Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Unit Assay Type Assay Description Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles
CHEMBL122806 aa2br_human Human No 8.0 EC50 = 10 nM Funct
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
348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1cccc(O)c1
CHEMBL122806 aa2br_human Human No 8.0 EC50 = 10 nM Funct
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1cccc(O)c1
CHEMBL388193 aa2br_human Human No 8.0 EC50 = 10.5 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL186113 aa2br_human Human Yes 6.0 EC50 = 1000 nM Funct
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
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
CHEMBL1688378 aa2br_human Human No 5.0 EC50 = 10000 nM Funct
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
333 3 3 8 0.9 CCCCC#Cc1nc(N)c2ncn([C@@H]3SC[C@@H](O)[C@H]3O)c2n1
CHEMBL317052 aa2br_human Human Yes 5.0 EC50 = 10000 nM Funct
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
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
CHEMBL1950553 aa2br_human Human Yes 5.0 EC50 = 10000 nM Funct
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
421 6 4 10 0.3 Nc1nc(OCCc2ccc(Cl)cc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
CHEMBL260563 aa2br_human Human Yes 4.0 EC50 = 100000 nM Bind
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
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
CHEMBL261623 aa2br_human Human No 4.0 EC50 = 100000 nM Bind
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
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
CHEMBL319387 aa2br_human Human Yes 4.0 EC50 = 100000 nM Bind
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
347 4 4 9 -0.4 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1
CHEMBL410115 aa2br_human Human No 4.0 EC50 = 100000 nM Bind
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
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
CHEMBL437842 aa2br_human Human No 4.0 EC50 = 100000 nM Bind
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
375 6 4 9 0.4 CCCCC#Cc1nc(NCC)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1
CHEMBL574597 aa2br_human Human Yes 4.0 EC50 = 100000 nM Bind
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
381 3 4 9 -0.1 CNc1nc(C#Cc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
CHEMBL3414942 aa2br_human Human No 6.0 EC50 = 1010 nM Funct
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
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
CHEMBL464859 aa2br_human Human Yes 7.0 EC50 = 104 nM Funct
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL225579 aa2br_human Human No 7.0 EC50 = 107 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL225459 aa2br_human Human No 7.0 EC50 = 109 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
504 6 5 10 0.9 C1=CC2=C(C=C1Br)NC=C2CCOC3=NC(=C4C(=N3)N(C=N4)[C@H]5[C@@H]([C@@H]([C@H](O5)CO)O)O)N
CHEMBL4210592 aa2br_human Human No 7.9 EC50 = 11.7 nM Funct
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
376 6 2 7 3.5 CCOc1ccc(-c2c(C#N)c(N)nc(SCc3ncc[nH]3)c2C#N)cc1
CHEMBL464859 aa2br_human Human Yes 7.0 EC50 = 110 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL4097468 aa2br_human Human No 6.0 EC50 = 1100 nM Funct
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
441 6 3 12 0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL2094083 aa2br_human Human No 6.0 EC50 = 1100 nM Bind
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
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
CHEMBL119709 aa2br_human Human Yes 5.0 EC50 = 11000 nM Funct
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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL3414947 aa2br_human Human No 6.0 EC50 = 1110 nM Funct
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
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
CHEMBL360837 aa2br_human Human No 5.9 EC50 = 1140 nM Funct
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
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
CHEMBL3414941 aa2br_human Human No 5.9 EC50 = 1150 nM Funct
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
407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL4756472 aa2br_human Human No 6.9 EC50 = 117.5 nM Funct
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
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
CHEMBL2042305 aa2br_human Human No 5.9 EC50 = 1173 nM Funct
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
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
CHEMBL122622 aa2br_human Human Yes 7.9 EC50 = 12 nM Funct
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccc(O)cc1
CHEMBL437168 aa2br_human Human No 7.9 EC50 = 12.3 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL4214347 aa2br_human Human No 7.9 EC50 = 12.7 nM Funct
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
455 8 2 7 4.3 N#Cc1c(N)nc(SCc2cccc(C(N)=O)c2)c(C#N)c1-c1ccc(OCC2CC2)cc1
CHEMBL2042311 aa2br_human Human No 6.9 EC50 = 120 nM Funct
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
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
CHEMBL186403 aa2br_human Human No 5.9 EC50 = 1200 nM Funct
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
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
CHEMBL2042310 aa2br_human Human No 4.9 EC50 = 12160 nM Funct
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
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
CHEMBL3133160 aa2br_human Human No 6.9 EC50 = 125.9 nM Funct
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
399 5 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O
CHEMBL374028 aa2br_human Human No 5.9 EC50 = 1250 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL3133156 aa2br_human Human No 5.9 EC50 = 1258.9 nM Funct
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
365 6 5 10 -1.0 CCCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O
CHEMBL2042299 aa2br_human Human No 6.9 EC50 = 126 nM Funct
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
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
CHEMBL225459 aa2br_human Human No 6.9 EC50 = 128 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
504 6 5 10 0.9 C1=CC2=C(C=C1Br)NC=C2CCOC3=NC(=C4C(=N3)N(C=N4)[C@H]5[C@@H]([C@@H]([C@H](O5)CO)O)O)N
CHEMBL4079464 aa2br_human Human No 4.9 EC50 = 12800 nM Funct
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
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
CHEMBL4102750 aa2br_human Human No 5.9 EC50 = 1290 nM Funct
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
475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL186113 aa2br_human Human Yes 5.9 EC50 = 1300 nM Funct
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL360837 aa2br_human Human No 5.9 EC50 = 1300 nM Funct
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
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
CHEMBL361925 aa2br_human Human No 5.9 EC50 = 1300 nM Funct
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
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
CHEMBL2113421 aa2br_human Human No 4.9 EC50 = 13000 nM Funct
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
336 3 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=S)NC2CC2)[C@@H](O)[C@H]1O
CHEMBL3414944 aa2br_human Human No 5.9 EC50 = 1340 nM Funct
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
403 5 3 13 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL4208189 aa2br_human Human No 6.9 EC50 = 139 nM Funct
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
402 7 2 7 3.9 N#Cc1c(N)nc(SCc2cnc[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1
CHEMBL2042304 aa2br_human Human No 7.9 EC50 = 14 nM Funct
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
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
CHEMBL464859 aa2br_human Human Yes 6.9 EC50 = 140 nM Bind
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based assay
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL464859 aa2br_human Human Yes 6.9 EC50 = 140 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL261546 aa2br_human Human No 6.8 EC50 = 143 nM Funct
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
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
CHEMBL374760 aa2br_human Human Yes 5.8 EC50 = 1440 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
437 6 4 10 0.8 Nc1nc(OCCc2ccc3ccccc3c2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
CHEMBL2042298 aa2br_human Human Yes 6.8 EC50 = 145 nM Funct
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
427 7 5 10 -0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O
CHEMBL4105473 aa2br_human Human No 6.8 EC50 = 147.9 nM Funct
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
800 15 5 12 6.5 C1=CC=C(C=C1)C(=O)C2=CSC(=C2C3=CC(=CC=C3)C(F)(F)F)C4=CC=C(C=C4)C(=O)NCCCCCCNC5=C6C(=NC=N5)N(C=N6)[C@H]7[C@@H]([C@@H]([C@H](O7)CO)O)O
CHEMBL464859 aa2br_human Human Yes 4.8 EC50 = 14791.1 nM Bind
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL3414938 aa2br_human Human No 5.8 EC50 = 1480 nM Funct
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
347 4 3 12 -1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL2042301 aa2br_human Human No 5.8 EC50 = 1489 nM Funct
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
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
CHEMBL1090123 aa2br_human Human Yes 4.8 EC50 = 14900 nM Funct
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
248 2 1 8 1.1 CSc1nc(N)n2nc(-c3ccco3)nc2n1
CHEMBL226194 aa2br_human Human No 7.8 EC50 = 15.2 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL464859 aa2br_human Human Yes 7.8 EC50 = 15.9 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL375501 aa2br_human Human No 6.8 EC50 = 150 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL464859 aa2br_human Human Yes 5.8 EC50 = 1510 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL464859 aa2br_human Human Yes 6.8 EC50 = 155 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL4078771 aa2br_human Human No 6.8 EC50 = 158.5 nM Funct
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
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
CHEMBL3133078 aa2br_human Human No 6.8 EC50 = 158.5 nM Funct
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
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
CHEMBL3133079 aa2br_human Human No 6.8 EC50 = 158.5 nM Funct
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
413 6 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O
CHEMBL3133153 aa2br_human Human No 5.8 EC50 = 1584.9 nM Funct
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
323 3 5 10 -2.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(N)nc32)[C@H](O)[C@@H]1O
CHEMBL3133154 aa2br_human Human No 5.8 EC50 = 1584.9 nM Funct
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
337 4 5 10 -1.8 CCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O
CHEMBL388405 aa2br_human Human No 7.8 EC50 = 16.4 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL4168653 aa2br_human Human Yes 7.8 EC50 = 17.0 nM Funct
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
302 5 1 7 0.0 O=C(CN1CCOC(Cn2cncn2)C1)Nc1cccnc1
CHEMBL464859 aa2br_human Human Yes 6.8 EC50 = 160 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL2113431 aa2br_human Human No 4.8 EC50 = 16000 nM Funct
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
324 3 4 9 -1.0 CCNC(=S)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O
CHEMBL4207286 aa2br_human Human No 6.8 EC50 = 164 nM Funct
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
366 5 3 7 1.6 CC(=O)Nc1ccc(-c2c(C#N)c(N)nc(SCC(N)=O)c2C#N)cc1
CHEMBL4059961 aa2br_human Human No 5.8 EC50 = 1650 nM Funct
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
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
CHEMBL139000 aa2br_human Human Yes 5.8 EC50 = 1680 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C
CHEMBL1092869 aa2br_human Human No 4.8 EC50 = 16800 nM Funct
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
381 4 2 8 3.5 CSc1nc(NC(=O)Nc2ccc(C)cc2)n2nc(-c3ccco3)nc2n1
CHEMBL487754 aa2br_human Human No 4.8 EC50 = 16850 nM Funct
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
410 5 4 9 0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@H](O)[C@@H]1O
CHEMBL4086624 aa2br_human Human No 7.8 EC50 = 17.8 nM Funct
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
552 12 5 11 2.6 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cccs2)c1
CHEMBL2092788 aa2br_human Human Yes 5.8 EC50 = 1700 nM Bind
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
425 5 5 10 -0.0 CCNc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
CHEMBL1092868 aa2br_human Human No 4.8 EC50 = 17100 nM Funct
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
367 4 2 8 3.1 CSc1nc(NC(=O)Nc2ccccc2)n2nc(-c3ccco3)nc2n1
CHEMBL410104 aa2br_human Human No 6.8 EC50 = 174 nM Funct
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
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
CHEMBL218585 aa2br_human Human No 6.8 EC50 = 175 nM Funct
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
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
CHEMBL225944 aa2br_human Human No 6.8 EC50 = 175 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL225233 aa2br_human Human No 5.8 EC50 = 1780 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
393 6 4 11 -0.3 Nc1nc(OCCc2cccs2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
CHEMBL4077152 aa2br_human Human No 7.7 EC50 = 18.6 nM Funct
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
849 15 6 13 6.7 C1=CC=C(C=C1)C(=O)C2=C(SC(=C2C3=CC(=CC=C3)C(F)(F)F)C4=CC=C(C=C4)C(=O)NCCCCCCNC5=C6C(=NC(=N5)Cl)N(C=N6)[C@H]7[C@@H]([C@@H]([C@H](O7)CO)O)O)N
CHEMBL4218613 aa2br_human Human No 6.7 EC50 = 182 nM Funct
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
409 8 3 8 2.0 N#Cc1c(N)nc(SCC(=O)NCO)c(C#N)c1-c1ccc(OCC2CC2)cc1
CHEMBL222748 aa2br_human Human No 5.7 EC50 = 1870 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL124345 aa2br_human Human No 7.7 EC50 = 19 nM Funct
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
332 4 2 6 3.1 C1=CC=C(C=C1)C2=C(C(=NC(=C2C#N)SCC3=NC=CN3)N)C#N
CHEMBL4076003 aa2br_human Human No 5.7 EC50 = 1930 nM Funct
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
413 6 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL4105164 aa2br_human Human No 5.7 EC50 = 1961 nM Funct
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
421 6 3 12 0.3 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL3133080 aa2br_human Human No 6.7 EC50 = 199.5 nM Funct
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
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
CHEMBL3133157 aa2br_human Human No 6.7 EC50 = 199.5 nM Funct
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
363 4 5 10 -1.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCC4)nc(N)nc32)[C@H](O)[C@@H]1O
CHEMBL2042297 aa2br_human Human No 8.6 EC50 = 2.3 nM Funct
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
326 3 4 9 -1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(F)nc32)[C@H](O)[C@@H]1O
CHEMBL425643 aa2br_human Human No 6.7 EC50 = 200 nM Funct
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
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
CHEMBL2096798 aa2br_human Human No 5.7 EC50 = 2000 nM Funct
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
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
CHEMBL4103712 aa2br_human Human No 4.7 EC50 = 20000 nM Funct
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
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
CHEMBL1089441 aa2br_human Human No 4.7 EC50 = 20000 nM Funct
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
427 5 2 8 4.5 Cc1ccc(NC(=O)Nc2nc(Oc3ccccc3)nc3nc(-c4ccco4)nn23)cc1
CHEMBL414055 aa2br_human Human No 5.7 EC50 = 2041.7 nM Funct
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
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
CHEMBL219413 aa2br_human Human No 6.7 EC50 = 210 nM Funct
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
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
CHEMBL4205729 aa2br_human Human No 6.7 EC50 = 211 nM Funct
