Ligand source activities (1 row/activity)



Get vendors


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

 Species

 Assay
Type

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

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
155535230 172105 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 597 11 5 13 2.6 Nc1nc(N/N=C/c2ccc(OCc3ccccc3)c(OCc3ccccc3)c2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.ejmech.2019.06.050
CHEMBL4471366 172105 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 597 11 5 13 2.6 Nc1nc(N/N=C/c2ccc(OCc3ccccc3)c(OCc3ccccc3)c2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.ejmech.2019.06.050
57387594 75509 None 0 Human Functional pEC50 = 9.1 9.1 9 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 506 8 4 9 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042304 75509 None 0 Human Functional pEC50 = 9.1 9.1 9 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 506 8 4 9 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
12150 2333 None 3 Human Functional pEC50 = 9.1 9.1 - 1
Antagonist activity at wild type human A2AAR expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation preincubated for 20 mins followed by CGS21680 addition and measured after 20 mins by by alpha screen assayAntagonist activity at wild type human A2AAR expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation preincubated for 20 mins followed by CGS21680 addition and measured after 20 mins by by alpha screen assay
ChEMBL 399 4 3 9 1.9 O[C@H]1[C@@H](O)[C@H](n2c3nc(C#CCCCC)nc(N)c3nc2c2cccs2)OC1 10.1021/acs.jmedchem.2c00462
164885960 2333 None 3 Human Functional pEC50 = 9.1 9.1 - 1
Antagonist activity at wild type human A2AAR expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation preincubated for 20 mins followed by CGS21680 addition and measured after 20 mins by by alpha screen assayAntagonist activity at wild type human A2AAR expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation preincubated for 20 mins followed by CGS21680 addition and measured after 20 mins by by alpha screen assay
ChEMBL 399 4 3 9 1.9 O[C@H]1[C@@H](O)[C@H](n2c3nc(C#CCCCC)nc(N)c3nc2c2cccs2)OC1 10.1021/acs.jmedchem.2c00462
CHEMBL5203469 2333 None 3 Human Functional pEC50 = 9.1 9.1 - 1
Antagonist activity at wild type human A2AAR expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation preincubated for 20 mins followed by CGS21680 addition and measured after 20 mins by by alpha screen assayAntagonist activity at wild type human A2AAR expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation preincubated for 20 mins followed by CGS21680 addition and measured after 20 mins by by alpha screen assay
ChEMBL 399 4 3 9 1.9 O[C@H]1[C@@H](O)[C@H](n2c3nc(C#CCCCC)nc(N)c3nc2c2cccs2)OC1 10.1021/acs.jmedchem.2c00462
9869857 66851 None 12 Human Functional pEC50 = 9 9.0 1 5
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as induction of cyclic AMP productionAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as induction of cyclic AMP production
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm300087j
CHEMBL186113 66851 None 12 Human Functional pEC50 = 9 9.0 1 5
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as induction of cyclic AMP productionAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as induction of cyclic AMP production
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm300087j
10834352 79358 None 0 Rat Functional pEC50 = 9 9.0 - 1
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 392 8 4 9 0.3 CCCCCCc1nc(N)c2ncn([C@@H]3O[C@H](C(=O)NCC)[C@@H](O)[C@H]3O)c2n1 10.1021/jm960376g
CHEMBL2113529 79358 None 0 Rat Functional pEC50 = 9 9.0 - 1
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 392 8 4 9 0.3 CCCCCCc1nc(N)c2ncn([C@@H]3O[C@H](C(=O)NCC)[C@@H](O)[C@H]3O)c2n1 10.1021/jm960376g
155518944 170452 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 465 8 6 12 0.2 CCCCc1nc(/C=N/Nc2nc(N)c3ncn([C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)c(Cl)[nH]1 10.1016/j.ejmech.2019.06.050
CHEMBL4447310 170452 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 465 8 6 12 0.2 CCCCc1nc(/C=N/Nc2nc(N)c3ncn([C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)c(Cl)[nH]1 10.1016/j.ejmech.2019.06.050
168270759 190101 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISAAntagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
ChEMBL 332 4 2 6 1.8 Nc1nc(C(=O)NCCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5171148 190101 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISAAntagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
ChEMBL 332 4 2 6 1.8 Nc1nc(C(=O)NCCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
168297484 192554 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISAAntagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2cccnc2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5208415 192554 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISAAntagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2cccnc2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
155513199 169840 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 469 8 5 11 1.4 CC(/C=N/Nc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1)Cc1ccc(C(C)C)cc1 10.1016/j.ejmech.2019.06.050
CHEMBL4438487 169840 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 469 8 5 11 1.4 CC(/C=N/Nc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1)Cc1ccc(C(C)C)cc1 10.1016/j.ejmech.2019.06.050
10436433 131441 None 0 Human Functional pEC50 = 8.9 8.9 478 2
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 512 9 5 15 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL368880 131441 None 0 Human Functional pEC50 = 8.9 8.9 478 2
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 512 9 5 15 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
3086599 904 None 36 Human Functional pEC50 = 8.9 8.9 1 6
Partial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based AssayPartial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based Assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/acs.jmedchem.0c01856
375 904 None 36 Human Functional pEC50 = 8.9 8.9 1 6
Partial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based AssayPartial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based Assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/acs.jmedchem.0c01856
424 904 None 36 Human Functional pEC50 = 8.9 8.9 1 6
Partial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based AssayPartial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based Assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/acs.jmedchem.0c01856
CHEMBL331372 904 None 36 Human Functional pEC50 = 8.9 8.9 1 6
Partial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based AssayPartial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based Assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/acs.jmedchem.0c01856
168276863 190297 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISAAntagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccncc2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5174275 190297 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISAAntagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccncc2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
11157262 123707 None 0 Human Functional pEC50 = 8.8 8.8 4 3
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 560 8 5 14 0.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Br)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL361925 123707 None 0 Human Functional pEC50 = 8.8 8.8 4 3
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 560 8 5 14 0.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Br)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
163215620 190452 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISAAntagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5176737 190452 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISAAntagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5203105 190452 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISAAntagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
9869857 66851 None 12 Rat Functional pEC50 = 8 8.0 -4 5
Efficacy against phenylephrine precontracted tissue relaxation in rat aortaEfficacy against phenylephrine precontracted tissue relaxation in rat aorta
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL186113 66851 None 12 Rat Functional pEC50 = 8 8.0 -4 5
Efficacy against phenylephrine precontracted tissue relaxation in rat aortaEfficacy against phenylephrine precontracted tissue relaxation in rat aorta
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
10020580 108029 None 3 Human Functional pEC50 = 8 8.0 7 4
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 347 4 4 9 -0.4 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm010952v
CHEMBL319387 108029 None 3 Human Functional pEC50 = 8 8.0 7 4
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 347 4 4 9 -0.4 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm010952v
155511332 169666 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 431 10 5 11 1.1 CCCCC/C=C/C=C/C=N/Nc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1016/j.ejmech.2019.06.050
CHEMBL4435740 169666 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 431 10 5 11 1.1 CCCCC/C=C/C=C/C=N/Nc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1016/j.ejmech.2019.06.050
118734364 118691 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 547 8 5 12 -0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5cccc(F)c5F)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416798 118691 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 547 8 5 12 -0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5cccc(F)c5F)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
