nc1ccccn1 10.1021/acsmedchemlett.2c00099
CHEMBL143703 35342 None 23 Human Binding pKd = 4.4 4.4 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 213 2 2 2 2.7 O=C(Nc1ccccc1)Nc1ccccn1 10.1021/acsmedchemlett.2c00099
2794757 190997 None 31 Human Binding pKd = 4.4 4.4 -2 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 211 1 1 4 2.4 Nc1nsc(-c2ccc(Cl)cc2)n1 10.1021/acsmedchemlett.2c00099
CHEMBL5184937 190997 None 31 Human Binding pKd = 4.4 4.4 -2 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 211 1 1 4 2.4 Nc1nsc(-c2ccc(Cl)cc2)n1 10.1021/acsmedchemlett.2c00099
CHEMBL5080679 217189 None 0 Human Binding pKd = 7.3 7.3 -3 4
Binding affinity to NLuc human A2B adenosine receptor expressed in HEK293-A cells in presence of 1 uM PSB603 by NanoBRET binding assayBinding affinity to NLuc human A2B adenosine receptor expressed in HEK293-A cells in presence of 1 uM PSB603 by NanoBRET binding assay
ChEMBL None None None CCCn1c(=O)c2[nH]c(C34CC5CC(CC(C5)C3)C4)nc2n(CCCNC(=O)c2ccc(C(=O)NCCNC(=O)CCNC(=O)CCCCCNC(=O)COc3ccc(/C=C/C4=[N+]5C(=Cc6ccc(-c7cccs7)n6[B-]5(F)F)C=C4)cc3)cc2)c1=O 10.1021/acs.jmedchem.0c02067
44583036 187061 None 0 Human Binding pKd = 7.2 7.2 7 5
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 400 8 3 7 0.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCCO)cc3)cc2n(C)c1=O 10.1021/jm900413e
CHEMBL490262 187061 None 0 Human Binding pKd = 7.2 7.2 7 5
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 400 8 3 7 0.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCCO)cc3)cc2n(C)c1=O 10.1021/jm900413e
CHEMBL521280 187061 None 0 Human Binding pKd = 7.2 7.2 7 5
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 400 8 3 7 0.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCCO)cc3)cc2n(C)c1=O 10.1021/jm900413e
28561 181478 None 48 Human Binding pKd = 4.2 4.2 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 177 1 1 4 1.8 Nc1nc(-c2ccccc2)ns1 10.1021/acsmedchemlett.2c00099
CHEMBL47633 181478 None 48 Human Binding pKd = 4.2 4.2 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 177 1 1 4 1.8 Nc1nc(-c2ccccc2)ns1 10.1021/acsmedchemlett.2c00099
CHEMBL5075285 216854 None 0 Human Binding pKd = 8.1 8.1 -7 4
Binding affinity to NLuc human A2B adenosine receptor expressed in HEK293-A cells in presence of 1 uM PSB603 by NanoBRET binding assayBinding affinity to NLuc human A2B adenosine receptor expressed in HEK293-A cells in presence of 1 uM PSB603 by NanoBRET binding assay
ChEMBL None None None CCCn1c(=O)c2[nH]c(C34CCC(C(=O)NCCNC(=O)CCNC(=O)CCNC(=O)CCCCCNC(=O)COc5ccc(/C=C/C6=[N+]7C(=Cc8ccc(-c9cccs9)n8[B-]7(F)F)C=C6)cc5)(CC3)CC4)nc2n(CCC)c1=O 10.1021/acs.jmedchem.0c02067
17457984 191829 None 3 Human Binding pKd = 4.1 4.1 -2 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 284 4 1 5 2.5 CC(C)n1ncc2cc(C(=O)NCc3ccco3)cnc21 10.1021/acsmedchemlett.2c00099
CHEMBL5197070 191829 None 3 Human Binding pKd = 4.1 4.1 -2 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 284 4 1 5 2.5 CC(C)n1ncc2cc(C(=O)NCc3ccco3)cnc21 10.1021/acsmedchemlett.2c00099
136 3292 None 26 Rat Binding pKd = 7.0 7.0 -26 18
Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00360a008
223 3292 None 26 Rat Binding pKd = 7.0 7.0 -26 18
Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00360a008
643606 3292 None 26 Rat Binding pKd = 7.0 7.0 -26 18
Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00360a008
CHEMBL10347 3292 None 26 Rat Binding pKd = 7.0 7.0 -26 18
Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00360a008
155555721 174497 None 11 Human Binding pKi = 10.1 10.1 1 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 572 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Br)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4552275 174497 None 11 Human Binding pKi = 10.1 10.1 1 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 572 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Br)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155555721 174497 None 11 Mouse Binding pKi = 9.9 9.9 -1 2
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 572 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Br)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4552275 174497 None 11 Mouse Binding pKi = 9.9 9.9 -1 2
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 572 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Br)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155521543 170713 None 0 Human Binding pKi = 9.9 9.9 645 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 572 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5Br)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4450864 170713 None 0 Human Binding pKi = 9.9 9.9 645 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 572 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5Br)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155530514 171651 None 0 Human Binding pKi = 9.8 9.8 6 5
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 586 7 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Br)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4464522 171651 None 0 Human Binding pKi = 9.8 9.8 6 5
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 586 7 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Br)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155550159 174007 None 0 Human Binding pKi = 9.8 9.8 501 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 586 7 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Br)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4540206 174007 None 0 Human Binding pKi = 9.8 9.8 501 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 586 7 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Br)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44186666 185764 None 0 Human Binding pKi = 9.8 9.8 144 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 562 6 2 7 2.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL486478 185764 None 0 Human Binding pKi = 9.8 9.8 144 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 562 6 2 7 2.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