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
367 6 2 7 2.3 CCOc1ccc(-c2c(C#N)c(N)nc(SCC(=O)NC)c2C#N)cc1
CHEMBL4076561 aa2br_human Human No 5.7 EC50 = 2140 nM Funct
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
463 6 3 13 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL222907 aa2br_human Human No 6.7 EC50 = 216 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL222442 aa2br_human Human No 5.7 EC50 = 2180 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL224874 aa2br_human Human No 6.7 EC50 = 220 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL224874 aa2br_human Human No 6.7 EC50 = 220 nM Bind
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
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
CHEMBL3414940 aa2br_human Human No 6.7 EC50 = 222 nM Funct
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
373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL4076495 aa2br_human Human No 6.7 EC50 = 223.9 nM Funct
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
671 14 6 13 3.4 C1=CC=C(C=C1)C(=O)C2=C(SC(=C2)C3=CC=C(C=C3)C(=O)NCCCCCCNC4=C5C(=NC=N4)N(C=N5)[C@H]6[C@@H]([C@@H]([C@H](O6)CO)O)O)N
CHEMBL4746617 aa2br_human Human No 6.7 EC50 = 223.9 nM Funct
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
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
CHEMBL4079433 aa2br_human Human No 5.7 EC50 = 2230 nM Funct
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
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
CHEMBL411332 aa2br_human Human No 6.6 EC50 = 227 nM Funct
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
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
CHEMBL2042308 aa2br_human Human No 5.6 EC50 = 2279 nM Funct
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
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
CHEMBL273807 aa2br_human Human Yes 7.6 EC50 = 23.4 nM Funct
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
486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N
CHEMBL4165135 aa2br_human Human Yes 7.6 EC50 = 23.4 nM Funct
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
322 6 2 7 2.6 CCCc1cc(O)nc(SC(C)C(=O)Nc2cc(C)no2)n1
CHEMBL4078479 aa2br_human Human No 6.6 EC50 = 235 nM Funct
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
549 6 3 12 1.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(I)c5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL477 aa2br_human Human Yes 4.6 EC50 = 23500 nM Funct
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
267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL4098377 aa2br_human Human No 5.6 EC50 = 2390 nM Funct
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
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
CHEMBL226304 aa2br_human Human No 6.6 EC50 = 240 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL464859 aa2br_human Human Yes 5.6 EC50 = 2400 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL2092941 aa2br_human Human Yes 5.6 EC50 = 2400 nM Bind
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
397 3 5 10 -0.9 Nc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
CHEMBL258534 aa2br_human Human No 5.6 EC50 = 2400 nM Bind
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
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
CHEMBL477 aa2br_human Human Yes 4.6 EC50 = 24000 nM Bind
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL477 aa2br_human Human Yes 4.6 EC50 = 24000 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cellsAgonist activity at human adenosine A2B receptor expressed in CHO cells
267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL477 aa2br_human Human Yes 4.6 EC50 = 24000 nM Funct
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
267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL477 aa2br_human Human Yes 4.6 EC50 = 24000 nM Funct
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL464859 aa2br_human Human Yes 6.6 EC50 = 250 nM Funct
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL3133159 aa2br_human Human No 5.6 EC50 = 2511.9 nM Funct
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
391 4 5 10 -0.5 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCCC4)nc(N)nc32)[C@H](O)[C@@H]1O
CHEMBL2042306 aa2br_human Human No 6.6 EC50 = 257 nM Funct
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
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
CHEMBL4086325 aa2br_human Human No 5.6 EC50 = 2570 nM Funct
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
447 6 3 13 0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL222945 aa2br_human Human No 5.6 EC50 = 2580 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
376 6 5 10 -1.0 Nc1nc(OCCc2cc[nH]c2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
CHEMBL261453 aa2br_human Human No 5.6 EC50 = 2600 nM Bind
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
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
CHEMBL2092786 aa2br_human Human No 5.6 EC50 = 2700 nM Bind
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
411 4 5 10 -0.4 CNc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
CHEMBL219411 aa2br_human Human No 6.6 EC50 = 273 nM Funct
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
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
CHEMBL4072009 aa2br_human Human No 6.5 EC50 = 288.4 nM Funct
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
815 15 6 13 6.1 C1=CC=C(C=C1)C(=O)C2=C(SC(=C2C3=CC(=CC=C3)C(F)(F)F)C4=CC=CC=C4C(=O)NCCCCCCNC5=C6C(=NC=N5)N(C=N6)[C@H]7[C@@H]([C@@H]([C@H](O7)CO)O)O)N
CHEMBL429684 aa2br_human Human No 6.5 EC50 = 289 nM Funct
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
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
CHEMBL1235128 aa2br_human Human Yes 4.5 EC50 = 29000 nM Funct
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
322 4 4 9 -1.4 CCCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O
CHEMBL2042307 aa2br_human Human No 6.5 EC50 = 296 nM Funct
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
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
CHEMBL223366 aa2br_human Human No 6.5 EC50 = 299 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
426 6 5 10 0.1 C1=CC=C2C(=C1)C(=CN2)CCOC3=NC(=C4C(=N3)N(C=N4)[C@H]5[C@@H]([C@@H]([C@H](O5)CO)O)O)N
CHEMBL464859 aa2br_human Human Yes 8.5 EC50 = 3.2 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL226242 aa2br_human Human No 7.5 EC50 = 30.2 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL226303 aa2br_human Human No 6.5 EC50 = 300 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL2096798 aa2br_human Human No 5.5 EC50 = 3000 nM Funct
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
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
CHEMBL2113435 aa2br_human Human No 4.5 EC50 = 30000 nM Funct
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
376 4 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCC(F)(F)F)[C@@H](O)[C@H]1O
CHEMBL388505 aa2br_human Human No 6.5 EC50 = 302 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL4202825 aa2br_human Human Yes 7.5 EC50 = 31 nM Funct
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
379 7 2 7 2.4 N#Cc1c(N)nc(c(c1c1ccc(cc1)OCC1CC1)C#N)SCC(=O)N
CHEMBL119709 aa2br_human Human Yes 7.5 EC50 = 31.6 nM Funct
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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL464859 aa2br_human Human Yes 5.5 EC50 = 3100 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL226307 aa2br_human Human No 6.5 EC50 = 315 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL3414945 aa2br_human Human No 5.5 EC50 = 3150 nM Funct
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
437 5 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL464859 aa2br_human Human Yes 6.5 EC50 = 316.2 nM Bind
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL388406 aa2br_human Human No 7.5 EC50 = 32.3 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL226243 aa2br_human Human No 7.5 EC50 = 32.4 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL2070399 aa2br_human Human No 4.5 EC50 = 32000 nM Funct
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
342 4 4 9 -1.6 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCCl)[C@@H](O)[C@H]1O
CHEMBL261515 aa2br_human Human No 5.5 EC50 = 3270 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
454 8 5 10 1.0 CCNc1nc(OCCc2c[nH]c3ccccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
CHEMBL464859 aa2br_human Human Yes 6.5 EC50 = 330 nM Funct
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL2070507 aa2br_human Human No 4.5 EC50 = 33000 nM Funct
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
334 3 4 9 -1.3 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CCC2)[C@@H](O)[C@H]1O
CHEMBL4210096 aa2br_human Human No 6.5 EC50 = 332 nM Funct
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
376 6 2 7 3.5 CCOc1ccc(-c2c(C#N)c(N)nc(SCc3ccn[nH]3)c2C#N)cc1
CHEMBL3827331 aa2br_human Human No 6.5 EC50 = 335 nM Funct
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)
538 15 0 9 4.1 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCCN(CC)CC)cc2)n(CCCC)c1=O
CHEMBL1090124 aa2br_human Human No 4.5 EC50 = 33700 nM Funct
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
245 2 1 8 0.4 CN(C)c1nc(N)n2nc(-c3ccco3)nc2n1
CHEMBL125979 aa2br_human Human No 7.5 EC50 = 34 nM Funct
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
362 5 2 7 3.1 COc1cccc(-c2c(C#N)c(N)nc(SCc3ncc[nH]3)c2C#N)c1
CHEMBL4163380 aa2br_human Human Yes 7.5 EC50 = 34.7 nM Funct
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
311 4 2 6 2.4 Cc1cc(NC(=O)CNc2ccc3c(c2)OC(F)(F)O3)on1
CHEMBL4167064 aa2br_human Human Yes 7.5 EC50 = 34.7 nM Funct
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
319 6 1 7 1.6 CC(C)c1noc(OCC(=O)NCc2ccc3c(c2)OCO3)n1
CHEMBL409483 aa2br_human Human No 6.5 EC50 = 340 nM Funct
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
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
CHEMBL1093313 aa2br_human Human Yes 5.5 EC50 = 3420 nM Funct
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
294 3 1 8 2.2 Nc1nc(Oc2ccccc2)nc2nc(-c3ccco3)nn12
CHEMBL4210852 aa2br_human Human No 6.5 EC50 = 347 nM Funct
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
470 8 1 8 4.9 COC(=O)c1cccc(CSc2nc(N)c(C#N)c(-c3ccc(OCC4CC4)cc3)c2C#N)c1
CHEMBL3414936 aa2br_human Human No 6.5 EC50 = 347 nM Funct
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
333 3 3 12 -1.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL374685 aa2br_human Human Yes 5.5 EC50 = 3490 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
387 6 4 10 -0.4 Nc1nc(OCCc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
CHEMBL4101850 aa2br_human Human No 7.5 EC50 = 35.5 nM Funct
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
815 15 6 13 6.1 C1=CC=C(C=C1)C(=O)C2=C(SC(=C2C3=CC(=CC=C3)C(F)(F)F)C4=CC(=CC=C4)C(=O)NCCCCCCNC5=C6C(=NC=N5)N(C=N6)[C@H]7[C@@H]([C@@H]([C@H](O7)CO)O)O)N
CHEMBL388194 aa2br_human Human No 7.5 EC50 = 35.5 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL3414939 aa2br_human Human No 5.5 EC50 = 3510 nM Funct
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
381 4 3 12 -0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL2042300 aa2br_human Human No 6.5 EC50 = 355 nM Funct
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
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
CHEMBL218989 aa2br_human Human No 6.5 EC50 = 359 nM Funct
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
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
CHEMBL226305 aa2br_human Human No 6.4 EC50 = 360 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL464859 aa2br_human Human Yes 5.4 EC50 = 3630.8 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL222194 aa2br_human Human No 6.4 EC50 = 365 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL219361 aa2br_human Human No 6.4 EC50 = 369 nM Funct
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
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
CHEMBL606095 aa2br_human Human No 4.4 EC50 = 37000 nM Funct
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
322 3 4 9 -1.4 CC(C)NC(=O)[C@H]1OC(n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O
CHEMBL4098408 aa2br_human Human No 5.4 EC50 = 3740 nM Funct
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
413 4 3 8 2.2 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(Nc4ccc(Cl)cc4F)ncnc32)[C@@H]1O
CHEMBL4206762 aa2br_human Human No 7.4 EC50 = 38 nM Funct
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
353 6 2 7 2.1 CCOc1ccc(-c2c(C#N)c(N)nc(SCC(N)=O)c2C#N)cc1
CHEMBL464859 aa2br_human Human Yes 7.4 EC50 = 38 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL3416810 aa2br_human Human No 6.4 EC50 = 389 nM Funct
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
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
CHEMBL331372 aa2br_human Human Yes 7.4 EC50 = 39.8 nM Funct
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
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
CHEMBL3133161 aa2br_human Human No 6.4 EC50 = 398.1 nM Funct
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
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
CHEMBL2042309 aa2br_human Human No 4.4 EC50 = 40310 nM Funct
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
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
CHEMBL4081876 aa2br_human Human No 6.4 EC50 = 408 nM Funct
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
501 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL226356 aa2br_human Human No 7.4 EC50 = 42.6 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL464859 aa2br_human Human Yes 7.4 EC50 = 42.7 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL1090806 aa2br_human Human No 4.4 EC50 = 42400 nM Funct
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
396 6 1 9 2.7 COc1ccc(CC(=O)Nc2nc(SC)nc3nc(-c4ccco4)nn23)cc1
CHEMBL464859 aa2br_human Human Yes 6.4 EC50 = 440 nM Funct
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL4081224 aa2br_human Human No 6.4 EC50 = 446.7 nM Funct
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
711 13 6 12 4.8 C1=CC(=CC(=C1)C(F)(F)F)C2=C(SC(=C2)N)C3=CC=C(C=C3)C(=O)NCCCCCCNC4=C5C(=NC=N4)N(C=N5)[C@H]6[C@@H]([C@@H]([C@H](O6)CO)O)O
CHEMBL226244 aa2br_human Human No 7.3 EC50 = 45.4 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL218988 aa2br_human Human No 6.4 EC50 = 450 nM Funct
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
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
CHEMBL519809 aa2br_human Human Yes 4.4 EC50 = 45000 nM Funct
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
294 2 4 9 -2.2 CNC(=O)[C@@H]1[C@H]([C@H]([C@@H](O1)N2C=NC3=C(N=CN=C32)N)O)O
CHEMBL2113434 aa2br_human Human Yes 4.4 EC50 = 45000 nM Funct
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
310 3 4 10 -2.3 CONC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O
CHEMBL4173768 aa2br_human Human Yes 7.3 EC50 = 46.8 nM Funct
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
344 5 2 8 0.6 CC(OC(=O)c1nccnc1N)C(=O)NCc1ccc2c(c1)OCO2
CHEMBL4075186 aa2br_human Human No 6.3 EC50 = 467.7 nM Funct
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
829 16 6 13 6.5 C1=CC=C(C=C1)C(=O)C2=C(SC(=C2C3=CC(=CC=C3)C(F)(F)F)C4=CC=C(C=C4)C(=O)NCCCCCCCNC5=C6C(=NC=N5)N(C=N6)[C@H]7[C@@H]([C@@H]([C@H](O7)CO)O)O)N
CHEMBL360646 aa2br_human Human No 5.3 EC50 = 4700 nM Funct
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
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
CHEMBL193692 aa2br_human Human Yes 6.3 EC50 = 485 nM Funct
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
447 7 4 9 1.7 C1=CC=C(C=C1)C(CNC2=C3C(=NC=N2)N(C=N3)[C@H]4[C@@H]([C@@H]([C@H](O4)CO)O)O)C5=CC=CC=C5
CHEMBL3133155 aa2br_human Human No 5.3 EC50 = 5011.9 nM Funct
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
351 5 5 10 -1.4 CCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O
CHEMBL4215091 aa2br_human Human No 7.3 EC50 = 51 nM Funct
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
403 7 2 8 3.3 N#Cc1c(N)nc(SCc2ncn[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1
CHEMBL186113 aa2br_human Human Yes 7.3 EC50 = 51 nM Funct
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