145946428 167641 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Antagonist activity at recombinant human adenosine receptor A2A expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation by measuring CGS21680 EC50 at 100 nM preincubated for 5 mins followed by CGS21680 addition and measured after 20 mins by alpha screen assay (Rvb = 0.89 +/- 0.17 nM)Antagonist activity at recombinant human adenosine receptor A2A expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation by measuring CGS21680 EC50 at 100 nM preincubated for 5 mins followed by CGS21680 addition and measured after 20 mins by alpha screen assay (Rvb = 0.89 +/- 0.17 nM)
ChEMBL 545 9 2 11 3.8 Nc1nc2c(cnn2CCCc2ccc(OCc3ccc(S(=O)(=O)O)cc3)cc2)c2nc(-c3ccco3)nn12 10.1039/C7MD00247E
CHEMBL4291479 167641 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Antagonist activity at recombinant human adenosine receptor A2A expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation by measuring CGS21680 EC50 at 100 nM preincubated for 5 mins followed by CGS21680 addition and measured after 20 mins by alpha screen assay (Rvb = 0.89 +/- 0.17 nM)Antagonist activity at recombinant human adenosine receptor A2A expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation by measuring CGS21680 EC50 at 100 nM preincubated for 5 mins followed by CGS21680 addition and measured after 20 mins by alpha screen assay (Rvb = 0.89 +/- 0.17 nM)
ChEMBL 545 9 2 11 3.8 Nc1nc2c(cnn2CCCc2ccc(OCc3ccc(S(=O)(=O)O)cc3)cc2)c2nc(-c3ccco3)nn12 10.1039/C7MD00247E
CHEMBL4300239 167641 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Antagonist activity at recombinant human adenosine receptor A2A expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation by measuring CGS21680 EC50 at 100 nM preincubated for 5 mins followed by CGS21680 addition and measured after 20 mins by alpha screen assay (Rvb = 0.89 +/- 0.17 nM)Antagonist activity at recombinant human adenosine receptor A2A expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation by measuring CGS21680 EC50 at 100 nM preincubated for 5 mins followed by CGS21680 addition and measured after 20 mins by alpha screen assay (Rvb = 0.89 +/- 0.17 nM)
ChEMBL 545 9 2 11 3.8 Nc1nc2c(cnn2CCCc2ccc(OCc3ccc(S(=O)(=O)O)cc3)cc2)c2nc(-c3ccco3)nn12 10.1039/C7MD00247E
29777576 195772 None 8 Human Functional pEC50 = 8.0 8.0 -3 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 299 3 1 4 3.6 O=C(Nc1noc(-c2ccccc2)n1)c1cccc(Cl)c1 10.1016/j.ejmech.2023.115419
CHEMBL5410449 195772 None 8 Human Functional pEC50 = 8.0 8.0 -3 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 299 3 1 4 3.6 O=C(Nc1noc(-c2ccccc2)n1)c1cccc(Cl)c1 10.1016/j.ejmech.2023.115419
11214123 136785 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
CHEMBL3740507 136785 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
127038755 136930 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 500 7 4 13 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(NC(C)Cc5ccc(Cl)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
CHEMBL3741805 136930 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 500 7 4 13 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(NC(C)Cc5ccc(Cl)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
118734354 118682 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 569 10 6 13 -1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(CC(=O)O)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416789 118682 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 569 10 6 13 -1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(CC(=O)O)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
11112670 79433 None 0 Human Functional pEC50 = 5.0 5.0 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 423 8 4 11 1.6 CC(C)C/C=N/Nc1nc(N)c2ncn([C@@H]3O[C@H](CSC(C)C)[C@@H](O)[C@H]3O)c2n1 10.1021/jm010952v
CHEMBL2113606 79433 None 0 Human Functional pEC50 = 5.0 5.0 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 423 8 4 11 1.6 CC(C)C/C=N/Nc1nc(N)c2ncn([C@@H]3O[C@H](CSC(C)C)[C@@H](O)[C@H]3O)c2n1 10.1021/jm010952v
343627 163172 None 1 Human Functional pEC50 = 5.0 5.0 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 222 2 0 6 -0.2 CCCn1c(=O)n(C)c(=O)c2c1ncn2C 10.1021/jm00100a008
CHEMBL417654 163172 None 1 Human Functional pEC50 = 5.0 5.0 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 222 2 0 6 -0.2 CCCn1c(=O)n(C)c(=O)c2c1ncn2C 10.1021/jm00100a008
137653409 159129 None 0 Human Functional pEC50 = 6.0 6.0 -21 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 567 12 6 12 2.2 Nc1ccc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)s1 10.1021/acs.jmedchem.8b00047
CHEMBL4096796 159129 None 0 Human Functional pEC50 = 6.0 6.0 -21 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 567 12 6 12 2.2 Nc1ccc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)s1 10.1021/acs.jmedchem.8b00047
12150 2333 None 3 Human Functional pEC50 = 7.0 7.0 - 1
Antagonist activity at human A2AAR H278A mutant A2AAR expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation preincubated for 20 mins followed by CGS21680 addition and measured after 20 mins by alpha screen assayAntagonist activity at human A2AAR H278A mutant A2AAR expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation preincubated for 20 mins followed by CGS21680 addition and measured after 20 mins by alpha screen assay
ChEMBL 399 4 3 9 1.9 O[C@H]1[C@@H](O)[C@H](n2c3nc(C#CCCCC)nc(N)c3nc2c2cccs2)OC1 10.1021/acs.jmedchem.2c00462
164885960 2333 None 3 Human Functional pEC50 = 7.0 7.0 - 1
Antagonist activity at human A2AAR H278A mutant A2AAR expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation preincubated for 20 mins followed by CGS21680 addition and measured after 20 mins by alpha screen assayAntagonist activity at human A2AAR H278A mutant A2AAR expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation preincubated for 20 mins followed by CGS21680 addition and measured after 20 mins by alpha screen assay
ChEMBL 399 4 3 9 1.9 O[C@H]1[C@@H](O)[C@H](n2c3nc(C#CCCCC)nc(N)c3nc2c2cccs2)OC1 10.1021/acs.jmedchem.2c00462
CHEMBL5203469 2333 None 3 Human Functional pEC50 = 7.0 7.0 - 1
Antagonist activity at human A2AAR H278A mutant A2AAR expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation preincubated for 20 mins followed by CGS21680 addition and measured after 20 mins by alpha screen assayAntagonist activity at human A2AAR H278A mutant A2AAR expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation preincubated for 20 mins followed by CGS21680 addition and measured after 20 mins by alpha screen assay
ChEMBL 399 4 3 9 1.9 O[C@H]1[C@@H](O)[C@H](n2c3nc(C#CCCCC)nc(N)c3nc2c2cccs2)OC1 10.1021/acs.jmedchem.2c00462
168285984 191851 None 0 Human Functional pEC50 = 6.0 6.0 -1174 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5197358 191851 None 0 Human Functional pEC50 = 6.0 6.0 -1174 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
377 2758 None 42 Human Functional pEC50 = 8.0 8.0 -6 10
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
425 2758 None 42 Human Functional pEC50 = 8.0 8.0 -6 10
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
448222 2758 None 42 Human Functional pEC50 = 8.0 8.0 -6 10
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
CHEMBL464859 2758 None 42 Human Functional pEC50 = 8.0 8.0 -6 10
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
39045556 196944 None 9 Human Functional pEC50 = 7.9 7.9 -4 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 321 4 1 7 2.4 c1ccc(CNc2nc(N3CCCCC3)c3nccnc3n2)nc1 10.1016/j.ejmech.2023.115419
CHEMBL5435338 196944 None 9 Human Functional pEC50 = 7.9 7.9 -4 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 321 4 1 7 2.4 c1ccc(CNc2nc(N3CCCCC3)c3nccnc3n2)nc1 10.1016/j.ejmech.2023.115419
118734357 118685 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 529 8 5 12 -0.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccccc5F)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416792 118685 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 529 8 5 12 -0.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccccc5F)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
46874551 203668 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 436 4 4 10 -0.6 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(C=O)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL603596 203668 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 436 4 4 10 -0.6 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(C=O)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
9976077 79418 None 1 Human Functional pEC50 = 6.0 6.0 19 2
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 365 6 5 11 -0.5 CC(C)C/C=N/Nc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm010952v
CHEMBL2113592 79418 None 1 Human Functional pEC50 = 6.0 6.0 19 2
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 365 6 5 11 -0.5 CC(C)C/C=N/Nc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm010952v
118734350 118678 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 525 8 5 12 -0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(C)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416785 118678 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 525 8 5 12 -0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(C)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
16202442 138414 None 1 Human Functional pEC50 = 5.0 5.0 -707 2
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 441 7 4 10 1.0 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL3771208 138414 None 1 Human Functional pEC50 = 5.0 5.0 -707 2
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 441 7 4 10 1.0 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
3086599 904 None 36 Rat Functional pEC50 = 6.9 6.9 -4 6
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/jm00009a007
375 904 None 36 Rat Functional pEC50 = 6.9 6.9 -4 6
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/jm00009a007
424 904 None 36 Rat Functional pEC50 = 6.9 6.9 -4 6
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/jm00009a007