155524032 170993 None 0 Human Binding pKi = 9.8 9.8 19054 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 620 6 2 7 2.6 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(I)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4454481 170993 None 0 Human Binding pKi = 9.8 9.8 19054 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 620 6 2 7 2.6 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(I)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
76328910 105577 None 0 Human Binding pKi = 9.8 9.8 -1 4
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 522 8 1 8 2.9 Cn1c(=O)c2[nH]c(-c3ccc(OCCCN4CCN(Cc5ccccc5Cl)CC4)cc3)nc2n(C)c1=O 10.1016/j.ejmech.2014.01.045
CHEMBL3121728 105577 None 0 Human Binding pKi = 9.8 9.8 -1 4
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 522 8 1 8 2.9 Cn1c(=O)c2[nH]c(-c3ccc(OCCCN4CCN(Cc5ccccc5Cl)CC4)cc3)nc2n(C)c1=O 10.1016/j.ejmech.2014.01.045
145977111 163860 None 0 Rat Binding pKi = 9.7 9.7 7 4
Displacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 617 9 3 7 3.9 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4205635 163860 None 0 Rat Binding pKi = 9.7 9.7 7 4
Displacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 617 9 3 7 3.9 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
44186580 184312 None 0 Human Binding pKi = 9.7 9.7 30 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL483261 184312 None 0 Human Binding pKi = 9.7 9.7 30 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
155529872 171609 None 0 Human Binding pKi = 9.7 9.7 165 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 558 7 2 8 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)c(OC)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4463929 171609 None 0 Human Binding pKi = 9.7 9.7 165 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 558 7 2 8 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)c(OC)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155532274 171800 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 572 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5cccc(Br)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4466625 171800 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 572 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5cccc(Br)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155560510 175152 None 0 Human Binding pKi = 9.6 9.6 851 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 549 8 2 8 2.9 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(N=[N+]=[N-])cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4567785 175152 None 0 Human Binding pKi = 9.6 9.6 851 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 549 8 2 8 2.9 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(N=[N+]=[N-])cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44186668 191619 None 0 Human Binding pKi = 9.6 9.6 245 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 562 6 2 7 2.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL519390 191619 None 0 Human Binding pKi = 9.6 9.6 245 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 562 6 2 7 2.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44186667 185765 None 0 Human Binding pKi = 9.5 9.5 478 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL486479 185765 None 0 Human Binding pKi = 9.5 9.5 478 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
155528136 171360 None 0 Human Binding pKi = 9.5 9.5 158 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4460114 171360 None 0 Human Binding pKi = 9.5 9.5 158 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155545762 173583 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 558 7 2 8 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(OC)c(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4530074 173583 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 558 7 2 8 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(OC)c(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44186581 3205 None 21 Human Binding pKi = 9.4 9.4 851 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl 10.1021/jm900413e
6561 3205 None 21 Human Binding pKi = 9.4 9.4 851 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl 10.1021/jm900413e
CHEMBL482436 3205 None 21 Human Binding pKi = 9.4 9.4 851 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl 10.1021/jm900413e
155514860 169984 None 0 Human Binding pKi = 9.4 9.4 478 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 522 7 2 7 2.3 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4440526 169984 None 0 Human Binding pKi = 9.4 9.4 478 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 522 7 2 7 2.3 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
450 2970 None 7 Human Binding pKi = 9.4 9.4 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm201292w
454 2970 None 7 Human Binding pKi = 9.4 9.4 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm201292w
5311041 2970 None 7 Human Binding pKi = 9.4 9.4 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm201292w
CHEMBL485862 2970 None 7 Human Binding pKi = 9.4 9.4 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm201292w