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
CHEMBL477 aa2br_human Human Yes 4.3 EC50 = 51286.1 nM Bind
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
267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL4089741 aa2br_human Human No 6.3 EC50 = 527 nM Funct
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
429 6 3 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL226245 aa2br_human Human No 7.3 EC50 = 53.6 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL3414946 aa2br_human Human No 6.3 EC50 = 530 nM Funct
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
461 5 3 12 1.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL261482 aa2br_human Human Yes 5.3 EC50 = 5300 nM Funct
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
320 3 4 9 -1.7 C1CC1NC(=O)[C@@H]2[C@H]([C@H]([C@@H](O2)N3C=NC4=C(N=CN=C43)N)O)O
CHEMBL376542 aa2br_human Human No 7.3 EC50 = 54.5 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
350 4 6 9 -2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NC(=N)N)ncnc32)[C@H](O)[C@@H]1O
CHEMBL2070508 aa2br_human Human Yes 4.3 EC50 = 54000 nM Funct
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
348 3 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CCCC2)[C@@H](O)[C@H]1O
CHEMBL3414937 aa2br_human Human No 6.3 EC50 = 542 nM Funct
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
367 3 3 12 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL361925 aa2br_human Human No 6.3 EC50 = 560 nM Funct
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
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
CHEMBL4071338 aa2br_human Human No 6.2 EC50 = 592 nM Funct
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
457 6 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL4096796 aa2br_human Human No 7.2 EC50 = 60.3 nM Funct
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
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
CHEMBL217952 aa2br_human Human No 6.2 EC50 = 603 nM Funct
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
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
CHEMBL2042302 aa2br_human Human No 5.2 EC50 = 6069 nM Funct
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
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
CHEMBL3350613 aa2br_human Human No 5.2 EC50 = 6100 nM Funct
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
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
CHEMBL2092787 aa2br_human Human No 5.2 EC50 = 6100 nM Bind
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
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
CHEMBL3350613 aa2br_human Human No 5.2 EC50 = 6100 nM Bind
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
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
CHEMBL4076565 aa2br_human Human No 6.2 EC50 = 616.6 nM Funct
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
857 16 6 13 6.4 CC(=O)NC1=C(C(=C(S1)C2=CC=C(C=C2)C(=O)NCCCCCCNC3=C4C(=NC=N3)N(C=N4)[C@H]5[C@@H]([C@@H]([C@H](O5)CO)O)O)C6=CC(=CC=C6)C(F)(F)F)C(=O)C7=CC=CC=C7
CHEMBL408918 aa2br_human Human No 5.2 EC50 = 6200 nM Bind
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
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
CHEMBL4063841 aa2br_human Human No 7.2 EC50 = 63.1 nM Funct
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
801 14 6 13 5.7 C1=CC=C(C=C1)C(=O)C2=C(SC(=C2C3=CC(=CC=C3)C(F)(F)F)C4=CC=C(C=C4)C(=O)NCCCCCNC5=C6C(=NC=N5)N(C=N6)[C@H]7[C@@H]([C@@H]([C@H](O7)CO)O)O)N
CHEMBL4087306 aa2br_human Human No 6.2 EC50 = 637 nM Funct
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
387 6 3 12 -0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL2042312 aa2br_human Human No 5.2 EC50 = 6694 nM Funct
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
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
CHEMBL3414940 aa2br_human Human No 6.2 EC50 = 675 nM Funct
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
373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL3414941 aa2br_human Human No 6.2 EC50 = 677 nM Funct
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
407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL368880 aa2br_human Human No 6.2 EC50 = 680 nM Funct
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
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
CHEMBL226193 aa2br_human Human No 8.1 EC50 = 7.3 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL4741079 aa2br_human Human No 6.2 EC50 = 708.0 nM Funct
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
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
CHEMBL3416782 aa2br_human Human No 5.2 EC50 = 7130 nM Funct
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
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
CHEMBL284969 aa2br_human Human Yes 4.1 EC50 = 72443.6 nM Bind
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
369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1
CHEMBL258535 aa2br_human Human No 6.1 EC50 = 730 nM Bind
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
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
CHEMBL2042303 aa2br_human Human No 6.1 EC50 = 739 nM Funct
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
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
CHEMBL4085418 aa2br_human Human No 7.1 EC50 = 75.9 nM Funct
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
856 16 6 13 6.2 CCNC(=O)[C@@H]1[C@H]([C@H]([C@@H](O1)N2C=NC3=C(N=CN=C32)NCCCCCCNC(=O)C4=CC=C(C=C4)C5=C(C(=C(S5)N)C(=O)C6=CC=CC=C6)C7=CC(=CC=C7)C(F)(F)F)O)O
CHEMBL373478 aa2br_human Human No 6.1 EC50 = 767 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL3133158 aa2br_human Human No 6.1 EC50 = 794.3 nM Funct
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
377 4 5 10 -0.9 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N)nc32)[C@H](O)[C@@H]1O
CHEMBL218596 aa2br_human Human No 7.1 EC50 = 82 nM Funct
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
417 6 5 11 -1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccco4)ncnc32)[C@H](O)[C@@H]1O
CHEMBL3414948 aa2br_human Human No 6.1 EC50 = 834 nM Funct
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
583 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccccc5I)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL4203420 aa2br_human Human No 7.1 EC50 = 84 nM Funct
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
402 7 2 7 3.9 N#Cc1c(N)nc(SCc2ccn[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1
CHEMBL4472401 aa2br_human Human No 6.1 EC50 = 852 nM Funct
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
286 4 2 7 1.8 N#Cc1c(N)nc(SCCO)c(C#N)c1-c1ccoc1
CHEMBL3416808 aa2br_human Human No 6.1 EC50 = 866 nM Funct
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
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
CHEMBL4582726 aa2br_human Human No 6.1 EC50 = 885 nM Funct
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
302 4 2 7 2.2 N#Cc1c(N)nc(SCCO)c(C#N)c1-c1cccs1
CHEMBL1089440 aa2br_human Human No 5.1 EC50 = 8870 nM Funct
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
413 5 2 8 4.2 O=C(Nc1ccccc1)Nc1nc(Oc2ccccc2)nc2nc(-c3ccco3)nn12
CHEMBL438418 aa2br_human Human No 5.1 EC50 = 8900 nM Bind
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
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
CHEMBL222500 aa2br_human Human No 6.1 EC50 = 896 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL122396 aa2br_human Human No 8.1 EC50 = 9 nM Funct
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
362 5 2 7 3.1 COc1ccc(-c2c(C#N)c(N)nc(SCc3ncc[nH]3)c2C#N)cc1
CHEMBL4216880 aa2br_human Human No 8.0 EC50 = 9.5 nM Funct
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
402 7 2 7 3.9 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1
CHEMBL4089092 aa2br_human Human No 7.0 EC50 = 91.2 nM Funct
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
696 13 5 11 5.3 C1=CC(=CC(=C1)C(F)(F)F)C2=C(SC=C2)C3=CC=C(C=C3)C(=O)NCCCCCCNC4=C5C(=NC=N4)N(C=N5)[C@H]6[C@@H]([C@@H]([C@H](O6)CO)O)O
CHEMBL410095 aa2br_human Human No 5.0 EC50 = 9100 nM Bind
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
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
CHEMBL262363 aa2br_human Human No 6.0 EC50 = 920 nM Bind
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
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
CHEMBL3416806 aa2br_human Human No 6.0 EC50 = 927 nM Funct
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
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
CHEMBL3416780 aa2br_human Human No 5.0 EC50 = 9287 nM Funct
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
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
CHEMBL3416781 aa2br_human Human No 5.0 EC50 = 9352 nM Funct
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
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
CHEMBL4213681 aa2br_human Human No 7.0 EC50 = 94 nM Funct
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
393 7 2 7 2.7 CNC(=O)CSc1nc(N)c(C#N)c(-c2ccc(OCC3CC3)cc2)c1C#N
CHEMBL464859 aa2br_human Human Yes 7.0 EC50 = 94.8 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL1234591 aa2br_human Human Yes 6.0 EC50 = 948 nM Bind
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based assay
324 4 5 10 -2.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCO)[C@@H](O)[C@H]1O
CHEMBL4104819 aa2br_human Human No 7.0 EC50 = 95.5 nM Funct
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
815 15 6 13 6.1 C1=CC=C(C=C1)C(=O)C2=C(SC(=C2C3=CC(=CC=C3)C(F)(F)F)C4=CC=C(C=C4)C(=O)NCCCCCCNC5=C6C(=NC=N5)N(C=N6)[C@H]7[C@@H]([C@@H]([C@H](O7)CO)O)O)N
CHEMBL186113 aa2br_human Human Yes 6.0 EC50 = 950 nM Funct
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
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
CHEMBL259938 aa2br_human Human No 6.0 EC50 = 960 nM Bind
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
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
CHEMBL406594 aa2br_human Human No 6.0 EC50 = 965 nM Funct
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
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
CHEMBL4069296 aa2br_human Human No 7.0 EC50 = 97.7 nM Funct
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
830 15 7 14 5.7 C1=CC=C(C=C1)C(=O)C2=C(SC(=C2C3=CC(=CC=C3)C(F)(F)F)C4=CC=C(C=C4)C(=O)NCCCCCCNC5=C6C(=NC(=N5)N)N(C=N6)[C@H]7[C@@H]([C@@H]([C@H](O7)CO)O)O)N
CHEMBL4517597 aa2br_human Human No 6.0 EC50 = 982 nM Funct
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
406 5 1 8 4.2 COC(=O)c1cccc(CSc2nc(N)c(C#N)c(-c3cccs3)c2C#N)c1
CHEMBL223845 aa2br_human Human No 6.0 EC50 = 989 nM Funct
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
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
CHEMBL4643397 aa2br_human Human No 9.5 IC50 = 0.3 nM Funct
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
500 7 3 11 1.8 Nc1nc(NCCN2CCN(c3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12
CHEMBL483688 aa2br_human Human Yes 9.3 IC50 = 0.5 nM Bind
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
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
CHEMBL483688 aa2br_human Human Yes 9.1 IC50 = 0.7 nM Bind
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
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
CHEMBL437309 aa2br_human Human No 9.0 IC50 = 1 nM Bind
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
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
CHEMBL4215606 aa2br_human Human Yes 9.0 IC50 = 1.1 nM Bind
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
540 7 0 7 2.8 CCCN1C(=O)N=C2N=C(c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)cc5)CC4)cc3)N=C2C1=O
CHEMBL483688 aa2br_human Human Yes 9.0 IC50 = 1.1 nM Funct
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
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
CHEMBL7113 aa2br_human Human No 8.9 IC50 = 1.4 nM Funct
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
262 1 1 5 2.7 Oc1c(-c2ccccc2)nnc2nc3ccccc3n12
CHEMBL1077943 aa2br_human Human No 8.9 IC50 = 1.4 nM Funct
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1
CHEMBL486479 aa2br_human Human No 8.8 IC50 = 1.6 nM Funct
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
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
CHEMBL483469 aa2br_human Human No 8.7 IC50 = 1.9 nM Funct
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
542 7 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O
CHEMBL113518 aa2br_human Human No 8.0 IC50 = 10 nM Funct
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
342 3 0 6 3.4 O=c1c(-c2ccco2)nnc2n(Cc3ccccc3)c3ccccc3n12
CHEMBL379217 aa2br_human Human No 8.0 IC50 = 10 nM Bind
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
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
CHEMBL212625 aa2br_human Human Yes 8.0 IC50 = 10.1 nM Funct
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
508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O
CHEMBL488541 aa2br_human Human No 8.0 IC50 = 10.9 nM Funct
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
522 8 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(CCc5ccccc5)CC4)cc3)[nH]c2c1=O
CHEMBL3937015 aa2br_human Human No 6.0 IC50 = 1000 nM Bind
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
395 4 2 4 5.7 O[C@H]1CC[C@H](Nc2ncc(-c3ccc4ccccc4c3)c(-c3ccccc3)n2)CC1
CHEMBL32481 aa2br_human Human No 7.0 IC50 = 103 nM Funct
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
449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)nn3C)[nH]c2n(CCC)c1=O
CHEMBL3913413 aa2br_human Human No 7.0 IC50 = 103 nM Funct
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
341 4 2 7 3.7 Nc1nc(NCc2cccc(F)c2)nc2sc(-c3ccco3)nc12
CHEMBL578008 aa2br_human Human No 5.0 IC50 = 10370 nM Funct
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
437 5 1 8 4.1 CCn1cc2c(nc(NC(=O)Cc3ccc4ccccc4c3)n3nc(-c4ccco4)nc23)n1
CHEMBL2071046 aa2br_human Human No 6.0 IC50 = 1042 nM Funct
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
532 5 3 9 2.9 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccc(F)cc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL258473 aa2br_human Human No 7.0 IC50 = 106 nM Funct
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
483 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4cccc(Cl)c4)n3)nc2n(CCC)c1=O
CHEMBL4067401 aa2br_human Human No 7.0 IC50 = 107 nM Bind
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
486 6 1 8 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CC)c1=O
CHEMBL1927444 aa2br_human Human No 5.0 IC50 = 10700 nM Funct
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
342 5 3 9 1.5 NCC1CCC(CNc2nc(N)n3nc(-c4ccco4)nc3n2)CC1
CHEMBL1962813 aa2br_human Human No 5.0 IC50 = 10700 nM Funct
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
342 5 3 9 1.5 NCC1CCC(CNc2nc(N)n3nc(-c4ccco4)nc3n2)CC1
CHEMBL287529 aa2br_human Human No 7.0 IC50 = 108 nM Funct
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
543 9 2 9 2.9 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(Br)cc4)nn3C)[nH]c2n(CCC)c1=O
CHEMBL1081873 aa2br_human Human No 7.0 IC50 = 109 nM Funct
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
347 5 1 7 3.3 O=C(c1cccnc1)c1nc(NCc2cccnc2)nc2ccsc12
CHEMBL4167125 aa2br_human Human No 7.0 IC50 = 109 nM Funct
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
324 4 2 8 2.9 Nc1nc(NCc2cccnc2)nc2sc(-c3ccco3)nc12
CHEMBL1955916 aa2br_human Human No 8.0 IC50 = 11 nM Funct
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
527 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Br)ccc5[nH]4)no3)nc2n(CCC)c1=O
CHEMBL335950 aa2br_human Human No 7.0 IC50 = 110 nM Funct
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
527 8 1 8 5.7 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12
CHEMBL1258397 aa2br_human Human No 6.0 IC50 = 1100 nM Funct
Antagonist activity at adenosine A2B receptor by cAMP assayAntagonist activity at adenosine A2B receptor by cAMP assay
451 6 2 7 5.2 COc1ccc(Nc2c(-c3ccc4nccnc4c3)c(C)nn2-c2ccccc2)c(C(=O)O)c1
CHEMBL4576194 aa2br_human Human No 6.0 IC50 = 1100 nM Bind
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
496 6 1 9 2.6 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1nc2cc(S(N)(=O)=O)ccc2o1
CHEMBL62350 aa2br_rat Rat Yes 6.0 IC50 = 1100 nM Funct