CHEMBL331372 904 None 36 Rat Functional pEC50 = 6.9 6.9 -4 6
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/jm00009a007
3086599 904 None 36 Rat Functional pEC50 = 6.9 6.9 -4 6
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/jm00018a017
375 904 None 36 Rat Functional pEC50 = 6.9 6.9 -4 6
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/jm00018a017
424 904 None 36 Rat Functional pEC50 = 6.9 6.9 -4 6
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/jm00018a017
CHEMBL331372 904 None 36 Rat Functional pEC50 = 6.9 6.9 -4 6
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/jm00018a017
56838950 75538 None 2 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells by cAMP accumulation assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells by cAMP accumulation assay
ChEMBL 483 7 5 12 -0.4 Nc1nc(SCCc2ccc(S(=O)(=O)O)cc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/ml200189u
CHEMBL2043295 75538 None 2 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells by cAMP accumulation assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells by cAMP accumulation assay
ChEMBL 483 7 5 12 -0.4 Nc1nc(SCCc2ccc(S(=O)(=O)O)cc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/ml200189u
163215620 190452 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISAAntagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5176737 190452 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISAAntagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5203105 190452 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISAAntagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
149362 75503 None 4 Human Functional pEC50 = 7.9 7.9 8 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 427 7 5 10 -0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042298 75503 None 4 Human Functional pEC50 = 7.9 7.9 8 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 427 7 5 10 -0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
49870952 58837 None 0 Human Functional pEC50 = 7.9 7.9 831 2
Agonist activity at human adenosine A2A receptor expressed in CHO cells by cyclic AMP functional assayAgonist activity at human adenosine A2A receptor expressed in CHO cells by cyclic AMP functional assay
ChEMBL 333 3 3 8 0.9 CCCCC#Cc1nc(N)c2ncn([C@@H]3SC[C@@H](O)[C@H]3O)c2n1 10.1021/ml1001823
CHEMBL1688378 58837 None 0 Human Functional pEC50 = 7.9 7.9 831 2
Agonist activity at human adenosine A2A receptor expressed in CHO cells by cyclic AMP functional assayAgonist activity at human adenosine A2A receptor expressed in CHO cells by cyclic AMP functional assay
ChEMBL 333 3 3 8 0.9 CCCCC#Cc1nc(N)c2ncn([C@@H]3SC[C@@H](O)[C@H]3O)c2n1 10.1021/ml1001823
92433056 195855 None 4 Human Functional pEC50 = 7.9 7.9 2 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 345 5 1 6 4.3 c1cncc(CNc2ncc(-c3ccncc3)c(-c3cccs3)n2)c1 10.1016/j.ejmech.2023.115419
CHEMBL5412076 195855 None 4 Human Functional pEC50 = 7.9 7.9 2 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 345 5 1 6 4.3 c1cncc(CNc2ncc(-c3ccncc3)c(-c3cccs3)n2)c1 10.1016/j.ejmech.2023.115419
377 2758 None 42 Human Functional pEC50 = 7.9 7.9 -6 10
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00215
425 2758 None 42 Human Functional pEC50 = 7.9 7.9 -6 10
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00215
448222 2758 None 42 Human Functional pEC50 = 7.9 7.9 -6 10
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00215
CHEMBL464859 2758 None 42 Human Functional pEC50 = 7.9 7.9 -6 10
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00215
3086599 904 None 36 Human Functional pEC50 = 7.9 7.9 1 6
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
375 904 None 36 Human Functional pEC50 = 7.9 7.9 1 6
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
424 904 None 36 Human Functional pEC50 = 7.9 7.9 1 6
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
CHEMBL331372 904 None 36 Human Functional pEC50 = 7.9 7.9 1 6
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
377 2758 None 42 Human Functional pEC50 = 7.9 7.9 -6 10
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
425 2758 None 42 Human Functional pEC50 = 7.9 7.9 -6 10
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
448222 2758 None 42 Human Functional pEC50 = 7.9 7.9 -6 10
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
CHEMBL464859 2758 None 42 Human Functional pEC50 = 7.9 7.9 -6 10
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
118732977 118582 None 0 Human Functional pEC50 = 7.9 7.9 -1 3
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 461 5 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N[C@H]5C[C@@H]6CC[C@@H]5C6)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414943 118582 None 0 Human Functional pEC50 = 7.9 7.9 -1 3
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 461 5 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N[C@H]5C[C@@H]6CC[C@@H]5C6)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
46874565 203785 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 453 4 4 11 -0.5 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc([N+](=O)[O-])cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL604234 203785 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 453 4 4 11 -0.5 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc([N+](=O)[O-])cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
76329265 106116 None 0 Human Functional pEC50 = 5.9 5.9 -79 4
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 377 4 5 10 -0.9 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133158 106116 None 0 Human Functional pEC50 = 5.9 5.9 -79 4
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 377 4 5 10 -0.9 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
118734359 118687 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 579 8 5 12 0.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccccc5C(F)(F)F)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416794 118687 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 579 8 5 12 0.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccccc5C(F)(F)F)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
145993667 167475 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Antagonist activity at recombinant human adenosine receptor A2A expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation by measuring CGS21680 EC50 at 1000 nM preincubated for 5 mins followed by CGS21680 addition and measured after 20 mins by alpha screen assay (Rvb = 0.89 +/- 0.17 nM)Antagonist activity at recombinant human adenosine receptor A2A expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation by measuring CGS21680 EC50 at 1000 nM preincubated for 5 mins followed by CGS21680 addition and measured after 20 mins by alpha screen assay (Rvb = 0.89 +/- 0.17 nM)
ChEMBL 1048 25 4 15 7.9 Nc1nc2c(cnn2CCCc2ccc(OCC(=O)NCCCCNC(=O)CCCCCNC(=O)COc3ccc(/C=C/C4=[N+]5C(=Cc6ccc(-c7cccs7)n6[B-]5(F)F)C=C4)cc3)cc2)c2nc(-c3ccco3)nn12 10.1039/C7MD00247E
CHEMBL4294888 167475 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Antagonist activity at recombinant human adenosine receptor A2A expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation by measuring CGS21680 EC50 at 1000 nM preincubated for 5 mins followed by CGS21680 addition and measured after 20 mins by alpha screen assay (Rvb = 0.89 +/- 0.17 nM)Antagonist activity at recombinant human adenosine receptor A2A expressed in CHO cells assessed as inhibition of CGS21680-induced cAMP accumulation by measuring CGS21680 EC50 at 1000 nM preincubated for 5 mins followed by CGS21680 addition and measured after 20 mins by alpha screen assay (Rvb = 0.89 +/- 0.17 nM)
ChEMBL 1048 25 4 15 7.9 Nc1nc2c(cnn2CCCc2ccc(OCC(=O)NCCCCNC(=O)CCCCCNC(=O)COc3ccc(/C=C/C4=[N+]5C(=Cc6ccc(-c7cccs7)n6[B-]5(F)F)C=C4)cc3)cc2)c2nc(-c3ccco3)nn12 10.1039/C7MD00247E
10387599 79407 None 0 Human Functional pEC50 = 4.9 4.9 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 423 9 4 11 1.6 CCCSC[C@H]1O[C@@H](n2cnc3c(N)nc(N/N=C/CC(C)C)nc32)[C@H](O)[C@@H]1O 10.1021/jm010952v
CHEMBL2113581 79407 None 0 Human Functional pEC50 = 4.9 4.9 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 423 9 4 11 1.6 CCCSC[C@H]1O[C@@H](n2cnc3c(N)nc(N/N=C/CC(C)C)nc32)[C@H](O)[C@@H]1O 10.1021/jm010952v
137636099 155915 None 0 Human Functional pEC50 = 7.9 7.9 -1 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 535 6 3 12 1.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4059961 155915 None 0 Human Functional pEC50 = 7.9 7.9 -1 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 535 6 3 12 1.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
46874530 204022 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 436 4 4 10 -0.6 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccccc4C=O)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL605473 204022 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 436 4 4 10 -0.6 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccccc4C=O)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
169316 20797 None 2 Human Functional pEC50 = 5.9 5.9 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 222 3 1 5 0.2 CCCCn1c(=O)n(C)c(=O)c2[nH]cnc21 10.1021/jm00100a008
CHEMBL130969 20797 None 2 Human Functional pEC50 = 5.9 5.9 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 222 3 1 5 0.2 CCCCn1c(=O)n(C)c(=O)c2[nH]cnc21 10.1021/jm00100a008
15646970 99333 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 222 3 1 5 0.3 CCCn1c(=O)n(CC)c(=O)c2[nH]cnc21 10.1021/jm00100a008
CHEMBL28194 99333 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 222 3 1 5 0.3 CCCn1c(=O)n(CC)c(=O)c2[nH]cnc21 10.1021/jm00100a008
137643164 158193 None 0 Human Functional pEC50 = 5.9 5.9 -74 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 552 12 5 11 2.6 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cccs2)c1 10.1021/acs.jmedchem.8b00047