155514957 170030 None 0 Human Binding pKi = 9.4 9.4 501 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5Cl)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4441276 170030 None 0 Human Binding pKi = 9.4 9.4 501 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5Cl)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44185870 184336 None 0 Human Binding pKi = 9.4 9.4 117 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 514 5 2 7 2.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL483487 184336 None 0 Human Binding pKi = 9.4 9.4 117 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 514 5 2 7 2.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
450 2970 None 7 Human Binding pKi = 9.4 9.4 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm900413e
454 2970 None 7 Human Binding pKi = 9.4 9.4 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm900413e
5311041 2970 None 7 Human Binding pKi = 9.4 9.4 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm900413e
CHEMBL485862 2970 None 7 Human Binding pKi = 9.4 9.4 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm900413e
155523968 170990 None 0 Human Binding pKi = 9.4 9.4 97 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 544 6 3 8 2.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)c(O)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4454417 170990 None 0 Human Binding pKi = 9.4 9.4 97 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 544 6 3 8 2.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)c(O)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155516277 170167 None 0 Human Binding pKi = 9.4 9.4 331 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 508 6 2 7 2.3 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5C)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4443090 170167 None 0 Human Binding pKi = 9.4 9.4 331 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 508 6 2 7 2.3 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5C)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44186626 184715 None 0 Human Binding pKi = 9.4 9.4 245 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 526 7 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL484900 184715 None 0 Human Binding pKi = 9.4 9.4 245 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 526 7 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44185872 191507 None 0 Human Binding pKi = 9.3 9.3 416 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 524 5 2 7 1.9 C#CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL519253 191507 None 0 Human Binding pKi = 9.3 9.3 416 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 524 5 2 7 1.9 C#CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
155561141 175078 None 0 Human Binding pKi = 9.3 9.3 676 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 604 7 2 7 2.9 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Br)c(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4566170 175078 None 0 Human Binding pKi = 9.3 9.3 676 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 604 7 2 7 2.9 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Br)c(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
450 2970 None 7 Human Binding pKi = 9.3 9.3 257 4
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01431
454 2970 None 7 Human Binding pKi = 9.3 9.3 257 4
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01431
5311041 2970 None 7 Human Binding pKi = 9.3 9.3 257 4
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01431
CHEMBL485862 2970 None 7 Human Binding pKi = 9.3 9.3 257 4
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01431
450 2970 None 7 Human Binding pKi = 9.3 9.3 257 4
Binding affinity to human recombinant A2B receptor expressed in HEK293 cell membranesBinding affinity to human recombinant A2B receptor expressed in HEK293 cell membranes
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01340
454 2970 None 7 Human Binding pKi = 9.3 9.3 257 4
Binding affinity to human recombinant A2B receptor expressed in HEK293 cell membranesBinding affinity to human recombinant A2B receptor expressed in HEK293 cell membranes
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01340
5311041 2970 None 7 Human Binding pKi = 9.3 9.3 257 4
Binding affinity to human recombinant A2B receptor expressed in HEK293 cell membranesBinding affinity to human recombinant A2B receptor expressed in HEK293 cell membranes
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01340
CHEMBL485862 2970 None 7 Human Binding pKi = 9.3 9.3 257 4
Binding affinity to human recombinant A2B receptor expressed in HEK293 cell membranesBinding affinity to human recombinant A2B receptor expressed in HEK293 cell membranes
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01340
127033645 139207 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [3H]OSIP339391 from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]OSIP339391 from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 526 10 3 7 3.0 CC(=O)NCCNc1nc(-c2ccccc2)nc2nc(C(=O)N3CCN(CCCc4ccccc4)CC3)[nH]c12 10.1021/acs.jmedchem.5b01586
CHEMBL3786849 139207 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [3H]OSIP339391 from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]OSIP339391 from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 526 10 3 7 3.0 CC(=O)NCCNc1nc(-c2ccccc2)nc2nc(C(=O)N3CCN(CCCc4ccccc4)CC3)[nH]c12 10.1021/acs.jmedchem.5b01586
127033645 139207 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [3H]OSIP339391 from human recombinant adenosine A2B receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]OSIP339391 from human recombinant adenosine A2B receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 526 10 3 7 3.0 CC(=O)NCCNc1nc(-c2ccccc2)nc2nc(C(=O)N3CCN(CCCc4ccccc4)CC3)[nH]c12 10.1021/acs.jmedchem.7b00138
CHEMBL3786849 139207 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [3H]OSIP339391 from human recombinant adenosine A2B receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]OSIP339391 from human recombinant adenosine A2B receptor expressed in HEK293