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
256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O
CHEMBL4127811 aa2br_human Human No 6.0 IC50 = 1105 nM Funct
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
285 4 2 6 2.6 Cc1nc2c(N)nc(NCCc3ccccc3)nc2s1
CHEMBL2071044 aa2br_human Human No 6.0 IC50 = 1107 nM Funct
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
514 5 3 9 2.8 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL3903604 aa2br_human Human No 7.0 IC50 = 111 nM Funct
Antagonist activity at adenosine A2b receptor (unknown origin)Antagonist activity at adenosine A2b receptor (unknown origin)
496 5 3 7 5.0 CCn1nc(-c2cccc(-c3cncc(O)c3)c2)cc(NC(=O)Nc2c(Cl)cncc2Cl)c1=O
CHEMBL573771 aa2br_human Human No 5.0 IC50 = 11100 nM Funct
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
539 8 1 8 5.8 O=C(Cc1ccc(-c2ccccc2)cc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12
CHEMBL1927632 aa2br_human Human No 5.0 IC50 = 11100 nM Funct
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
217 1 2 8 -0.1 Nc1nc(N)n2nc(-c3ccco3)nc2n1
CHEMBL3798383 aa2br_human Human No 7.0 IC50 = 112 nM Funct
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
307 3 2 7 2.4 Nc1nc(-c2ccco2)nc2cn(Cc3ccccc3O)nc12
CHEMBL4172264 aa2br_human Human No 7.0 IC50 = 112 nM Funct
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
343 5 2 8 3.6 Nc1nc(NCCc2cccs2)nc2sc(-c3ccco3)nc12
CHEMBL1955918 aa2br_human Human No 6.9 IC50 = 114 nM Funct
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
479 9 2 10 2.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(OC)ccc5[nH]4)no3)nc2n(CCC)c1=O
CHEMBL261027 aa2br_human Human No 6.9 IC50 = 115 nM Funct
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
575 8 2 8 3.1 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(I)cc4)n3)nc2n(CCC)c1=O
CHEMBL431703 aa2br_human Human No 6.9 IC50 = 115 nM Funct
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
509 10 3 10 1.8 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(C(=O)O)cc4)nn3C)[nH]c2n(CCC)c1=O
CHEMBL3754573 aa2br_human Human No 4.9 IC50 = 11800 nM Funct
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
397 7 2 8 4.0 c1ccc(CNc2nc(NCc3ccccc3)n3nc(-c4ccco4)nc3n2)cc1
CHEMBL1171165 aa2br_human Human No 7.9 IC50 = 12 nM Funct
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
467 7 1 7 4.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(F)c4)c3)sc12
CHEMBL1171897 aa2br_human Human No 7.9 IC50 = 12 nM Funct
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
387 5 1 5 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12
CHEMBL4521489 aa2br_human Human No 7.9 IC50 = 12 nM Bind
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
424 8 0 8 2.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cn3ccnc3)sc21
CHEMBL208705 aa2br_human Human No 7.9 IC50 = 12 nM Bind
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
411 4 2 7 1.4 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)Nc4ccccn4)cc3)cc2n(C)c1=O
CHEMBL210969 aa2br_human Human No 7.9 IC50 = 12 nM Bind
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
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
CHEMBL3952586 aa2br_human Human No 6.9 IC50 = 120 nM Funct
Antagonist activity at adenosine A2b receptor (unknown origin)Antagonist activity at adenosine A2b receptor (unknown origin)
562 7 3 6 5.8 CCn1nc(-c2cccc(-c3cccc(C(=O)NC4CC4)c3)c2)cc(NC(=O)Nc2c(Cl)cncc2Cl)c1=O
CHEMBL1081335 aa2br_human Human No 6.9 IC50 = 120 nM Funct
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
313 5 2 6 2.4 CCNC(=O)c1nc(NCc2cccnc2)nc2ccsc12
CHEMBL1672627 aa2br_human Human Yes 6.9 IC50 = 120 nM Funct
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
335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2cccnc2)n1)C1CC1
CHEMBL2312725 aa2br_human Human Yes 6.9 IC50 = 120 nM Funct
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
250 1 1 5 2.7 Nc1nc2ccccc2c2cc(-c3ccco3)nn12
CHEMBL284615 aa2br_human Human No 6.9 IC50 = 120 nM Funct
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
537 11 2 11 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(C(=O)OCC)cc4)nn3C)[nH]c2n(CCC)c1=O
CHEMBL408186 aa2br_human Human No 6.9 IC50 = 120 nM Funct
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
509 10 2 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(NC(=O)Cc4ccc(OC)c(OC)c4)nn3C)nc2n(CCC)c1=O
CHEMBL4165484 aa2br_human Human No 6.9 IC50 = 120 nM Funct
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
367 5 2 8 3.9 COc1cccc(CNc2nc(N)c3nc(-c4ccc(C)o4)sc3n2)c1
CHEMBL4589654 aa2br_human Human No 5.9 IC50 = 1200 nM Bind
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
468 8 1 9 2.4 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(C)(O)c3cncn3C)sc21
CHEMBL16687 aa2br_human Human Yes 5.9 IC50 = 1200 nM Bind
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
285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1
CHEMBL48681 aa2br_rat Rat No 5.9 IC50 = 1200 nM Funct
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
365 1 2 6 2.8 Cn1c(-c2ccc(F)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21
CHEMBL1935756 aa2br_human Human No 6.9 IC50 = 122 nM Funct
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
404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3cnn(C)c3c3nc(-c4ccco4)nn23)cc1
CHEMBL573327 aa2br_human Human No 5.9 IC50 = 1220 nM Funct
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
463 7 1 8 4.6 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1
CHEMBL3317565 aa2br_human Human No 6.9 IC50 = 123 nM Funct
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
319 3 1 5 3.1 Nc1nc(Cc2ccccc2F)nc2cn(-c3ccccc3)nc12
CHEMBL576018 aa2br_human Human No 4.9 IC50 = 12400 nM Funct
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
451 6 1 8 4.5 CCCn1cc2c(nc(NC(=O)Cc3cccc4ccccc34)n3nc(-c4ccco4)nc23)n1
CHEMBL1077752 aa2br_human Human No 5.9 IC50 = 1259 nM Funct
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
303 4 1 6 3.7 CCNc1nc(C(=O)c2ccc(C)s2)c2sccc2n1
CHEMBL121766 aa2br_human Human No 6.9 IC50 = 127 nM Bind
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
419 7 1 7 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2OC)CC1
CHEMBL32225 aa2br_human Human No 6.9 IC50 = 128 nM Funct
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
483 8 2 8 2.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(Cl)cc4)nn3C)[nH]c2n(CCC)c1=O
CHEMBL1079232 aa2br_human Human No 5.9 IC50 = 1295 nM Funct
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
376 6 1 7 3.9 COc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)cc1
CHEMBL4581984 aa2br_human Human No 7.9 IC50 = 13 nM Funct
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
375 5 2 7 3.1 N#Cc1c(N)nc(SCc2cccc(C(N)=O)c2)c(C#N)c1-c1ccco1
CHEMBL1172442 aa2br_human Human No 7.9 IC50 = 13 nM Funct
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
484 9 1 7 3.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N(C)CCOC)cc3)sc12
CHEMBL1082064 aa2br_human Human No 7.9 IC50 = 13 nM Funct
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
353 4 1 6 3.5 CC(Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1
CHEMBL211071 aa2br_human Human No 7.9 IC50 = 13 nM Bind
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
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
CHEMBL1760896 aa2br_human Human No 7.9 IC50 = 13 nM Funct
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
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
CHEMBL4172818 aa2br_human Human No 7.9 IC50 = 13.2 nM Funct
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
325 4 2 9 2.3 Nc1nc(NCc2cnccn2)nc2sc(-c3ccco3)nc12
CHEMBL4458469 aa2br_human Human No 6.9 IC50 = 130 nM Bind
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
366 5 1 6 2.5 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1ncc[nH]1
CHEMBL4540909 aa2br_human Human No 6.9 IC50 = 130 nM Bind
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
325 4 0 6 2.3 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CC#N
CHEMBL341777 aa2br_human Human No 6.9 IC50 = 130 nM Funct
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
479 8 1 9 4.0 O=C(COc1ccccc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12
CHEMBL4457584 aa2br_human Human No 5.9 IC50 = 1300 nM Bind
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
366 5 1 6 2.5 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1cnc[nH]1
CHEMBL51829 aa2br_rat Rat No 5.9 IC50 = 1300 nM Funct
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
348 1 2 7 2.1 Cn1c(-c2ccccn2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21
CHEMBL574483 aa2br_human Human No 4.9 IC50 = 13000 nM Funct
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
391 4 1 8 2.6 Cn1cc2c(nc(NC(=O)Cc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1
CHEMBL1094132 aa2br_human Human No 5.9 IC50 = 1324 nM Funct
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
420 5 2 5 5.2 O=C(Nc1ccccc1)Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12
CHEMBL1094131 aa2br_human Human No 5.9 IC50 = 1327 nM Funct
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
439 5 1 5 5.4 O=C(Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12)c1cccc(Cl)c1
CHEMBL97961 aa2br_human Human No 4.9 IC50 = 13300 nM Bind
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
356 4 2 7 2.5 NCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12
CHEMBL4126427 aa2br_human Human No 6.9 IC50 = 134 nM Funct
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
291 4 2 7 2.7 Cc1nc2c(N)nc(NCCc3cccs3)nc2s1
CHEMBL3752431 aa2br_human Human No 4.9 IC50 = 13422 nM Funct
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
299 3 2 8 2.1 Nc1nc(NC2CCCCC2)nc2nc(-c3ccco3)nn12
CHEMBL4213768 aa2br_human Human No 6.9 IC50 = 135 nM Funct
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
433 8 3 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2c1=O
CHEMBL4442438 aa2br_human Human No 6.9 IC50 = 135 nM Bind
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
332 5 0 5 2.7 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CCF
CHEMBL576369 aa2br_human Human No 4.9 IC50 = 13700 nM Funct
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
379 4 1 9 2.5 Cn1cc2c(nc(NC(=O)Cc3ccsc3)n3nc(-c4ccco4)nc23)n1
CHEMBL576185 aa2br_human Human No 5.9 IC50 = 1390 nM Funct
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
463 7 1 8 4.6 CC(C)CCn1cc2c(nc(NC(=O)Cc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1
CHEMBL4458223 aa2br_human Human No 7.9 IC50 = 14 nM Bind
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
414 8 1 7 2.9 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(O)C3CC3)sc21
CHEMBL211762 aa2br_human Human No 7.9 IC50 = 14 nM Bind
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
439 6 2 7 1.1 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(C)c1=O
CHEMBL1760886 aa2br_human Human No 7.9 IC50 = 14 nM Funct
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
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
CHEMBL50051 aa2br_human Human No 7.9 IC50 = 14 nM Funct
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
337 1 2 7 2.3 Cn1c(-c2ccco2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21
CHEMBL4167557 aa2br_human Human No 7.9 IC50 = 14 nM Funct
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
327 5 2 8 3.2 Nc1nc(NCCc2ccco2)nc2sc(-c3ccco3)nc12
CHEMBL138593 aa2br_human Human No 6.9 IC50 = 140 nM Funct
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
493 9 1 9 4.4 O=C(COc1ccccc1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12
CHEMBL32582 aa2br_human Human No 6.9 IC50 = 140 nM Funct
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
496 9 2 11 2.1 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc5c(c4)OCO5)no3)[nH]c2n(CCC)c1=O
CHEMBL51192 aa2br_human Human No 6.9 IC50 = 140 nM Funct
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
353 3 2 6 2.7 CCC(O)(C#Cc1nc(N)c2nc(-c3cccc(F)c3)n(C)c2n1)CC
CHEMBL4204683 aa2br_human Human No 6.9 IC50 = 141 nM Funct
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
447 9 3 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCc4ccccc4)cc3)[nH]c2c1=O
CHEMBL573089 aa2br_human Human No 5.8 IC50 = 1440 nM Funct
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
497 7 1 8 5.3 CC(C)CCn1cc2c(nc(NC(=O)Cc3c(Cl)cccc3Cl)n3nc(-c4ccco4)nc23)n1
CHEMBL3986586 aa2br_human Human No 6.8 IC50 = 145 nM Funct
Antagonist activity at adenosine A2b receptor (unknown origin)Antagonist activity at adenosine A2b receptor (unknown origin)
635 9 3 8 5.0 CCn1nc(-c2cccc(-c3cccc(C(=O)NCCN4CCOCC4)c3)c2)cc(NC(=O)Nc2c(Cl)cncc2Cl)c1=O
CHEMBL4441343 aa2br_human Human No 6.8 IC50 = 145 nM Bind
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
380 5 0 7 2.6 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1nccn1C
CHEMBL3945895 aa2br_human Human No 6.8 IC50 = 146 nM Funct
Antagonist activity at adenosine A2b receptor (unknown origin)Antagonist activity at adenosine A2b receptor (unknown origin)
716 11 4 8 6.0 CCn1nc(-c2cccc(-c3cc(C(=O)NCC[C@H]4CCCN4C)cc(C(=O)NC4CC4)c3)c2)cc(NC(=O)Nc2c(Cl)cncc2Cl)c1=O
CHEMBL4633630 aa2br_human Human No 6.8 IC50 = 146 nM Funct
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
556 9 4 11 2.0 Nc1nc(NCC2CCN(CC(=O)NCc3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12
CHEMBL1096078 aa2br_human Human No 5.8 IC50 = 1467 nM Funct
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
450 6 2 6 5.2 COc1ccc(NC(=O)Nc2nc(-c3ccccc3)nc3nn(Cc4ccccc4)cc23)cc1
CHEMBL1079044 aa2br_human Human No 6.8 IC50 = 148 nM Funct
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
353 5 1 8 3.4 O=C(c1cncs1)c1nc(NCc2cccnc2)nc2ccsc12
CHEMBL1079132 aa2br_human Human No 6.8 IC50 = 148 nM Funct
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
352 5 1 7 4.0 O=C(c1ccsc1)c1nc(NCc2cccnc2)nc2ccsc12
CHEMBL112756 aa2br_human Human No 7.8 IC50 = 15 nM Funct
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
338 2 0 5 3.7 O=c1c(-c2ccccc2)nnc2n(-c3ccccc3)c3ccccc3n12
CHEMBL1171898 aa2br_human Human No 7.8 IC50 = 15 nM Funct
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
373 4 1 5 3.7 COc1ccc(N(C)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12
CHEMBL1955899 aa2br_human Human No 7.8 IC50 = 15 nM Funct
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
496 8 2 9 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)ccc5[nH]4)nn3C)nc2n(CCC)c1=O
CHEMBL210931 aa2br_human Human No 7.8 IC50 = 15 nM Bind
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
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
CHEMBL212528 aa2br_human Human No 7.8 IC50 = 15 nM Bind
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
483 8 2 8 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCc4ccc(OC)cn4)cc3)cc2n(C)c1=O
CHEMBL7608 aa2br_human Human No 7.8 IC50 = 15.3 nM Funct
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
252 1 1 6 2.2 Oc1c(-c2ccco2)nnc2nc3ccccc3n12
CHEMBL4457476 aa2br_human Human No 6.8 IC50 = 150 nM Bind
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
374 7 1 7 1.9 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(CO)sc21
CHEMBL4538262 aa2br_human Human No 6.8 IC50 = 150 nM Bind
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
428 8 1 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(C)(O)C3CC3)sc21
CHEMBL435022 aa2br_human Human No 6.8 IC50 = 150 nM Funct
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
445 8 1 9 3.8 CC(C)CCn1cc2c(nc(NC(=O)COc3ccccc3)n3nc(-c4ccco4)nc23)n1
CHEMBL300624 aa2br_human Human No 6.8 IC50 = 150 nM Funct
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
325 1 2 6 1.9 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC(C)(C)O)nc21
CHEMBL4582620 aa2br_human Human No 5.8 IC50 = 1500 nM Bind
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
370 6 0 6 2.9 COCCn1c(=O)n(CC2(c3ccccc3)CC2)c(=O)c2c(C)csc21
CHEMBL2311150 aa2br_human Human Yes 5.8 IC50 = 1500 nM Funct
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
412 8 0 8 2.9 CCCn1c(=O)c2c(nc(/C=C/c3ccc(OC)c(OC)c3)n2C)n(CCC)c1=O
CHEMBL27508 aa2br_human Human Yes 5.8 IC50 = 1500 nM Funct
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
412 8 0 8 2.9 CCCn1c(=O)c2c(nc(/C=C/c3ccc(OC)c(OC)c3)n2C)n(CCC)c1=O
CHEMBL573779 aa2br_human Human No 4.8 IC50 = 15000 nM Funct