CHEMBL4086624 158193 None 0 Human Functional pEC50 = 5.9 5.9 -74 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 552 12 5 11 2.6 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cccs2)c1 10.1021/acs.jmedchem.8b00047
46874590 204023 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 536 6 4 11 0.8 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(CCC(=O)OC(C)(C)C)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL605478 204023 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 536 6 4 11 0.8 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(CCC(=O)OC(C)(C)C)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
11742562 87215 None 0 Human Functional pEC50 = 5.9 5.9 16 2
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation countingAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation counting
ChEMBL 415 6 5 12 -0.5 COc1ccc(/C=N/Nc2nc(N)c3ncn([C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)cc1 10.1016/j.bmc.2012.11.021
CHEMBL2326828 87215 None 0 Human Functional pEC50 = 5.9 5.9 16 2
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation countingAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation counting
ChEMBL 415 6 5 12 -0.5 COc1ccc(/C=N/Nc2nc(N)c3ncn([C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)cc1 10.1016/j.bmc.2012.11.021
168276883 190309 None 0 Human Functional pEC50 = 5.9 5.9 -2630 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5174429 190309 None 0 Human Functional pEC50 = 5.9 5.9 -2630 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
3636010 21024 None 6 Human Functional pEC50 = 4.9 4.9 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 250 5 1 5 1.1 CCCCn1cnc2c1c(=O)[nH]c(=O)n2CCC 10.1021/jm00100a008
CHEMBL131164 21024 None 6 Human Functional pEC50 = 4.9 4.9 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 250 5 1 5 1.1 CCCCn1cnc2c1c(=O)[nH]c(=O)n2CCC 10.1021/jm00100a008
168279634 191141 None 0 Human Functional pEC50 = 4.9 4.9 -2137 3
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(Cl)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5186981 191141 None 0 Human Functional pEC50 = 4.9 4.9 -2137 3
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(Cl)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
168287894 191460 None 0 Human Functional pEC50 = 4.9 4.9 -1348 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(Cl)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5191989 191460 None 0 Human Functional pEC50 = 4.9 4.9 -1348 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(Cl)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
57387824 75504 None 0 Human Functional pEC50 = 7.9 7.9 8 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 442 7 6 11 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(N)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042299 75504 None 0 Human Functional pEC50 = 7.9 7.9 8 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 442 7 6 11 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(N)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
57384288 75507 None 0 Human Functional pEC50 = 7.9 7.9 53 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 674 9 7 12 3.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042302 75507 None 0 Human Functional pEC50 = 7.9 7.9 53 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 674 9 7 12 3.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
137659441 159192 None 0 Human Functional pEC50 = 7.8 7.8 -1 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 441 6 3 12 0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4097468 159192 None 0 Human Functional pEC50 = 7.8 7.8 -1 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 441 6 3 12 0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
137642153 158460 None 0 Human Functional pEC50 = 7.8 7.8 4 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 429 6 3 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4089741 158460 None 0 Human Functional pEC50 = 7.8 7.8 4 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 429 6 3 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
10378132 21884 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 264 5 0 6 1.1 CCCCn1c(=O)c2c(ncn2C)n(CCC)c1=O 10.1021/jm00100a008
CHEMBL132001 21884 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 264 5 0 6 1.1 CCCCn1c(=O)c2c(ncn2C)n(CCC)c1=O 10.1021/jm00100a008
137649083 157399 None 0 Human Functional pEC50 = 6.8 6.8 -7 3
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 849 15 6 13 6.7 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3nc(Cl)nc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4077152 157399 None 0 Human Functional pEC50 = 6.8 6.8 -7 3
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 849 15 6 13 6.7 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3nc(Cl)nc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
71508700 87217 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation countingAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation counting
ChEMBL 459 9 10 16 -5.1 Nc1nc(N/N=C/[C@@H](O)[C@H](O)[C@H](O)[C@@H](O)CO)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.bmc.2012.11.021
CHEMBL2326831 87217 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation countingAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation counting
ChEMBL 459 9 10 16 -5.1 Nc1nc(N/N=C/[C@@H](O)[C@H](O)[C@H](O)[C@@H](O)CO)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.bmc.2012.11.021
168280775 191266 None 0 Human Functional pEC50 = 4.8 4.8 -933 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 524 7 4 10 2.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(C(C)(C)C)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5188601 191266 None 0 Human Functional pEC50 = 4.8 4.8 -933 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 524 7 4 10 2.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(C(C)(C)C)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
118734344 118672 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 529 8 5 12 -0.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(F)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416779 118672 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 529 8 5 12 -0.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(F)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
137661505 159590 None 0 Human Functional pEC50 = 6.8 6.8 -4 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4101850 159590 None 0 Human Functional pEC50 = 6.8 6.8 -4 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
155547064 173709 None 1 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 410 5 5 12 -0.7 N#Cc1ccc(/C=N/Nc2nc(N)c3ncn([C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)cc1 10.1016/j.ejmech.2019.06.050
CHEMBL4533415 173709 None 1 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 410 5 5 12 -0.7 N#Cc1ccc(/C=N/Nc2nc(N)c3ncn([C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)cc1 10.1016/j.ejmech.2019.06.050
378 3041 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 408 3 4 9 -0.4 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(C#Cc1ccccc1)nc2N 10.1021/jm00009a007
9953255 3041 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 408 3 4 9 -0.4 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(C#Cc1ccccc1)nc2N 10.1021/jm00009a007
CHEMBL223270 3041 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 408 3 4 9 -0.4 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(C#Cc1ccccc1)nc2N 10.1021/jm00009a007
12905388 91803 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 194 1 1 5 -0.6 CCn1c(=O)c2nc[nH]c2n(C)c1=O 10.1021/jm00100a008
CHEMBL24107 91803 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 194 1 1 5 -0.6 CCn1c(=O)c2nc[nH]c2n(C)c1=O 10.1021/jm00100a008
15931313 19085 None 2 Human Functional pEC50 = 4.8 4.8 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 236 4 1 5 0.7 CCCn1cnc2c1c(=O)[nH]c(=O)n2CCC 10.1021/jm00100a008
CHEMBL128900 19085 None 2 Human Functional pEC50 = 4.8 4.8 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 236 4 1 5 0.7 CCCn1cnc2c1c(=O)[nH]c(=O)n2CCC 10.1021/jm00100a008
118734347 118675 None 0 Human Functional pEC50 = 6.8 6.8 45 2
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 637 8 5 12 0.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(I)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416782 118675 None 0 Human Functional pEC50 = 6.8 6.8 45 2
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 637 8 5 12 0.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(I)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
137661132 159268 None 0 Human Functional pEC50 = 7.8 7.8 -2 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 491 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4098377 159268 None 0 Human Functional pEC50 = 7.8 7.8 -2 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 491 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
137642036 158244 None 0 Human Functional pEC50 = 7.8 7.8 -4 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 387 6 3 12 -0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4087306 158244 None 0 Human Functional pEC50 = 7.8 7.8 -4 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 387 6 3 12 -0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
86344 100093 None 9 Human Functional pEC50 = 5.8 5.8 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 208 2 1 5 -0.2 CCCn1c(=O)n(C)c(=O)c2[nH]cnc21 10.1021/jm00100a008
CHEMBL286976 100093 None 9 Human Functional pEC50 = 5.8 5.8 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 208 2 1 5 -0.2 CCCn1c(=O)n(C)c(=O)c2[nH]cnc21 10.1021/jm00100a008
164617261 184774 None 1 Human Functional pEC50 = 6.8 6.8 20 2
Antagonist activity at human A2A receptor on T-cells assessed as increase of IL-2 production preincubated for 1 hr followed by addition of T-cell activator CD3/CD28 and measured after 1 hr by plate reader methodAntagonist activity at human A2A receptor on T-cells assessed as increase of IL-2 production preincubated for 1 hr followed by addition of T-cell activator CD3/CD28 and measured after 1 hr by plate reader method
ChEMBL 274 2 1 4 3.1 Nc1nc(Cc2ccccc2)cn2c1nc1ccccc12 10.1016/j.ejmech.2020.113040
CHEMBL4849795 184774 None 1 Human Functional pEC50 = 6.8 6.8 20 2
Antagonist activity at human A2A receptor on T-cells assessed as increase of IL-2 production preincubated for 1 hr followed by addition of T-cell activator CD3/CD28 and measured after 1 hr by plate reader methodAntagonist activity at human A2A receptor on T-cells assessed as increase of IL-2 production preincubated for 1 hr followed by addition of T-cell activator CD3/CD28 and measured after 1 hr by plate reader method
ChEMBL 274 2 1 4 3.1 Nc1nc(Cc2ccccc2)cn2c1nc1ccccc12 10.1016/j.ejmech.2020.113040
CHEMBL5088305 217641 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Partial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based AssayPartial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based Assay
ChEMBL None None None N#Cc1c(-c2ccccc2)cc(SCc2ncc[nH]2)nc1N 10.1021/acs.jmedchem.0c01856
71508696 87219 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation countingAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation counting
ChEMBL 453 5 5 11 0.8 Nc1nc(N/N=C/c2ccc(Cl)c(Cl)c2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.bmc.2012.11.021
CHEMBL2326843 87219 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation countingAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation counting
ChEMBL 453 5 5 11 0.8 Nc1nc(N/N=C/c2ccc(Cl)c(Cl)c2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.bmc.2012.11.021
46874555 203702 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 450 4 4 10 -0.2 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(C(C)=O)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL603808 203702 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 450 4 4 10 -0.2 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(C(C)=O)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
377 2758 None 42 Human Functional pEC50 = 7.8 7.8 -6 10
Activity at human adenosine A2A receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2A receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
425 2758 None 42 Human Functional pEC50 = 7.8 7.8 -6 10
Activity at human adenosine A2A receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2A receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
448222 2758 None 42 Human Functional pEC50 = 7.8 7.8 -6 10
Activity at human adenosine A2A receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2A receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
CHEMBL464859 2758 None 42 Human Functional pEC50 = 7.8 7.8 -6 10
Activity at human adenosine A2A receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2A receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
377 2758 None 42 Human Functional pEC50 = 7.8 7.8 -6 10
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells by cAMP accumulation assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells by cAMP accumulation assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/ml200189u
425 2758 None 42 Human Functional pEC50 = 7.8 7.8 -6 10
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells by cAMP accumulation assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells by cAMP accumulation assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/ml200189u
448222 2758 None 42 Human Functional pEC50 = 7.8 7.8 -6 10
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells by cAMP accumulation assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells by cAMP accumulation assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/ml200189u
CHEMBL464859 2758 None 42 Human Functional pEC50 = 7.8 7.8 -6 10
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells by cAMP accumulation assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells by cAMP accumulation assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/ml200189u
155561909 175918 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 428 6 5 12 -0.5 CN(C)c1ccc(/C=N/Nc2nc(N)c3ncn([C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)cc1 10.1016/j.ejmech.2019.06.050
CHEMBL4584669 175918 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 428 6 5 12 -0.5 CN(C)c1ccc(/C=N/Nc2nc(N)c3ncn([C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)cc1 10.1016/j.ejmech.2019.06.050
118732972 118577 None 0 Human Functional pEC50 = 5.8 5.8 -269 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 347 4 3 12 -1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414938 118577 None 0 Human Functional pEC50 = 5.8 5.8 -269 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 347 4 3 12 -1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
16109359 161872 None 0 Human Functional pEC50 = 6.8 6.8 -64 4
Activity at human adenosine A2A receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2A receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells
ChEMBL 924 21 6 14 4.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCNC(=O)CCCCCNC(=O)COc4ccc(/C=C/C5=[N+]6C(=Cc7ccc(-c8cccs8)n7[B-]6(F)F)C=C5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061279i
CHEMBL414055 161872 None 0 Human Functional pEC50 = 6.8 6.8 -64 4
Activity at human adenosine A2A receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2A receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells
ChEMBL 924 21 6 14 4.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCNC(=O)CCCCCNC(=O)COc4ccc(/C=C/C5=[N+]6C(=Cc7ccc(-c8cccs8)n7[B-]6(F)F)C=C5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061279i
118734343 118671 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 539 10 5 12 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(CCc5ccccc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416778 118671 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 539 10 5 12 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(CCc5ccccc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
377 2758 None 42 Human Functional pEC50 = 7.8 7.8 -6 10
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation countingAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation counting
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmc.2012.11.021
425 2758 None 42 Human Functional pEC50 = 7.8 7.8 -6 10
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation countingAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation counting
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmc.2012.11.021
448222 2758 None 42 Human Functional pEC50 = 7.8 7.8 -6 10
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation countingAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation counting
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmc.2012.11.021
CHEMBL464859 2758 None 42 Human Functional pEC50 = 7.8 7.8 -6 10
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation countingAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation counting
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmc.2012.11.021
3086599 904 None 36 Human Functional pEC50 = 7.7 7.7 1 6
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/acs.jmedchem.5b00215
375 904 None 36 Human Functional pEC50 = 7.7 7.7 1 6
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/acs.jmedchem.5b00215
424 904 None 36 Human Functional pEC50 = 7.7 7.7 1 6
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/acs.jmedchem.5b00215
CHEMBL331372 904 None 36 Human Functional pEC50 = 7.7 7.7 1 6
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/acs.jmedchem.5b00215
45875637 195990 None 3 Human Functional pEC50 = 7.7 7.7 -5 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 300 3 1 4 3.2 O=C(Nc1nc(C2CC2)cs1)C1COc2ccccc2C1 10.1016/j.ejmech.2023.115419
CHEMBL5414803 195990 None 3 Human Functional pEC50 = 7.7 7.7 -5 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 300 3 1 4 3.2 O=C(Nc1nc(C2CC2)cs1)C1COc2ccccc2C1 10.1016/j.ejmech.2023.115419
127041419 136981 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 534 7 4 13 1.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(NC(C)Cc5ccc(C(F)(F)F)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
CHEMBL3742258 136981 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 534 7 4 13 1.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(NC(C)Cc5ccc(C(F)(F)F)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
11795830 79355 None 0 Rat Functional pEC50 = 6.7 6.7 2 2
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 410 5 4 9 0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(/C=C/c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm960376g
CHEMBL2113526 79355 None 0 Rat Functional pEC50 = 6.7 6.7 2 2
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 410 5 4 9 0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(/C=C/c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm960376g
10248875 79394 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 375 5 5 12 -0.9 Nc1nc(N/N=C/c2ccco2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm00018a017
CHEMBL2113564 79394 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 375 5 5 12 -0.9 Nc1nc(N/N=C/c2ccco2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm00018a017
57387596 75516 None 0 Human Functional pEC50 = 8.7 8.7 3 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 492 7 4 9 1.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042311 75516 None 0 Human Functional pEC50 = 8.7 8.7 3 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 492 7 4 9 1.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
3086599 904 None 36 Human Functional pEC50 = 8.7 8.7 1 6
Agonist activity at human adenosine A2a receptor expressed in CHO cells assessed as stimulation of cAMP formation after 24 hrsAgonist activity at human adenosine A2a receptor expressed in CHO cells assessed as stimulation of cAMP formation after 24 hrs