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
393 5 1 9 3.0 CCn1cc2c(nc(NC(=O)Cc3cccs3)n3nc(-c4ccco4)nc23)n1
CHEMBL4557250 aa2br_human Human No 6.8 IC50 = 152 nM Funct
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
362 5 2 7 3.5 N#Cc1c(N)nc(SCc2cccc(CO)c2)c(C#N)c1-c1ccco1
CHEMBL3799848 aa2br_human Human No 6.8 IC50 = 152 nM Funct
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
339 3 1 6 3.7 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4Cl)cc3n2)o1
CHEMBL32281 aa2br_human Human No 6.8 IC50 = 152 nM Funct
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
449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)n(C)n3)[nH]c2n(CCC)c1=O
CHEMBL400812 aa2br_human Human No 5.8 IC50 = 1527 nM Funct
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
425 4 1 7 3.6 COc1ccc(C(=O)Nc2nc3ccccc3n3c(=O)c(-c4ccc(C)cc4)nn23)cc1
CHEMBL2071045 aa2br_human Human No 5.8 IC50 = 1542 nM Funct
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
542 7 3 9 3.2 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCCCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL259177 aa2br_human Human No 6.8 IC50 = 156 nM Funct
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
527 8 2 8 3.3 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Br)cc4)n3)nc2n(CCC)c1=O
CHEMBL4645283 aa2br_human Human No 6.8 IC50 = 156 nM Funct
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
570 10 4 11 2.1 Nc1nc(NCC2CCN(CC(=O)NCCc3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12
CHEMBL1170135 aa2br_human Human No 7.8 IC50 = 16 nM Funct
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
480 6 1 6 4.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCCCC4)cc3)sc12
CHEMBL1171200 aa2br_human Human No 7.8 IC50 = 16 nM Funct
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
466 6 1 6 4.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCCC4)cc3)sc12
CHEMBL1080068 aa2br_human Human No 7.8 IC50 = 16 nM Funct
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
386 5 1 7 4.6 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2cc(Cl)sc12
CHEMBL209019 aa2br_human Human No 7.8 IC50 = 16 nM Bind
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
493 5 1 7 1.7 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)cc2n(C)c1=O
CHEMBL1760884 aa2br_human Human No 7.8 IC50 = 16 nM Funct
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
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
CHEMBL482855 aa2br_human Human No 7.8 IC50 = 16.2 nM Funct
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
538 8 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O
CHEMBL32770 aa2br_human Human No 6.8 IC50 = 160 nM Funct
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
467 8 2 8 2.4 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4cccc(F)c4)nn3C)[nH]c2n(CCC)c1=O
CHEMBL48681 aa2br_human Human No 6.8 IC50 = 160 nM Funct
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
365 1 2 6 2.8 Cn1c(-c2ccc(F)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21
CHEMBL4450782 aa2br_human Human No 5.8 IC50 = 1600 nM Bind
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
310 4 0 6 2.2 COCCn1c(=O)n(CC(C)(C)C)c(=O)c2c(C)csc21
CHEMBL297949 aa2br_rat Rat No 5.8 IC50 = 1600 nM Funct
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
377 2 2 7 2.7 COc1cccc(-c2nc3c(N)nc(C#CC4(O)CCCCC4)nc3n2C)c1
CHEMBL3941513 aa2br_human Human No 6.8 IC50 = 169 nM Funct
Antagonist activity at adenosine A2b receptor (unknown origin)Antagonist activity at adenosine A2b receptor (unknown origin)
633 9 3 7 6.2 CCn1nc(-c2cccc(-c3cccc(C(=O)NCCN4CCCCC4)c3)c2)cc(NC(=O)Nc2c(Cl)cncc2Cl)c1=O
CHEMBL1079115 aa2br_human Human No 7.8 IC50 = 17 nM Funct
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
380 5 1 7 4.9 Cc1ccc(C(=O)c2nc(NC(C)c3cccnc3)nc3ccsc23)s1
CHEMBL209208 aa2br_human Human No 7.8 IC50 = 17 nM Bind
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
455 7 2 8 1.0 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCOc4ccccn4)cc3)cc2n(C)c1=O
CHEMBL212464 aa2br_human Human No 7.8 IC50 = 17 nM Bind
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
467 8 2 7 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(C)c1=O
CHEMBL380177 aa2br_human Human No 7.8 IC50 = 17 nM Bind
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
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
CHEMBL1760892 aa2br_human Human No 7.8 IC50 = 17 nM Funct
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
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
CHEMBL336217 aa2br_human Human No 6.8 IC50 = 170 nM Funct
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
479 7 1 8 5.1 CC(C)CCn1cc2c(nc(NC(=O)Cc3cccc4ccccc34)n3nc(-c4ccco4)nc23)n1
CHEMBL4453664 aa2br_human Human No 5.8 IC50 = 1700 nM Bind
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
469 7 1 7 2.7 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CCc1ccc(S(N)(=O)=O)cc1
CHEMBL4469697 aa2br_human Human No 5.8 IC50 = 1700 nM Bind
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
416 8 0 8 2.6 CCOC(=O)c1sc2c(c1C)c(=O)n(CCc1ccccc1)c(=O)n2CCOC
CHEMBL3969954 aa2br_human Human No 6.8 IC50 = 172 nM Funct
Antagonist activity at adenosine A2b receptor (unknown origin)Antagonist activity at adenosine A2b receptor (unknown origin)
495 5 3 6 5.6 CCn1nc(-c2cccc(-c3cccc(O)c3)c2)cc(NC(=O)Nc2c(Cl)cncc2Cl)c1=O
CHEMBL4450312 aa2br_human Human No 4.8 IC50 = 17330 nM Funct
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
351 2 4 9 1.2 Nc1nc(-c2cc(O)c(O)c(O)c2)cn2c(=O)n(-c3ccccc3)nc12
CHEMBL4208432 aa2br_human Human No 6.8 IC50 = 174 nM Funct
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
461 10 3 6 2.6 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCc4ccccc4)cc3)[nH]c2c1=O
CHEMBL2069325 aa2br_human Human No 5.8 IC50 = 1755 nM Funct
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
528 6 3 9 2.8 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL1079043 aa2br_human Human No 6.8 IC50 = 176 nM Funct
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
353 5 1 8 3.4 O=C(c1nccs1)c1nc(NCc2cccnc2)nc2ccsc12
CHEMBL3951103 aa2br_human Human No 5.8 IC50 = 1768 nM Funct
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
351 6 2 7 4.0 Nc1nc(NCCCc2ccccc2)nc2sc(-c3ccco3)nc12
CHEMBL97700 aa2br_human Human No 5.8 IC50 = 1770 nM Bind
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
384 6 2 7 3.3 NCCCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12
CHEMBL1079118 aa2br_human Human No 7.8 IC50 = 18 nM Funct
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
352 5 1 7 4.0 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2ccsc12
CHEMBL1079894 aa2br_human Human No 7.8 IC50 = 18 nM Funct
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
353 4 1 6 3.5 C[C@H](Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1
CHEMBL209944 aa2br_human Human No 7.8 IC50 = 18 nM Bind
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
563 10 2 7 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccccc5)CC4)cc3)cc2n(CCC)c1=O
CHEMBL210456 aa2br_human Human No 7.8 IC50 = 18 nM Bind
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
441 5 2 8 1.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)cn1
CHEMBL1760900 aa2br_human Human No 7.8 IC50 = 18 nM Funct
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
520 5 1 5 6.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)N3CCC(c4cccc(C(F)(F)F)c4)CC3)sc12
CHEMBL3980049 aa2br_human Human No 7.8 IC50 = 18 nM Funct
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
369 5 4 9 3.0 Nc1nc(NCCc2ccc(O)c(O)c2)nc2sc(-c3ccco3)nc12
CHEMBL483688 aa2br_human Human Yes 7.7 IC50 = 18.3 nM Funct
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
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
CHEMBL1955911 aa2br_human Human No 6.8 IC50 = 180 nM Funct
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
490 8 2 10 1.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc(=O)c5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O
CHEMBL4451942 aa2br_human Human No 6.8 IC50 = 180 nM Bind
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
370 5 0 6 3.0 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CC1CCCO1
CHEMBL135719 aa2br_human Human No 6.8 IC50 = 180 nM Funct
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
513 7 1 8 5.3 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12
CHEMBL4130003 aa2br_human Human No 5.7 IC50 = 1810 nM Funct
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
271 3 2 6 2.6 Cc1nc2c(N)nc(NCc3ccccc3)nc2s1
CHEMBL574489 aa2br_human Human No 5.7 IC50 = 1810 nM Funct
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
421 7 1 9 3.8 CCCCn1cc2c(nc(NC(=O)Cc3cccs3)n3nc(-c4ccco4)nc23)n1
CHEMBL285900 aa2br_human Human No 6.7 IC50 = 185 nM Funct
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
555 11 2 9 3.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(OCc5ccccc5)cc4)nn3C)[nH]c2n(CCC)c1=O
CHEMBL3984266 aa2br_human Human No 6.7 IC50 = 185 nM Funct
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
289 5 2 7 3.1 CCCCNc1nc(N)c2nc(-c3ccco3)sc2n1
CHEMBL410895 aa2br_human Human No 6.7 IC50 = 188 nM Funct
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
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
CHEMBL1078030 aa2br_human Human No 6.7 IC50 = 189 nM Funct
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
339 4 1 6 2.9 O=C(c1nc(NCc2cccnc2)nc2ccsc12)N1CCCC1
CHEMBL1172270 aa2br_human Human No 7.7 IC50 = 19 nM Funct
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
401 5 1 5 4.5 COc1ccc(N(C(C)=O)C(C)C)c2sc(NC(=O)c3ccc(F)cc3)nc12
CHEMBL1172275 aa2br_human Human No 7.7 IC50 = 19 nM Funct
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
435 6 1 7 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4ccnc4)cc3)sc12
CHEMBL1172277 aa2br_human Human No 7.7 IC50 = 19 nM Funct
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
490 8 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(CN(C)S(C)(=O)=O)cc3)sc12
CHEMBL1077915 aa2br_human Human No 7.7 IC50 = 19 nM Funct
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
380 5 1 7 4.9 Cc1ccc(C(=O)c2nc(NC(C)c3ccccn3)nc3ccsc23)s1
CHEMBL1080421 aa2br_human Human No 7.7 IC50 = 19 nM Funct
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
395 7 2 8 4.4 CCNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1
CHEMBL1760891 aa2br_human Human No 7.7 IC50 = 19 nM Funct
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
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
CHEMBL1789250 aa2br_human Human No 7.7 IC50 = 19 nM Funct
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
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
CHEMBL4553423 aa2br_human Human No 6.7 IC50 = 190 nM Bind
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
452 8 0 9 2.4 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)c3cn(C)cn3)sc21
CHEMBL132806 aa2br_human Human No 6.7 IC50 = 190 nM Funct
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
429 7 1 8 4.0 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1
CHEMBL97753 aa2br_human Human No 5.7 IC50 = 1900 nM Funct
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
399 6 2 7 3.4 O=C(O)CCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12
CHEMBL1258622 aa2br_human Human No 4.7 IC50 = 19000 nM Funct
Antagonist activity at adenosine A2B receptor by cAMP assayAntagonist activity at adenosine A2B receptor by cAMP assay
489 5 2 6 6.3 Cc1ccccc1-n1nc(C(F)(F)F)c(-c2ccc3nccnc3c2)c1Nc1ccccc1C(=O)O
CHEMBL1955921 aa2br_human Human No 6.7 IC50 = 197 nM Funct
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
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
CHEMBL2030704 aa2br_human Human No 8.7 IC50 = 2.1 nM Funct
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
362 2 0 6 3.9 O=c1c(-c2ccco2)nnc2n(-c3ccc(Cl)cc3)c3ccccc3n12
CHEMBL519390 aa2br_human Human No 8.6 IC50 = 2.3 nM Funct
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
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
CHEMBL4569909 aa2br_human Human No 8.6 IC50 = 2.4 nM Bind
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
438 8 1 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cc3nc[nH]c3C)sc21
CHEMBL2030703 aa2br_human Human No 8.6 IC50 = 2.4 nM Funct
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
372 2 0 5 4.4 O=c1c(-c2ccccc2)nnc2n(-c3ccc(Cl)cc3)c3ccccc3n12
CHEMBL2030705 aa2br_human Human No 8.6 IC50 = 2.5 nM Funct
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
366 4 0 5 4.0 O=c1c(-c2ccccc2)nnc2n(CCc3ccccc3)c3ccccc3n12
CHEMBL1955922 aa2br_human Human No 7.7 IC50 = 20 nM Funct
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
332 5 2 7 0.4 CCCn1c(=O)c2[nH]c(-c3cc(=O)[nH]n3C)nc2n(CCC)c1=O
CHEMBL210457 aa2br_human Human No 7.7 IC50 = 20 nM Bind
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
455 6 2 8 1.1 COc1ccc(CNS(=O)(=O)c2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)nc1
CHEMBL1760901 aa2br_human Human No 7.7 IC50 = 20 nM Funct
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
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
CHEMBL7098 aa2br_human Human No 7.7 IC50 = 20.4 nM Funct
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
266 1 0 6 1.8 Cn1c2ccccc2n2c(=O)c(-c3ccco3)nnc12
CHEMBL438938 aa2br_human Human No 6.7 IC50 = 200 nM Funct
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
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
CHEMBL4450633 aa2br_human Human No 6.7 IC50 = 200 nM Bind
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
443 7 1 8 1.2 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)N3CC(O)C3)sc21
CHEMBL4452532 aa2br_human Human No 6.7 IC50 = 200 nM Bind
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
427 8 0 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(CN3CCCC3)sc21
CHEMBL4459477 aa2br_human Human No 6.7 IC50 = 200 nM Bind
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
358 6 0 6 2.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C)sc21
CHEMBL4522738 aa2br_human Human No 6.7 IC50 = 200 nM Bind
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
405 4 1 7 1.3 CCn1c(=O)c2c(C)c(C(=O)N3CC(O)C3)sc2n(CCC(F)(F)F)c1=O
CHEMBL4070936 aa2br_human Human No 5.7 IC50 = 2000 nM Bind
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
460 7 2 8 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C(=O)O)c4)c3)nc2n(CCC)c1=O
CHEMBL3968147 aa2br_human Human No 6.7 IC50 = 206 nM Funct
Antagonist activity at adenosine A2b receptor (unknown origin)Antagonist activity at adenosine A2b receptor (unknown origin)
693 16 4 8 6.5 CCn1nc(-c2cccc(-c3cccc(C(=O)NCCCCCCCN(C)CCO)c3)c2)cc(NC(=O)Nc2c(Cl)cncc2Cl)c1=O
CHEMBL1927428 aa2br_human Human No 4.7 IC50 = 20600 nM Funct
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
374 6 3 10 1.7 CC(C)(C)OC(=O)NCCCNc1nc(N)n2nc(-c3ccco3)nc2n1
CHEMBL2070886 aa2br_human Human No 5.7 IC50 = 2061 nM Funct
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
471 5 2 9 3.1 Cn1cc2c(nc(NC(=O)NC3CCN(Cc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL4127395 aa2br_human Human No 5.7 IC50 = 2072 nM Funct
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
277 3 2 7 2.7 Cc1nc2c(N)nc(NCc3cccs3)nc2s1
CHEMBL127876 aa2br_human Human No 5.7 IC50 = 2080 nM Bind
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cccc(Cl)c2)CC1
CHEMBL1170134 aa2br_human Human No 7.7 IC50 = 21 nM Funct
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
482 6 1 7 3.4 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCOCC4)cc3)sc12
CHEMBL1170136 aa2br_human Human No 7.7 IC50 = 21 nM Funct
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
435 6 1 7 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4cccn4)cc3)sc12
CHEMBL1170367 aa2br_human Human No 7.7 IC50 = 21 nM Funct
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
373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccnn3C)sc12
CHEMBL1170582 aa2br_human Human No 7.7 IC50 = 21 nM Funct
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
426 6 2 6 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)NC)cc3)sc12
CHEMBL1171162 aa2br_human Human No 7.7 IC50 = 21 nM Funct
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