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/ml5002486
375 904 None 36 Human Functional pEC50 = 8.7 8.7 1 6
Agonist activity at human adenosine A2a receptor expressed in CHO cells assessed as stimulation of cAMP formation after 24 hrsAgonist activity at human adenosine A2a receptor expressed in CHO cells assessed as stimulation of cAMP formation after 24 hrs
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/ml5002486
424 904 None 36 Human Functional pEC50 = 8.7 8.7 1 6
Agonist activity at human adenosine A2a receptor expressed in CHO cells assessed as stimulation of cAMP formation after 24 hrsAgonist activity at human adenosine A2a receptor expressed in CHO cells assessed as stimulation of cAMP formation after 24 hrs
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/ml5002486
CHEMBL331372 904 None 36 Human Functional pEC50 = 8.7 8.7 1 6
Agonist activity at human adenosine A2a receptor expressed in CHO cells assessed as stimulation of cAMP formation after 24 hrsAgonist activity at human adenosine A2a receptor expressed in CHO cells assessed as stimulation of cAMP formation after 24 hrs
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1021/ml5002486
70689262 78006 None 0 Human Functional pEC50 = 8.7 8.7 1 3
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
CHEMBL2096798 78006 None 0 Human Functional pEC50 = 8.7 8.7 1 3
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
118732971 118575 None 0 Human Functional pEC50 = 8.6 8.6 11 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 333 3 3 12 -1.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414936 118575 None 0 Human Functional pEC50 = 8.6 8.6 11 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 333 3 3 12 -1.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
377 2758 None 42 Human Functional pEC50 = 8.6 8.6 -6 10
Irreversible agonist activity at human adenosine A2A 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 A2A receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
425 2758 None 42 Human Functional pEC50 = 8.6 8.6 -6 10
Irreversible agonist activity at human adenosine A2A 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 A2A receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
448222 2758 None 42 Human Functional pEC50 = 8.6 8.6 -6 10
Irreversible agonist activity at human adenosine A2A 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 A2A receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
CHEMBL464859 2758 None 42 Human Functional pEC50 = 8.6 8.6 -6 10
Irreversible agonist activity at human adenosine A2A 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 A2A receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
137648928 157497 None 0 Human Functional pEC50 = 8.5 8.5 -1 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 549 6 3 12 1.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(I)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4078479 157497 None 0 Human Functional pEC50 = 8.5 8.5 -1 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 549 6 3 12 1.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(I)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
11352497 123033 None 0 Rat Functional pEC50 = 8.5 8.5 2 3
Efficacy against phenylephrine precontracted tissue relaxation in rat aortaEfficacy against phenylephrine precontracted tissue relaxation in rat aorta
ChEMBL 498 8 6 15 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(O)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL360837 123033 None 0 Rat Functional pEC50 = 8.5 8.5 2 3
Efficacy against phenylephrine precontracted tissue relaxation in rat aortaEfficacy against phenylephrine precontracted tissue relaxation in rat aorta
ChEMBL 498 8 6 15 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(O)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
45811961 195922 None 4 Human Functional pEC50 = 7.7 7.7 -7 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 286 3 2 3 1.8 CC(C)N1CC(C(=O)Nc2nc3ccccc3[nH]2)CC1=O 10.1016/j.ejmech.2023.115419
CHEMBL5413438 195922 None 4 Human Functional pEC50 = 7.7 7.7 -7 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 286 3 2 3 1.8 CC(C)N1CC(C(=O)Nc2nc3ccccc3[nH]2)CC1=O 10.1016/j.ejmech.2023.115419
49870953 58838 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as induction of cAMP production after 30 mins by immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as induction of cAMP production after 30 mins by immunoassay
ChEMBL 335 5 3 8 1.6 CCCC/C=C/c1nc(N)c2ncn([C@@H]3SC[C@@H](O)[C@H]3O)c2n1 10.1021/jm201229j
CHEMBL1688379 58838 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as induction of cAMP production after 30 mins by immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as induction of cAMP production after 30 mins by immunoassay
ChEMBL 335 5 3 8 1.6 CCCC/C=C/c1nc(N)c2ncn([C@@H]3SC[C@@H](O)[C@H]3O)c2n1 10.1021/jm201229j
168297905 192540 None 0 Human Functional pEC50 = 5.7 5.7 -977 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 516 8 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5208245 192540 None 0 Human Functional pEC50 = 5.7 5.7 -977 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 516 8 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
75380603 195365 None 2 Human Functional pEC50 = 7.7 7.7 -1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 327 6 2 6 2.4 CCOc1nc(NC(CO)c2ccco2)ncc1Br 10.1016/j.ejmech.2023.115419
CHEMBL5402079 195365 None 2 Human Functional pEC50 = 7.7 7.7 -1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 327 6 2 6 2.4 CCOc1nc(NC(CO)c2ccco2)ncc1Br 10.1016/j.ejmech.2023.115419
118732975 118580 None 0 Human Functional pEC50 = 7.7 7.7 -2 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL3414941 118580 None 0 Human Functional pEC50 = 7.7 7.7 -2 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
118732974 118579 None 0 Human Functional pEC50 = 7.7 7.7 -1 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL3414940 118579 None 0 Human Functional pEC50 = 7.7 7.7 -1 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
377 2758 None 42 Human Functional pEC50 = 7.7 7.7 -6 10
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
425 2758 None 42 Human Functional pEC50 = 7.7 7.7 -6 10
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
448222 2758 None 42 Human Functional pEC50 = 7.7 7.7 -6 10
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
CHEMBL464859 2758 None 42 Human Functional pEC50 = 7.7 7.7 -6 10
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
46874592 204053 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 436 5 4 9 0.1 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#CCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL605690 204053 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 436 5 4 9 0.1 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#CCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
168288912 191737 None 0 Human Functional pEC50 = 5.7 5.7 -17378 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5195714 191737 None 0 Human Functional pEC50 = 5.7 5.7 -17378 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
10403711 96386 None 27 Human Functional pEC50 = 7.6 7.6 -2 3
Agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as stimulation of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human A2A adenosine receptor expressed in CHO cells assessed as stimulation of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 320 3 4 9 -1.7 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CC2)[C@@H](O)[C@H]1O 10.1021/jm300095s
CHEMBL261482 96386 None 27 Human Functional pEC50 = 7.6 7.6 -2 3
Agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as stimulation of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human A2A adenosine receptor expressed in CHO cells assessed as stimulation of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 320 3 4 9 -1.7 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CC2)[C@@H](O)[C@H]1O 10.1021/jm300095s
46874629 203743 None 0 Rat Functional pEC50 = 6.7 6.7 1 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 447 4 4 11 -1.4 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#CCN4CCSCC4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL604026 203743 None 0 Rat Functional pEC50 = 6.7 6.7 1 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 447 4 4 11 -1.4 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#CCN4CCSCC4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
57387822 75517 None 0 Human Functional pEC50 = 5.7 5.7 -1 3
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 840 13 7 12 6.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042312 75517 None 0 Human Functional pEC50 = 5.7 5.7 -1 3
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 840 13 7 12 6.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
215610 76963 None 2 Human Functional pEC50 = 6.7 6.7 239 2
Agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as stimulation of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human A2A adenosine receptor expressed in CHO cells assessed as stimulation of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 348 3 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CCCC2)[C@@H](O)[C@H]1O 10.1021/jm300095s
CHEMBL2070508 76963 None 2 Human Functional pEC50 = 6.7 6.7 239 2
Agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as stimulation of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human A2A adenosine receptor expressed in CHO cells assessed as stimulation of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 348 3 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CCCC2)[C@@H](O)[C@H]1O 10.1021/jm300095s
46874574 203860 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Functional activity against A2a adenosine receptor from rat aorta.Functional activity against A2a adenosine receptor from rat aorta.
ChEMBL 414 3 4 10 -0.4 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4cccs4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL604649 203860 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Functional activity against A2a adenosine receptor from rat aorta.Functional activity against A2a adenosine receptor from rat aorta.
ChEMBL 414 3 4 10 -0.4 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4cccs4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
71657835 159831 None 4 Human Functional pEC50 = 5.6 5.6 -7 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4104819 159831 None 4 Human Functional pEC50 = 5.6 5.6 -7 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
137650461 157348 None 0 Human Functional pEC50 = 5.6 5.6 -6 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 857 16 6 13 6.4 CC(=O)Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4076565 157348 None 0 Human Functional pEC50 = 5.6 5.6 -6 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 857 16 6 13 6.4 CC(=O)Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
118732973 118578 None 0 Human Functional pEC50 = 6.6 6.6 -30 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 381 4 3 12 -0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414939 118578 None 0 Human Functional pEC50 = 6.6 6.6 -30 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 381 4 3 12 -0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
118734358 118686 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 545 8 5 12 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccccc5Cl)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416793 118686 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 545 8 5 12 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccccc5Cl)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
46874547 204156 None 0 Rat Functional pEC50 = 6.6 6.6 3 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 409 3 4 10 -1.0 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccccn4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL606318 204156 None 0 Rat Functional pEC50 = 6.6 6.6 3 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 409 3 4 10 -1.0 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccccn4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
118732978 118583 None 0 Human Functional pEC50 = 7.6 7.6 -2 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 403 5 3 13 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414944 118583 None 0 Human Functional pEC50 = 7.6 7.6 -2 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 403 5 3 13 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
2844 283 None 61 Human Functional pEC50 = 7.6 7.6 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
60961 283 None 61 Human Functional pEC50 = 7.6 7.6 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
60961.0 283 None 61 Human Functional pEC50 = 7.6 7.6 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
90 283 None 61 Human Functional pEC50 = 7.6 7.6 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
CHEMBL477 283 None 61 Human Functional pEC50 = 7.6 7.6 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
DB00640 283 None 61 Human Functional pEC50 = 7.6 7.6 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
377 2758 None 42 Human Functional pEC50 = 6.6 6.6 -6 10
Agonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
425 2758 None 42 Human Functional pEC50 = 6.6 6.6 -6 10
Agonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
448222 2758 None 42 Human Functional pEC50 = 6.6 6.6 -6 10
Agonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
CHEMBL464859 2758 None 42 Human Functional pEC50 = 6.6 6.6 -6 10
Agonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
76311194 106102 None 0 Human Functional pEC50 = 6.6 6.6 -158 4
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 525 5 5 10 -0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133078 106102 None 0 Human Functional pEC50 = 6.6 6.6 -158 4
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 525 5 5 10 -0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
76318403 106115 None 0 Human Functional pEC50 = 5.6 5.6 -501 4
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 363 4 5 10 -1.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133157 106115 None 0 Human Functional pEC50 = 5.6 5.6 -501 4
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 363 4 5 10 -1.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
10449535 76962 None 0 Human Functional pEC50 = 7.6 7.6 -1 3
Agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as stimulation of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human A2A adenosine receptor expressed in CHO cells assessed as stimulation of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 334 3 4 9 -1.3 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CCC2)[C@@H](O)[C@H]1O 10.1021/jm300095s
CHEMBL2070507 76962 None 0 Human Functional pEC50 = 7.6 7.6 -1 3
Agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as stimulation of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human A2A adenosine receptor expressed in CHO cells assessed as stimulation of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 334 3 4 9 -1.3 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CCC2)[C@@H](O)[C@H]1O 10.1021/jm300095s
168293442 192244 None 0 Human Functional pEC50 = 4.6 4.6 -109647 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 546 7 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Br)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5203632 192244 None 0 Human Functional pEC50 = 4.6 4.6 -109647 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 546 7 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Br)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
10093028 79393 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 411 6 5 11 0.1 Nc1nc(N/N=C/C=C/c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm00018a017
CHEMBL2113563 79393 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 411 6 5 11 0.1 Nc1nc(N/N=C/C=C/c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm00018a017
CHEMBL5078507 217047 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Partial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based AssayPartial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based Assay
ChEMBL None None None N#Cc1c(N)nc(SCc2ncc[nH]2)nc1-c1ccccc1 10.1021/acs.jmedchem.0c01856
137646655 157718 None 0 Human Functional pEC50 = 5.6 5.6 -41 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 711 13 6 12 4.8 Nc1cc(-c2cccc(C(F)(F)F)c2)c(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)s1 10.1021/acs.jmedchem.8b00047
CHEMBL4081224 157718 None 0 Human Functional pEC50 = 5.6 5.6 -41 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 711 13 6 12 4.8 Nc1cc(-c2cccc(C(F)(F)F)c2)c(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)s1 10.1021/acs.jmedchem.8b00047
118734376 118702 None 0 Human Functional pEC50 = 7.6 7.6 14 2
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 602 10 4 12 1.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCCCc6ccccc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416810 118702 None 0 Human Functional pEC50 = 7.6 7.6 14 2
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 602 10 4 12 1.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCCCc6ccccc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
10330676 21319 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 208 2 1 5 -0.2 CCCn1c(=O)[nH]c(=O)c2c1ncn2C 10.1021/jm00100a008
CHEMBL131371 21319 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 208 2 1 5 -0.2 CCCn1c(=O)[nH]c(=O)c2c1ncn2C 10.1021/jm00100a008
137657926 159862 None 0 Human Functional pEC50 = 7.5 7.5 -3 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 421 6 3 12 0.3 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4105164 159862 None 0 Human Functional pEC50 = 7.5 7.5 -3 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 421 6 3 12 0.3 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
46874587 203979 None 0 Rat Functional pEC50 = 7.5 7.5 251 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 415 3 4 11 -1.0 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4nccs4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL605265 203979 None 0 Rat Functional pEC50 = 7.5 7.5 251 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 415 3 4 11 -1.0 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4nccs4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
118732981 118586 None 0 Human Functional pEC50 = 7.5 7.5 1 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 495 5 3 12 2.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414947 118586 None 0 Human Functional pEC50 = 7.5 7.5 1 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 495 5 3 12 2.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
135457558 79389 None 0 Rat Functional pEC50 = 6.6 6.6 17 2
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 457 7 6 13 -0.2 COc1cc(/C=C/C=N/Nc2nc(N)c3ncn([C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)ccc1O 10.1021/jm00018a017
CHEMBL2113559 79389 None 0 Rat Functional pEC50 = 6.6 6.6 17 2
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 457 7 6 13 -0.2 COc1cc(/C=C/C=N/Nc2nc(N)c3ncn([C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)ccc1O 10.1021/jm00018a017
2153 3800 None 72 Human Functional pEC50 = 4.6 4.6 -2 5
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00100a008
2153.0 3800 None 72 Human Functional pEC50 = 4.6 4.6 -2 5
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00100a008
2620 3800 None 72 Human Functional pEC50 = 4.6 4.6 -2 5
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00100a008
413 3800 None 72 Human Functional pEC50 = 4.6 4.6 -2 5
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00100a008
CHEMBL190 3800 None 72 Human Functional pEC50 = 4.6 4.6 -2 5
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00100a008
DB00277 3800 None 72 Human Functional pEC50 = 4.6 4.6 -2 5
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00100a008
168293564 192266 None 0 Human Functional pEC50 = 6.5 6.5 -45 4
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 849 13 6 13 6.8 Nc1sc(-c2ccc(C(=O)NCCCc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5203917 192266 None 0 Human Functional pEC50 = 6.5 6.5 -45 4