359 5 2 6 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cn[nH]c3)sc12
CHEMBL1170367 aa2br_human Human No 7.7 IC50 = 21 nM Funct
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
373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccnn3C)sc12
CHEMBL4540558 aa2br_human Human No 6.7 IC50 = 210 nM Bind
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
362 6 0 6 2.6 COCCn1c(=O)n(CCc2ccccc2F)c(=O)c2c(C)csc21
CHEMBL541455 aa2br_human Human No 6.7 IC50 = 210 nM Funct
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
463 7 1 8 4.2 O=C(Cc1ccccc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12
CHEMBL62350 aa2br_human Human Yes 6.7 IC50 = 210 nM Funct
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
256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O
CHEMBL4443243 aa2br_human Human No 5.7 IC50 = 2100 nM Bind
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
388 7 1 7 2.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)O)sc21
CHEMBL261028 aa2br_human Human No 6.7 IC50 = 212 nM Funct
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
463 8 2 8 2.8 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(C)cc4)n3)nc2n(CCC)c1=O
CHEMBL2071048 aa2br_human Human No 5.7 IC50 = 2122 nM Funct
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
528 5 3 9 3.1 Cc1ccc(CNC(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)cc1
CHEMBL2071051 aa2br_human Human No 5.7 IC50 = 2144 nM Funct
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
507 3 2 10 1.2 CN1CCN(C(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)CC1
CHEMBL2079181 aa2br_human Human No 5.7 IC50 = 2144 nM Funct
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
507 3 2 10 1.2 CN1CCN(C(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)CC1
CHEMBL1079142 aa2br_human Human No 6.7 IC50 = 215 nM Funct
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
360 5 1 6 4.2 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)cc1
CHEMBL1955913 aa2br_human Human No 6.7 IC50 = 219 nM Funct
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
520 10 1 12 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4noc(-c5cccc(OC)c5)n4)nn3C)nc2n(CCC)c1=O
CHEMBL1955905 aa2br_human Human No 6.7 IC50 = 220 nM Funct
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
506 9 3 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(=O)O)ccc5[nH]4)nn3C)nc2n(CCC)c1=O
CHEMBL4440686 aa2br_human Human No 6.7 IC50 = 220 nM Bind
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
294 4 0 6 1.4 CCn1c(=O)c2c3c(sc2n(CCOC)c1=O)CCC3
CHEMBL50051 aa2br_rat Rat No 6.7 IC50 = 220 nM Funct
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
337 1 2 7 2.3 Cn1c(-c2ccco2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21
CHEMBL3752514 aa2br_human Human No 5.7 IC50 = 2214 nM Funct
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
307 4 2 8 2.0 Nc1nc(NCc2ccccc2)nc2nc(-c3ccco3)nn12
CHEMBL3963331 aa2br_human Human No 6.7 IC50 = 222 nM Funct
Antagonist activity at adenosine A2b receptor (unknown origin)Antagonist activity at adenosine A2b receptor (unknown origin)
523 6 3 6 5.6 CCn1nc(-c2cccc(-c3cccc(C(=O)O)c3)c2)cc(NC(=O)Nc2c(Cl)cncc2Cl)c1=O
CHEMBL409736 aa2br_human Human No 6.7 IC50 = 222 nM Funct
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
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
CHEMBL1170130 aa2br_human Human No 7.6 IC50 = 23 nM Funct
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
391 4 1 4 4.7 CCN(C(C)=O)c1ccc(Cl)c2nc(NC(=O)c3ccc(F)cc3)sc12
CHEMBL1171718 aa2br_human Human No 7.6 IC50 = 23 nM Funct
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
415 6 1 5 4.7 COc1ccc(N(CC(C)C)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12
CHEMBL48153 aa2br_human Human No 7.6 IC50 = 23 nM Funct
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
365 1 2 6 2.8 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21
CHEMBL486893 aa2br_human Human No 7.6 IC50 = 23.4 nM Funct
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
552 7 2 9 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O
CHEMBL4203745 aa2br_human Human Yes 7.6 IC50 = 23.5 nM Bind
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
506 7 0 7 2.2 CCCN1C(=O)N=C2N=C(c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)N=C2C1=O
CHEMBL1172268 aa2br_human Human No 6.6 IC50 = 230 nM Funct
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
409 5 1 5 4.3 COc1ccc(N(C(C)=O)C(F)F)c2sc(NC(=O)c3ccc(F)cc3)nc12
CHEMBL4585480 aa2br_human Human No 5.6 IC50 = 2300 nM Bind
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
448 8 0 7 3.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)c3ccccc3)sc21
CHEMBL1955926 aa2br_human Human No 6.6 IC50 = 236 nM Funct
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
508 9 2 10 2.5 CCCn1c(=O)c2[nH]c(-c3cc(OCC(=O)Nc4ccc5c(c4)OCO5)nn3C)cc2n(CCC)c1=O
CHEMBL4128596 aa2br_human Human No 5.6 IC50 = 2387 nM Funct
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
363 5 2 7 4.0 COc1cccc(CNc2nc(N)c3nc(-c4ccccc4)sc3n2)c1
CHEMBL3932413 aa2br_human Human No 7.6 IC50 = 24 nM Funct
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
339 4 3 8 3.2 Nc1nc(NCc2cccc(O)c2)nc2sc(-c3ccco3)nc12
CHEMBL317310 aa2br_human Human No 5.6 IC50 = 2400 nM Bind
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
369 2 1 6 4.2 CC(C)(C)C(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12
CHEMBL96041 aa2br_human Human No 5.6 IC50 = 2410 nM Bind
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
385 2 1 7 4.5 CC(C)(C)OC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12
CHEMBL2070880 aa2br_human Human No 5.6 IC50 = 2428 nM Funct
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
381 3 3 9 1.1 Cn1cc2c(nc(NC(=O)NC3CCNCC3)n3nc(-c4ccco4)nc23)n1
CHEMBL1181982 aa2br_human Human No 6.6 IC50 = 244 nM Funct
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
390 3 2 8 1.7 Cn1cc2c(nc(NC(=O)Nc3ccc[n+](C)c3)n3nc(-c4ccco4)nc23)n1
CHEMBL203660 aa2br_human Human No 6.6 IC50 = 244 nM Funct
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
390 3 2 8 1.7 Cn1cc2c(nc(NC(=O)Nc3ccc[n+](C)c3)n3nc(-c4ccco4)nc23)n1
CHEMBL3317578 aa2br_human Human No 6.6 IC50 = 247 nM Funct
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
345 5 2 6 3.3 Nc1nc(CCCc2ccccc2O)nc2cn(-c3ccccc3)nc12
CHEMBL3917647 aa2br_human Human No 7.6 IC50 = 25 nM Funct
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
353 5 3 8 3.3 Nc1nc(NCCc2cccc(O)c2)nc2sc(-c3ccco3)nc12
CHEMBL339936 aa2br_human Human No 6.6 IC50 = 250 nM Bind
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
419 7 1 7 2.9 COc1ccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1
CHEMBL4452799 aa2br_human Human No 6.6 IC50 = 250 nM Bind
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
442 9 0 7 3.9 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(COC3CCCC3)sc21
CHEMBL203054 aa2br_human Human No 6.6 IC50 = 250 nM Funct
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
414 3 2 9 3.7 Cn1cc2c(nc(NC(=O)Nc3cc4ccccc4o3)n3nc(-c4ccco4)nc23)n1
CHEMBL134566 aa2br_human Human No 6.6 IC50 = 250 nM Funct
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
477 8 1 8 4.5 O=C(Cc1ccccc1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12
CHEMBL48153 aa2br_rat Rat No 6.6 IC50 = 250 nM Funct
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
365 1 2 6 2.8 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21
CHEMBL1935746 aa2br_human Human No 6.6 IC50 = 251 nM Funct
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
358 5 1 7 3.6 Nc1nc2cn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12
CHEMBL1076503 aa2br_human Human No 6.6 IC50 = 256 nM Funct
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
325 5 2 6 2.6 O=C(NC1CC1)c1nc(NCc2cccnc2)nc2ccsc12
CHEMBL1955907 aa2br_human Human No 7.6 IC50 = 26 nM Funct
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
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
CHEMBL1760898 aa2br_human Human No 7.6 IC50 = 26 nM Funct
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
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
CHEMBL4560841 aa2br_human Human No 6.6 IC50 = 260 nM Bind
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
441 7 0 7 2.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)N3CCCC3)sc21
CHEMBL203060 aa2br_human Human No 6.6 IC50 = 260 nM Funct
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
391 3 2 9 1.5 Cn1cc2c(nc(NC(=O)Nc3ccc[n+]([O-])c3)n3nc(-c4ccco4)nc23)n1
CHEMBL3987016 aa2br_human Human Yes 5.6 IC50 = 2600 nM Bind
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
459 6 2 5 4.4 CCS(=O)(=O)Nc1ccc(Oc2ccc(F)cc2F)c(-c2cn(C)c(=O)c3[nH]ccc23)c1
CHEMBL4205635 aa2br_human Human No 6.6 IC50 = 262 nM Funct
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
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
CHEMBL4127213 aa2br_human Human No 5.6 IC50 = 2622 nM Funct
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
363 5 2 7 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3ccccc3)sc2n1
CHEMBL3950249 aa2br_human Human No 6.6 IC50 = 263 nM Funct
Antagonist activity at adenosine A2b receptor (unknown origin)Antagonist activity at adenosine A2b receptor (unknown origin)
537 7 3 6 5.6 CCn1nc(-c2cccc(-c3cccc(CC(=O)O)c3)c2)cc(NC(=O)Nc2c(Cl)cncc2Cl)c1=O
CHEMBL318251 aa2br_human Human No 5.6 IC50 = 2650 nM Bind
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
327 2 1 6 3.1 CC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12
CHEMBL430044 aa2br_human Human No 6.6 IC50 = 266 nM Funct
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
479 9 2 9 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4cccc(OC)c4)n3)nc2n(CCC)c1=O
CHEMBL1935762 aa2br_human Human No 7.6 IC50 = 27 nM Funct
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
345 4 1 8 2.6 Nc1nc2cn(CCc3ccccc3)nc2c2nc(-c3ccco3)nn12
CHEMBL1955924 aa2br_human Human No 7.6 IC50 = 27 nM Funct
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
461 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)nn3C)cc2n(CCC)c1=O
CHEMBL212642 aa2br_human Human No 7.6 IC50 = 27 nM Bind
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
494 5 1 8 1.1 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccncc5)CC4)cc3)cc2n(C)c1=O
CHEMBL95811 aa2br_human Human No 6.6 IC50 = 270 nM Bind
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
370 5 2 7 2.9 NCCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12
CHEMBL122037 aa2br_human Human No 5.6 IC50 = 2700 nM Bind
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.
326 4 1 5 3.7 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(Cl)cc3)nn12
CHEMBL1094143 aa2br_human Human No 6.6 IC50 = 272 nM Funct
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
405 5 1 5 4.8 O=C(Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12)c1ccccc1
CHEMBL4175878 aa2br_human Human No 5.6 IC50 = 2773 nM Funct
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
369 5 2 8 4.0 COc1cccc(CNc2nc(N)c3nc(-c4cccs4)sc3n2)c1
CHEMBL1169934 aa2br_human Human No 7.6 IC50 = 28 nM Funct
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
394 5 1 6 3.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C#N)cc3)sc12
CHEMBL1171349 aa2br_human Human No 7.6 IC50 = 28 nM Funct
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
437 6 1 9 2.9 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4cnnn4)cc3)sc12
CHEMBL1172276 aa2br_human Human No 7.6 IC50 = 28 nM Funct
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
466 7 1 6 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(CN4CCCC4=O)cc3)sc12
CHEMBL4643898 aa2br_human Human No 7.6 IC50 = 28 nM Funct
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
402 5 3 9 2.2 Nc1nc(NCc2ccc(S(N)(=O)=O)cc2)nc2sc(-c3ccco3)nc12
CHEMBL1760895 aa2br_human Human No 7.6 IC50 = 28 nM Funct
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
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
CHEMBL4522981 aa2br_rat Rat Yes 6.6 IC50 = 280 nM Bind
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
433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O
CHEMBL4537687 aa2br_human Human No 6.6 IC50 = 280 nM Bind
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
345 6 0 7 1.8 COCCn1c(=O)n(CCc2cccnc2)c(=O)c2c(C)csc21
CHEMBL1185010 aa2br_human Human No 6.6 IC50 = 280 nM Funct
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
390 3 2 8 1.7 Cn1cc2c(nc(NC(=O)Nc3cccc[n+]3C)n3nc(-c4ccco4)nc23)n1
CHEMBL383689 aa2br_human Human No 6.6 IC50 = 280 nM Funct
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
390 3 2 8 1.7 Cn1cc2c(nc(NC(=O)Nc3cccc[n+]3C)n3nc(-c4ccco4)nc23)n1
CHEMBL4473551 aa2br_human Human No 5.6 IC50 = 2800 nM Bind
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
470 8 0 6 4.6 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(F)(F)c3ccccc3)sc21
CHEMBL3931329 aa2br_human Human No 6.6 IC50 = 283 nM Funct
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
353 5 2 8 3.5 COc1ccc(CNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1
CHEMBL1078001 aa2br_human Human No 6.5 IC50 = 287 nM Funct
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
380 4 1 7 3.9 Cc1ccc(C(=O)c2nc(NC(=O)c3cccnc3)nc3ccsc23)s1
CHEMBL1171163 aa2br_human Human No 7.5 IC50 = 29 nM Funct
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
373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(C)c3)sc12
CHEMBL3800587 aa2br_human Human No 6.5 IC50 = 293 nM Funct
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
335 4 1 7 3.0 COc1cccc(Cn2cc3nc(-c4ccc(C)o4)nc(N)c3n2)c1
CHEMBL2030707 aa2br_human Human No 8.5 IC50 = 3.1 nM Funct
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
372 2 0 5 4.4 O=c1c(-c2ccccc2)nnc2n(-c3ccccc3)c3ccc(Cl)cc3n12
CHEMBL484900 aa2br_human Human No 8.5 IC50 = 3.2 nM Funct
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
526 7 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)[nH]c2c1=O
CHEMBL1077943 aa2br_human Human No 8.5 IC50 = 3.5 nM Funct
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
381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1
CHEMBL486688 aa2br_human Human No 8.5 IC50 = 3.6 nM Funct
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
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
CHEMBL482436 aa2br_human Human Yes 8.4 IC50 = 3.6 nM Funct
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
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
CHEMBL183 aa2br_human Human Yes 8.4 IC50 = 3.8 nM Bind
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
304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1
CHEMBL4448231 aa2br_human Human No 7.5 IC50 = 30 nM Bind
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
450 8 1 7 3.5 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(O)c3ccccc3)sc21
CHEMBL1760897 aa2br_human Human No 7.5 IC50 = 30 nM Funct
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
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
CHEMBL1789197 aa2br_human Human No 7.5 IC50 = 30 nM Funct
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
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
CHEMBL4528081 aa2br_human Human No 6.5 IC50 = 300 nM Bind
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
344 6 0 6 2.4 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)csc21
CHEMBL52735 aa2br_human Human Yes 5.5 IC50 = 3000 nM Funct
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
320 2 0 6 2.2 COC(=O)C1=C2C=CN(C)C=C2c2nc(-c3ccccc3)nn2C1
CHEMBL1079893 aa2br_human Human No 5.5 IC50 = 3073 nM Funct
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
353 4 1 6 3.5 C[C@@H](Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1
CHEMBL1076504 aa2br_human Human No 6.5 IC50 = 309 nM Funct
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
327 5 2 6 2.8 CC(C)NC(=O)c1nc(NCc2cccnc2)nc2ccsc12
CHEMBL1935752 aa2br_human Human No 7.5 IC50 = 31 nM Funct
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
255 1 1 8 0.9 Cn1ncc2nc(N)n3nc(-c4ccco4)nc3c21
CHEMBL3958838 aa2br_human Human Yes 6.5 IC50 = 313 nM Funct
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
353 5 2 8 3.5 COc1ccccc1CNc1nc(N)c2nc(-c3ccco3)sc2n1
CHEMBL3317579 aa2br_human Human No 6.5 IC50 = 314 nM Funct
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
345 5 2 6 3.3 Nc1nc(CCCc2cccc(O)c2)nc2cn(-c3ccccc3)nc12
CHEMBL1935754 aa2br_human Human No 6.5 IC50 = 319 nM Funct
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
345 4 1 8 2.6 Nc1nc2cnn(CCc3ccccc3)c2c2nc(-c3ccco3)nn12
CHEMBL1935757 aa2br_human Human No 7.5 IC50 = 32 nM Funct
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
432 6 2 9 3.8 CCCn1ncc2nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc3c21
CHEMBL1935763 aa2br_human Human No 7.5 IC50 = 32 nM Funct
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
359 5 1 8 2.9 Nc1nc2cn(CCCc3ccccc3)nc2c2nc(-c3ccco3)nn12
CHEMBL1080241 aa2br_human Human No 7.5 IC50 = 32 nM Funct
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
367 5 2 8 3.6 Nc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1
CHEMBL1955909 aa2br_human Human No 7.5 IC50 = 32 nM Funct
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
514 8 2 9 3.4 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)c(F)cc5[nH]4)nn3C)nc2n(CCC)c1=O
CHEMBL3950142 aa2br_human Human No 7.5 IC50 = 32 nM Funct
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
323 4 2 7 3.5 Nc1nc(NCc2ccccc2)nc2sc(-c3ccco3)nc12
CHEMBL2322916 aa2br_human Human No 6.5 IC50 = 320 nM Funct
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
225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1
CHEMBL2322916 aa2br_human Human No 6.5 IC50 = 320 nM Funct
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
225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1
CHEMBL2322916 aa2br_human Human No 6.5 IC50 = 320 nM Funct
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
225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1
CHEMBL203998 aa2br_human Human No 6.5 IC50 = 320 nM Funct
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
391 3 2 9 1.5 Cn1cc2c(nc(NC(=O)Nc3cccc[n+]3[O-])n3nc(-c4ccco4)nc23)n1
CHEMBL2322916 aa2br_human Human No 6.5 IC50 = 320 nM Bind
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
225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1
CHEMBL324100 aa2br_human Human No 5.5 IC50 = 3200 nM Funct
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
328 2 0 6 3.3 O=c1c(-c2ccco2)nnc2n(-c3ccccc3)c3ccccc3n12
CHEMBL375293 aa2br_human Human Yes 6.5 IC50 = 321 nM Funct
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
316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1
CHEMBL286838 aa2br_human Human No 6.5 IC50 = 322 nM Funct
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
472 8 1 10 0.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)N4CCN(C)CC4)nn3C)[nH]c2n(CCC)c1=O
CHEMBL3963278 aa2br_human Human No 6.5 IC50 = 323 nM Funct
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
275 4 2 7 2.8 CCCNc1nc(N)c2nc(-c3ccco3)sc2n1
CHEMBL2071050 aa2br_human Human No 5.5 IC50 = 3235 nM Funct
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
501 4 3 10 2.5 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)Nc4ccncc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL2078766 aa2br_human Human No 5.5 IC50 = 3235 nM Funct
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
501 4 3 10 2.5 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)Nc4ccncc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL2071049 aa2br_human Human No 5.5 IC50 = 3244 nM Funct
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
544 6 3 10 2.8 COc1ccc(CNC(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)cc1
CHEMBL1935760 aa2br_human Human No 7.5 IC50 = 33 nM Funct
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
255 1 1 8 0.9 Cn1cc2nc(N)n3nc(-c4ccco4)nc3c2n1
CHEMBL1171526 aa2br_human Human No 7.5 IC50 = 33 nM Funct
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
417 7 1 6 3.7 COCCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12
CHEMBL4175676 aa2br_human Human No 7.5 IC50 = 33 nM Funct
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
324 4 2 8 2.9 Nc1nc(NCc2ccncc2)nc2sc(-c3ccco3)nc12
CHEMBL4444370 aa2br_human Human No 5.5 IC50 = 3300 nM Bind
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
378 6 0 6 3.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cl)sc21
CHEMBL3317576 aa2br_human Human No 6.5 IC50 = 334 nM Funct
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
359 6 1 6 3.6 COc1cccc(CCCc2nc(N)c3nn(-c4ccccc4)cc3n2)c1
CHEMBL4642713 aa2br_human Human No 6.5 IC50 = 334 nM Funct
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
450 5 1 10 3.4 CCOC(=O)c1ccc(N2CCN(c3nc(N)c4nc(-c5ccco5)sc4n3)CC2)cc1
CHEMBL4632532 aa2br_human Human No 7.5 IC50 = 34 nM Funct
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
416 6 3 9 2.2 Nc1nc(NCCc2ccc(S(N)(=O)=O)cc2)nc2sc(-c3ccco3)nc12
CHEMBL4517977 aa2br_human Human No 5.5 IC50 = 3400 nM Bind
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
380 5 1 6 2.9 Cc1[nH]cnc1Cn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)csc21
CHEMBL375293 aa2br_mouse Mouse Yes 6.5 IC50 = 349 nM Funct
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
316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1
CHEMBL1172274 aa2br_human Human No 7.5 IC50 = 35 nM Funct
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
427 6 1 7 3.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)OC)cc3)sc12
CHEMBL1955904 aa2br_human Human No 7.5 IC50 = 35 nM Funct
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
534 10 2 11 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(=O)OCC)ccc5[nH]4)nn3C)nc2n(CCC)c1=O
CHEMBL1170518 aa2br_human Human No 6.5 IC50 = 350 nM Funct
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
359 4 2 5 3.7 COc1ccc(NC(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12
CHEMBL1170525 aa2br_human Human No 6.5 IC50 = 350 nM Funct
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
430 6 2 6 2.8 CNC(=O)CN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12
CHEMBL1170518 aa2br_human Human No 6.5 IC50 = 350 nM Funct
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
359 4 2 5 3.7 COc1ccc(NC(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12
CHEMBL4128787 aa2br_human Human No 5.5 IC50 = 3516 nM Funct
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
301 4 2 7 2.6 COc1cccc(CNc2nc(N)c3nc(C)sc3n2)c1
CHEMBL3797666 aa2br_human Human No 6.5 IC50 = 354 nM Funct
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
323 3 1 6 3.2 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4F)cc3n2)o1
CHEMBL4128138 aa2br_human Human No 6.5 IC50 = 358 nM Funct
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
333 4 2 6 3.9 Nc1nc(NCc2ccccc2)nc2sc(-c3ccccc3)nc12
CHEMBL1170129 aa2br_human Human No 7.4 IC50 = 36 nM Funct
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
447 6 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(S(C)(=O)=O)cc3)sc12
CHEMBL3952824 aa2br_human Human No 7.4 IC50 = 36.7 nM Funct
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
380 6 1 7 4.6 CCc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1
CHEMBL578224 aa2br_human Human No 6.4 IC50 = 363 nM Funct
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
449 5 1 8 4.0 Cn1cc2c(nc(NC(=O)C(c3ccccc3)c3ccccc3)n3nc(-c4ccco4)nc23)n1
CHEMBL124485 aa2br_human Human No 5.4 IC50 = 3660 nM Bind
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccc(Cl)cc2)CC1
CHEMBL1077750 aa2br_human Human No 5.4 IC50 = 3672 nM Funct
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
288 3 0 5 3.9 CCc1nc(C(=O)c2ccc(C)s2)c2sccc2n1
CHEMBL3941862 aa2br_human Human No 6.4 IC50 = 368 nM Funct
Antagonist activity at adenosine A2b receptor (unknown origin)Antagonist activity at adenosine A2b receptor (unknown origin)
678 12 4 8 5.4 CCNC(=O)c1cc(C(=O)NCCCN(C)C)cc(-c2cccc(-c3cc(NC(=O)Nc4c(Cl)cncc4Cl)c(=O)n(CC)n3)c2)c1
CHEMBL1170137 aa2br_human Human No 7.4 IC50 = 37 nM Funct
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
462 7 2 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(NS(C)(=O)=O)cc3)sc12
CHEMBL4128862 aa2br_human Human No 5.4 IC50 = 3725 nM Funct
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
257 2 2 6 2.7 Cc1nc2c(N)nc(Nc3ccccc3)nc2s1
CHEMBL1170583 aa2br_human Human No 7.4 IC50 = 38 nM Funct
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
495 6 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCN(C)CC4)cc3)sc12
CHEMBL260331 aa2br_human Human Yes 7.4 IC50 = 38 nM Funct
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
509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2
CHEMBL1955902 aa2br_human Human No 7.4 IC50 = 38 nM Funct
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
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
CHEMBL260331 aa2br_human Human Yes 7.4 IC50 = 38 nM Funct
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
509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2
CHEMBL3317575 aa2br_human Human No 6.4 IC50 = 387 nM Funct
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
359 6 1 6 3.6 COc1ccccc1CCCc1nc(N)c2nn(-c3ccccc3)cc2n1
CHEMBL3935610 aa2br_human Human No 6.4 IC50 = 389 nM Funct
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
337 5 2 7 3.6 Nc1nc(NCCc2ccccc2)nc2sc(-c3ccco3)nc12
CHEMBL4168980 aa2br_human Human No 6.4 IC50 = 389 nM Funct
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
367 5 2 8 3.9 COc1ccccc1CNc1nc(N)c2nc(-c3ccc(C)o3)sc2n1
CHEMBL1081160 aa2br_human Human No 7.4 IC50 = 39 nM Funct
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
395 6 1 8 4.1 CN(C)c1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1
CHEMBL4458042 aa2br_human Human No 7.4 IC50 = 39 nM Bind
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
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
CHEMBL4453228 aa2br_human Human No 6.4 IC50 = 390 nM Bind
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
308 4 0 6 1.8 CCn1c(=O)c2c3c(sc2n(CCOC)c1=O)CCCC3
CHEMBL4536104 aa2br_human Human No 6.4 IC50 = 390 nM Bind
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
431 8 0 8 2.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)N(C)OC)sc21
CHEMBL3799921 aa2br_human Human No 6.4 IC50 = 395 nM Funct
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
321 3 2 7 2.7 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4O)cc3n2)o1
CHEMBL211813 aa2br_human Human No 8.4 IC50 = 4 nM Bind
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
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
CHEMBL4162638 aa2br_human Human No 8.4 IC50 = 4.2 nM Funct
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
338 5 2 8 3.0 Nc1nc(NCCc2cccnc2)nc2sc(-c3ccco3)nc12
CHEMBL519813 aa2br_human Human No 8.4 IC50 = 4.5 nM Funct
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
494 6 2 7 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O
CHEMBL1935753 aa2br_human Human No 7.4 IC50 = 40 nM Funct
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
283 3 1 8 1.7 CCCn1ncc2nc(N)n3nc(-c4ccco4)nc3c21
CHEMBL1172269 aa2br_human Human No 7.4 IC50 = 40 nM Funct
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
441 5 1 5 4.6 COc1ccc(N(CC(F)(F)F)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12
CHEMBL33491 aa2br_human Human No 7.4 IC50 = 40 nM Funct
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
493 9 2 9 2.7 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)C)C
CHEMBL189904 aa2br_human Human No 6.4 IC50 = 400 nM Funct
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
336 4 0 6 2.2 CCCn1c(=O)c2c(nc3n2CC(C)=C3)n(Cc2ccccc2)c1=O
CHEMBL4522981 aa2br_mouse Mouse Yes 6.4 IC50 = 400 nM Bind
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
433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O
CHEMBL189904 aa2br_human Human No 6.4 IC50 = 400 nM Funct
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
336 4 0 6 2.2 CCCn1c(=O)c2c(nc3n2CC(C)=C3)n(Cc2ccccc2)c1=O
CHEMBL4128190 aa2br_human Human No 5.4 IC50 = 4017 nM Funct
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
365 5 2 9 2.7 COc1ccccc1CNc1nc(N)c2nc(-c3cnccn3)sc2n1
CHEMBL1760887 aa2br_human Human No 7.4 IC50 = 41 nM Funct
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
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
CHEMBL49925 aa2br_rat Rat No 6.4 IC50 = 410 nM Funct
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
372 1 2 7 2.5 Cn1c(-c2cccc(C#N)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21
CHEMBL1078347 aa2br_human Human No 6.4 IC50 = 414 nM Funct
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
379 5 1 6 5.5 Cc1ccc(C(=O)c2nc(NC(C)c3ccccc3)nc3ccsc23)s1
CHEMBL1078087 aa2br_human Human No 5.4 IC50 = 4142 nM Funct
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
380 5 0 7 4.3 Cc1ccc(C(=O)c2nc(N(C)Cc3cccnc3)nc3ccsc23)s1
CHEMBL62350 aa2br_human Human Yes 6.4 IC50 = 415 nM Bind
Inhibitory activity against cyclic AMP production in human Adenosine A2B receptor assayInhibitory activity against cyclic AMP production in human Adenosine A2B receptor assay
256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O
CHEMBL1935743 aa2br_human Human No 7.4 IC50 = 42 nM Funct
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
254 1 1 7 1.5 Cn1cc2nc(N)n3nc(-c4ccco4)nc3c2c1
CHEMBL1171524 aa2br_human Human No 7.4 IC50 = 42 nM Funct
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
417 7 2 6 3.4 COc1ccc(N(CCCO)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12
CHEMBL4449139 aa2br_human Human No 7.4 IC50 = 42 nM Bind
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
443 9 0 7 2.9 CCN(CC)C(=O)c1sc2c(c1C)c(=O)n(CCc1ccccc1)c(=O)n2CCOC
CHEMBL1760885 aa2br_human Human No 7.4 IC50 = 42 nM Funct
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
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
CHEMBL2322918 aa2br_human Human No 6.4 IC50 = 420 nM Funct
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
301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12
CHEMBL2322918 aa2br_human Human No 6.4 IC50 = 420 nM Funct
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
301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12
CHEMBL2322918 aa2br_human Human No 6.4 IC50 = 420 nM Funct
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
301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12
CHEMBL2322918 aa2br_human Human No 6.4 IC50 = 420 nM Bind
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
301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12
CHEMBL297685 aa2br_rat Rat No 6.4 IC50 = 420 nM Funct
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
351 1 2 6 2.4 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCC3)nc21
CHEMBL3798214 aa2br_human Human No 6.4 IC50 = 421 nM Funct
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
323 3 1 6 3.2 Cc1ccc(-c2nc(N)c3nn(Cc4cccc(F)c4)cc3n2)o1
CHEMBL183 aa2br_human Human Yes 7.4 IC50 = 43 nM Funct
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
304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1
CHEMBL258571 aa2br_human Human No 7.4 IC50 = 43 nM Funct
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
483 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Cl)cc4)n3)nc2n(CCC)c1=O
CHEMBL1078348 aa2br_human Human No 7.4 IC50 = 43 nM Funct
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
366 5 1 7 4.3 Cc1ccc(C(=O)c2nc(NCc3ccccn3)nc3ccsc23)s1
CHEMBL1955925 aa2br_human Human No 7.4 IC50 = 43 nM Funct
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
482 9 2 8 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)cc2n(CCC)c1=O
CHEMBL211347 aa2br_human Human No 7.4 IC50 = 43 nM Bind
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
507 6 2 7 2.2 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccccc5)CC4)cc3)cc2n(C)c1=O
CHEMBL4446433 aa2br_human Human No 6.4 IC50 = 430 nM Bind
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
387 7 1 7 1.5 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(N)=O)sc21
CHEMBL3317574 aa2br_human Human No 6.4 IC50 = 432 nM Funct
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
329 5 1 5 3.6 Nc1nc(CCCc2ccccc2)nc2cn(-c3ccccc3)nc12
CHEMBL3752621 aa2br_human Human No 5.4 IC50 = 4360 nM Funct
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
426 6 3 8 4.0 O=C(Nc1ccccc1)Nc1nc(NCc2ccccc2)nc2nc(-c3ccco3)nn12
CHEMBL4127351 aa2br_human Human No 5.4 IC50 = 4380 nM Funct
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
347 5 2 6 4.0 Nc1nc(NCCc2ccccc2)nc2sc(-c3ccccc3)nc12
CHEMBL1760894 aa2br_human Human No 7.4 IC50 = 44 nM Funct
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
534 7 1 6 5.5 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)C3CCN(Cc4cccc(C(F)(F)F)c4)CC3)sc12
CHEMBL2322917 aa2br_human Human No 6.4 IC50 = 440 nM Funct
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
287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12
CHEMBL2322917 aa2br_human Human No 6.4 IC50 = 440 nM Funct
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
287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12
CHEMBL2322917 aa2br_human Human No 6.4 IC50 = 440 nM Funct
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
287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12
CHEMBL4475483 aa2br_human Human No 6.4 IC50 = 440 nM Bind
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
380 6 0 6 3.0 COCCn1c(=O)n(CC(F)(F)c2ccccc2)c(=O)c2c(C)csc21
CHEMBL4569387 aa2br_human Human No 6.4 IC50 = 440 nM Bind
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
282 4 0 6 1.5 CCn1c(=O)c2c(C)c(C)sc2n(CCOC)c1=O
CHEMBL2322917 aa2br_human Human No 6.4 IC50 = 440 nM Bind
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
287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12
CHEMBL296389 aa2br_rat Rat No 6.4 IC50 = 440 nM Funct
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
379 1 2 6 3.2 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCCC3)nc21
CHEMBL301512 aa2br_rat Rat No 6.4 IC50 = 440 nM Funct
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
365 1 2 6 2.8 Cn1c(-c2ccccc2F)nc2c(N)nc(C#CC3(O)CCCCC3)nc21
CHEMBL52432 aa2br_rat Rat No 5.4 IC50 = 4400 nM Funct
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
271 0 2 6 1.0 Cn1cnc2c(N)nc(C#CC3(O)CCCCC3)nc21
CHEMBL1935761 aa2br_human Human No 7.4 IC50 = 45 nM Funct
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
283 3 1 8 1.7 CCCn1cc2nc(N)n3nc(-c4ccco4)nc3c2n1
CHEMBL1955903 aa2br_human Human No 7.4 IC50 = 45 nM Funct
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
476 8 2 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C)ccc5[nH]4)nn3C)nc2n(CCC)c1=O
CHEMBL1078086 aa2br_human Human No 6.4 IC50 = 450 nM Funct
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
380 6 1 7 4.3 Cc1ccc(C(=O)c2nc(NCCc3cccnc3)nc3ccsc23)s1
CHEMBL3904408 aa2br_human Human No 6.3 IC50 = 452 nM Funct
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
353 5 2 8 3.5 COc1cccc(CNc2nc(N)c3nc(-c4ccco4)sc3n2)c1
CHEMBL4162037 aa2br_human Human No 5.3 IC50 = 4571 nM Funct
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
369 5 2 8 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3cccs3)sc2n1
CHEMBL3896989 aa2br_human Human No 6.3 IC50 = 459 nM Funct
Antagonist activity at adenosine A2b receptor (unknown origin)Antagonist activity at adenosine A2b receptor (unknown origin)
707 17 4 8 6.5 CCn1nc(-c2cccc(-c3cccc(CC(=O)NCCCCCCCN(C)CCO)c3)c2)cc(NC(=O)Nc2c(Cl)cncc2Cl)c1=O
CHEMBL1935745 aa2br_human Human No 7.3 IC50 = 46 nM Funct
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
344 4 1 7 3.2 Nc1nc2cn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12
CHEMBL33305 aa2br_human Human No 7.3 IC50 = 46 nM Funct
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
525 11 2 11 2.1 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(OC)c(OC)c4)nn3C)[nH]c2n(CCC)c1=O
CHEMBL1079117 aa2br_human Human No 6.3 IC50 = 468 nM Funct
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
350 5 1 7 3.8 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)o1
CHEMBL3907658 aa2br_human Human No 7.3 IC50 = 47 nM Funct
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
367 6 2 8 3.6 COc1cccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)c1
CHEMBL4437132 aa2br_human Human No 5.3 IC50 = 4700 nM Bind
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
330 6 0 6 2.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2ccsc21
CHEMBL444787 aa2br_human Human No 6.3 IC50 = 477 nM Funct
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
588 9 2 8 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)nc3)[nH]c2n(CCC)c1=O
CHEMBL113142 aa2br_human Human Yes 7.3 IC50 = 48 nM Funct
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
337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1
CHEMBL4543255 aa2br_human Human No 6.3 IC50 = 480 nM Bind
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
286 3 1 4 2.3 Cc1csc2[nH]c(=O)n(CCc3ccccc3)c(=O)c12
CHEMBL3908770 aa2br_human Human No 6.3 IC50 = 482 nM Funct
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
353 5 3 8 3.3 Nc1nc(NCCc2ccc(O)cc2)nc2sc(-c3ccco3)nc12
CHEMBL1079116 aa2br_human Human No 6.3 IC50 = 487 nM Funct
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
386 5 1 7 4.6 O=C(c1ccc(Cl)s1)c1nc(NCc2cccnc2)nc2ccsc12
CHEMBL1760893 aa2br_human Human No 7.3 IC50 = 49 nM Funct
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
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
CHEMBL296389 aa2br_human Human No 7.3 IC50 = 49 nM Funct
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
379 1 2 6 3.2 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCCC3)nc21
CHEMBL1096754 aa2br_human Human No 7.3 IC50 = 49.8 nM Funct
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
329 3 1 5 3.3 Cn1cc2c(NC(=O)c3ccccc3)nc(-c3ccccc3)nc2n1
CHEMBL4475461 aa2br_human Human No 6.3 IC50 = 490 nM Bind
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
384 6 0 6 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c3c(sc21)CCCC3
CHEMBL51107 aa2br_rat Rat No 6.3 IC50 = 490 nM Funct
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
381 1 2 6 3.3 Cn1c(-c2cccc(Cl)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21
CHEMBL4448896 aa2br_human Human No 5.3 IC50 = 4900 nM Bind
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
420 7 0 6 4.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(-c3ccccc3)sc21
CHEMBL4562969 aa2br_human Human No 5.3 IC50 = 4900 nM Bind
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
316 5 0 6 2.0 COCCn1c(=O)n(CC=C(F)F)c(=O)c2c(C)csc21
CHEMBL574775 aa2br_human Human No 6.3 IC50 = 491 nM Funct
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
477 7 1 8 4.9 CCCn1cc2c(nc(NC(=O)C(c3ccccc3)c3ccccc3)n3nc(-c4ccco4)nc23)n1
CHEMBL1081334 aa2br_human Human No 6.3 IC50 = 495 nM Funct
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
299 4 2 6 2.1 CNC(=O)c1nc(NCc2cccnc2)nc2ccsc12
CHEMBL4632532 aa2br_human Human No 8.3 IC50 = 5.2 nM Funct
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
416 6 3 9 2.2 Nc1nc(NCCc2ccc(S(N)(=O)=O)cc2)nc2sc(-c3ccco3)nc12
CHEMBL482648 aa2br_human Human No 8.3 IC50 = 5.3 nM Funct
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
524 7 2 8 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O
CHEMBL483065 aa2br_human Human No 8.3 IC50 = 5.3 nM Funct
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
538 6 2 9 1.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O
CHEMBL2030706 aa2br_human Human No 8.3 IC50 = 5.3 nM Funct
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
356 4 0 6 3.5 O=c1c(-c2ccco2)nnc2n(CCc3ccccc3)c3ccccc3n12
CHEMBL334325 aa2br_human Human No 7.3 IC50 = 50 nM Bind
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
419 7 1 7 2.9 COc1cccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)c1
CHEMBL4462879 aa2br_human Human No 7.3 IC50 = 50 nM Bind
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
421 7 1 7 2.0 CCN(CCO)C(=O)c1sc2c(c1C)c(=O)n(CC)c(=O)n2CCC(F)(F)F
CHEMBL51353 aa2br_human Human No 6.3 IC50 = 500 nM Funct
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
381 1 2 6 3.3 Cn1c(-c2ccc(Cl)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21
CHEMBL576017 aa2br_human Human No 4.3 IC50 = 50000 nM Funct
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
511 8 1 8 5.2 O=C(Cc1cccc(Cl)c1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12
CHEMBL4129565 aa2br_human Human No 5.3 IC50 = 5013 nM Funct
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
365 5 2 9 2.7 COc1cccc(CNc2nc(N)c3nc(-c4cnccn4)sc3n2)c1
CHEMBL2071047 aa2br_human Human No 6.3 IC50 = 505 nM Funct
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
548 5 3 9 3.4 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccc(Cl)cc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL578005 aa2br_human Human No 5.3 IC50 = 5060 nM Funct
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
447 7 1 8 4.1 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1
CHEMBL1955917 aa2br_human Human No 7.3 IC50 = 51 nM Funct
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
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
CHEMBL113142 aa2br_human Human Yes 7.3 IC50 = 51 nM Funct
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
337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1
CHEMBL300624 aa2br_rat Rat No 6.3 IC50 = 510 nM Funct
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
325 1 2 6 1.9 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC(C)(C)O)nc21
CHEMBL1079141 aa2br_human Human No 6.3 IC50 = 511 nM Funct
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
346 5 1 6 3.9 O=C(c1ccccc1)c1nc(NCc2cccnc2)nc2ccsc12
CHEMBL3798766 aa2br_human Human No 6.3 IC50 = 512 nM Funct
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
321 4 1 7 2.7 COc1ccccc1Cn1cc2nc(-c3ccco3)nc(N)c2n1
CHEMBL1672627 aa2br_mouse Mouse Yes 6.3 IC50 = 512 nM Funct
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
335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2cccnc2)n1)C1CC1
CHEMBL3973260 aa2br_human Human No 7.3 IC50 = 52.3 nM Funct
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
378 6 1 7 4.6 C=Cc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1
CHEMBL4451942 aa2br_human Human No 6.3 IC50 = 520 nM Bind
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
370 5 0 6 3.0 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CC1CCCO1
CHEMBL1955910 aa2br_human Human No 7.3 IC50 = 53 nM Funct
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
490 8 2 9 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C)c(C)cc5[nH]4)nn3C)nc2n(CCC)c1=O
CHEMBL1098108 aa2br_human Human No 7.3 IC50 = 53.9 nM Funct
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
359 4 1 6 3.3 COc1ccc(C(=O)Nc2nc(-c3ccccc3)nc3nn(C)cc23)cc1
CHEMBL48682 aa2br_rat Rat No 5.3 IC50 = 5300 nM Funct
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
243 1 1 5 1.8 Cn1c(-c2cccc(F)c2)nc2c(N)ncnc21
CHEMBL577135 aa2br_human Human No 5.3 IC50 = 5370 nM Funct
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
451 6 1 8 4.5 CCCn1cc2c(nc(NC(=O)Cc3ccc4ccccc4c3)n3nc(-c4ccco4)nc23)n1
CHEMBL1079059 aa2br_human Human No 5.3 IC50 = 5376 nM Funct
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
260 2 0 5 3.3 Cc1ccc(C(=O)c2ncnc3ccsc23)s1
CHEMBL1955900 aa2br_human Human No 7.3 IC50 = 54 nM Funct
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
492 9 2 10 2.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(OC)ccc5[nH]4)nn3C)nc2n(CCC)c1=O
CHEMBL326752 aa2br_human Human Yes 7.3 IC50 = 54.3 nM Funct
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
352 3 0 5 3.8 O=c1c(-c2ccccc2)nnc2n(Cc3ccccc3)c3ccccc3n12
CHEMBL4541543 aa2br_human Human No 6.3 IC50 = 540 nM Bind
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
434 8 0 6 4.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cc3ccccc3)sc21
CHEMBL51192 aa2br_rat Rat No 6.3 IC50 = 540 nM Funct
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
353 3 2 6 2.7 CCC(O)(C#Cc1nc(N)c2nc(-c3cccc(F)c3)n(C)c2n1)CC
CHEMBL4168016 aa2br_human Human No 6.3 IC50 = 547 nM Funct
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
345 4 2 8 4.1 Nc1nc(NCc2cccs2)nc2sc(-c3cccs3)nc12
CHEMBL1935766 aa2br_human Human No 6.3 IC50 = 548 nM Funct
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
494 7 2 9 4.6 COc1ccc(NC(=O)Nc2nc3cn(CCc4ccccc4)nc3c3nc(-c4ccco4)nn23)cc1
CHEMBL574263 aa2br_human Human No 5.3 IC50 = 5480 nM Funct
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
497 7 1 8 5.0 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(C(F)(F)F)cc3)n3nc(-c4ccco4)nc23)n1
CHEMBL1078349 aa2br_human Human No 7.3 IC50 = 55 nM Funct
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
366 5 1 7 4.3 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)s1
CHEMBL4589448 aa2br_human Human No 7.3 IC50 = 55 nM Bind
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
383 5 0 6 3.1 Cc1csc2c1c(=O)n(CCc1cccnc1)c(=O)n2CCC(F)(F)F
CHEMBL3934626 aa2br_human Human No 6.3 IC50 = 553 nM Funct
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
367 6 2 8 3.6 COc1ccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1
CHEMBL4128638 aa2br_human Human No 5.3 IC50 = 5538 nM Funct
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
301 4 2 7 2.6 COc1ccccc1CNc1nc(N)c2nc(C)sc2n1
CHEMBL1077985 aa2br_human Human No 5.3 IC50 = 5577 nM Funct
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
365 5 1 6 4.9 Cc1ccc(C(=O)c2nc(NCc3ccccc3)nc3ccsc23)s1
CHEMBL4474572 aa2br_human Human No 7.3 IC50 = 56 nM Bind
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
382 5 0 5 3.7 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CCC(F)(F)F
CHEMBL52276 aa2br_human Human No 5.3 IC50 = 5600 nM Funct
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
415 1 2 6 3.7 Cn1c(-c2cccc(C(F)(F)F)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21
CHEMBL1082063 aa2br_human Human No 6.2 IC50 = 571 nM Funct
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
367 5 2 6 3.8 O=C(NC1CCCCC1)c1nc(NCc2cccnc2)nc2ccsc12
CHEMBL7909 aa2br_human Human No 7.2 IC50 = 58 nM Funct
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
276 1 0 5 2.2 Cn1c2ccccc2n2c(=O)c(-c3ccccc3)nnc12
CHEMBL261810 aa2br_human Human No 7.2 IC50 = 58 nM Funct
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
449 8 2 8 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccccc4)n3)nc2n(CCC)c1=O
CHEMBL4644153 aa2br_human Human No 7.2 IC50 = 58 nM Funct
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
457 4 2 10 1.9 Nc1nc(N2CCN(c3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12
CHEMBL1935764 aa2br_human Human No 6.2 IC50 = 580 nM Funct
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
404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3cn(C)nc3c3nc(-c4ccco4)nn23)cc1
CHEMBL125670 aa2br_human Human No 5.2 IC50 = 5830 nM Bind
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2Cl)CC1
CHEMBL573780 aa2br_human Human No 5.2 IC50 = 5840 nM Funct
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
539 8 1 8 5.7 O=C(Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12)C(c1ccccc1)c1ccccc1
CHEMBL4522981 aa2br_human Human Yes 7.2 IC50 = 59 nM Bind
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
433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O
CHEMBL1935755 aa2br_human Human No 6.2 IC50 = 595 nM Funct
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
359 5 1 8 2.9 Nc1nc2cnn(CCCc3ccccc3)c2c2nc(-c3ccco3)nn12
CHEMBL1171164 aa2br_human Human No 8.2 IC50 = 6 nM Funct
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
517 7 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(C(F)(F)F)c4)c3)sc12
CHEMBL209742 aa2br_human Human No 8.2 IC50 = 6 nM Bind
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
479 4 1 7 1.7 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(C)c1=O
CHEMBL212416 aa2br_human Human No 8.2 IC50 = 6 nM Bind
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
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
CHEMBL1171164 aa2br_human Human No 8.2 IC50 = 6 nM Funct
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
517 7 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(C(F)(F)F)c4)c3)sc12
CHEMBL1955915 aa2br_human Human No 8.2 IC50 = 6.4 nM Funct
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
483 8 2 9 3.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)ccc5[nH]4)no3)nc2n(CCC)c1=O
CHEMBL1081160 aa2br_human Human No 8.2 IC50 = 6.5 nM Funct
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
395 6 1 8 4.1 CN(C)c1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1
CHEMBL1080421 aa2br_human Human No 8.2 IC50 = 6.7 nM Funct
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
395 7 2 8 4.4 CCNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1
CHEMBL1170526 aa2br_human Human No 7.2 IC50 = 60 nM