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 849 13 6 13 6.8 Nc1sc(-c2ccc(C(=O)NCCCc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
137656845 159890 None 0 Human Functional pEC50 = 5.5 5.5 -19 3
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 800 15 5 12 6.5 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccc(-c2scc(C(=O)c3ccccc3)c2-c2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.8b00047
CHEMBL4105473 159890 None 0 Human Functional pEC50 = 5.5 5.5 -19 3
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 800 15 5 12 6.5 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccc(-c2scc(C(=O)c3ccccc3)c2-c2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.8b00047
46874572 203859 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 476 3 4 9 0.6 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(C(F)(F)F)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL604647 203859 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 476 3 4 9 0.6 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(C(F)(F)F)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
11527363 110120 None 0 Human Functional pEC50 = 8.5 8.5 -3 2
Agonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by EIAAgonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by EIA
ChEMBL 615 13 2 10 3.7 CCN(CC)CCN1CCN(C(=O)CCc2cccc(CSc3nc(N)c(C#N)c(-c4ccc(NC(C)=O)cc4)n3)n2)CC1 10.1021/jm401643m
CHEMBL3235280 110120 None 0 Human Functional pEC50 = 8.5 8.5 -3 2
Agonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by EIAAgonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by EIA
ChEMBL 615 13 2 10 3.7 CCN(CC)CCN1CCN(C(=O)CCc2cccc(CSc3nc(N)c(C#N)c(-c4ccc(NC(C)=O)cc4)n3)n2)CC1 10.1021/jm401643m
70689262 78006 None 0 Human Functional pEC50 = 8.5 8.5 1 3
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL2096798 78006 None 0 Human Functional pEC50 = 8.5 8.5 1 3
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
11386951 66906 None 0 Human Functional pEC50 = 8.5 8.5 389 2
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 527 9 5 16 -0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc([N+](=O)[O-])cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL186403 66906 None 0 Human Functional pEC50 = 8.5 8.5 389 2
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 527 9 5 16 -0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc([N+](=O)[O-])cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
377 2758 None 42 Human Functional pEC50 = 8.5 8.5 -6 10
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
425 2758 None 42 Human Functional pEC50 = 8.5 8.5 -6 10
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
448222 2758 None 42 Human Functional pEC50 = 8.5 8.5 -6 10
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
CHEMBL464859 2758 None 42 Human Functional pEC50 = 8.5 8.5 -6 10
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
56627882 118576 None 0 Human Functional pEC50 = 8.4 8.4 5 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 367 3 3 12 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414937 118576 None 0 Human Functional pEC50 = 8.4 8.4 5 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 367 3 3 12 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
10198863 171815 None 2 Human Functional pEC50 = 7.5 7.5 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 250 5 1 5 1.1 CCCCn1c(=O)c2nc[nH]c2n(CCC)c1=O 10.1021/jm00100a008
CHEMBL446679 171815 None 2 Human Functional pEC50 = 7.5 7.5 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 250 5 1 5 1.1 CCCCn1c(=O)c2nc[nH]c2n(CCC)c1=O 10.1021/jm00100a008
57388056 75512 None 0 Human Functional pEC50 = 7.5 7.5 4 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 685 12 5 10 4.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(Br)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042307 75512 None 0 Human Functional pEC50 = 7.5 7.5 4 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 685 12 5 10 4.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(Br)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
44437214 169357 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine receptor A2a expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation measured as NECA EC50 at 7 uM incubated for 15 mins in presence of [3H]cAMP by liquid scintillation counting (Rvb = 77 nM)Antagonist activity at human adenosine receptor A2a expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation measured as NECA EC50 at 7 uM incubated for 15 mins in presence of [3H]cAMP by liquid scintillation counting (Rvb = 77 nM)
ChEMBL 355 3 1 8 0.6 Cn1c(=O)c2c(nc3n2CCCN3CCc2ccc(O)cc2)n(C)c1=O 10.1016/j.bmc.2016.07.028
CHEMBL441145 169357 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine receptor A2a expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation measured as NECA EC50 at 7 uM incubated for 15 mins in presence of [3H]cAMP by liquid scintillation counting (Rvb = 77 nM)Antagonist activity at human adenosine receptor A2a expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation measured as NECA EC50 at 7 uM incubated for 15 mins in presence of [3H]cAMP by liquid scintillation counting (Rvb = 77 nM)
ChEMBL 355 3 1 8 0.6 Cn1c(=O)c2c(nc3n2CCCN3CCc2ccc(O)cc2)n(C)c1=O 10.1016/j.bmc.2016.07.028
46874560 203741 None 0 Rat Functional pEC50 = 6.5 6.5 1 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 429 4 4 10 -1.0 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#CCN4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL604019 203741 None 0 Rat Functional pEC50 = 6.5 6.5 1 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 429 4 4 10 -1.0 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#CCN4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
118734345 118673 None 0 Human Functional pEC50 = 7.5 7.5 301 2
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 545 8 5 12 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(Cl)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416780 118673 None 0 Human Functional pEC50 = 7.5 7.5 301 2
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 545 8 5 12 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(Cl)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
127038756 136943 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 544 7 4 13 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(NC(C)Cc5ccc(Br)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
CHEMBL3741931 136943 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 544 7 4 13 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(NC(C)Cc5ccc(Br)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
137651747 157573 None 0 Human Functional pEC50 = 7.5 7.5 1 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4079433 157573 None 0 Human Functional pEC50 = 7.5 7.5 1 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
10400587 21186 None 1 Human Functional pEC50 = 5.5 5.5 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 264 5 0 6 1.1 CCCCn1cnc2c1c(=O)n(C)c(=O)n2CCC 10.1021/jm00100a008
CHEMBL131275 21186 None 1 Human Functional pEC50 = 5.5 5.5 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 264 5 0 6 1.1 CCCCn1cnc2c1c(=O)n(C)c(=O)n2CCC 10.1021/jm00100a008
76329266 106118 None 0 Human Functional pEC50 = 5.5 5.5 -100 4
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 399 5 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133160 106118 None 0 Human Functional pEC50 = 5.5 5.5 -100 4
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 399 5 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
46874534 204051 None 0 Rat Functional pEC50 = 5.5 5.5 2 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 422 3 4 9 -0.1 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(C)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL605685 204051 None 0 Rat Functional pEC50 = 5.5 5.5 2 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 422 3 4 9 -0.1 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(C)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
118732979 118584 None 0 Human Functional pEC50 = 7.5 7.5 -4 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 437 5 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414945 118584 None 0 Human Functional pEC50 = 7.5 7.5 -4 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 437 5 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
168269866 190097 None 0 Human Functional pEC50 = 5.5 5.5 -11220 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 468 7 4 10 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5171042 190097 None 0 Human Functional pEC50 = 5.5 5.5 -11220 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 468 7 4 10 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
377 2758 None 42 Rat Functional pEC50 = 7.5 7.5 -22 10
Efficacy against phenylephrine precontracted tissue relaxation in rat aortaEfficacy against phenylephrine precontracted tissue relaxation in rat aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
425 2758 None 42 Rat Functional pEC50 = 7.5 7.5 -22 10
Efficacy against phenylephrine precontracted tissue relaxation in rat aortaEfficacy against phenylephrine precontracted tissue relaxation in rat aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
448222 2758 None 42 Rat Functional pEC50 = 7.5 7.5 -22 10
Efficacy against phenylephrine precontracted tissue relaxation in rat aortaEfficacy against phenylephrine precontracted tissue relaxation in rat aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
CHEMBL464859 2758 None 42 Rat Functional pEC50 = 7.5 7.5 -22 10
Efficacy against phenylephrine precontracted tissue relaxation in rat aortaEfficacy against phenylephrine precontracted tissue relaxation in rat aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
46874519 203897 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 438 4 4 10 -0.4 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(OC)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL604849 203897 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 438 4 4 10 -0.4 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(OC)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
137650918 157337 None 0 Human Functional pEC50 = 6.5 6.5 -10 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 671 14 6 13 3.4 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)cc1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4076495 157337 None 0 Human Functional pEC50 = 6.5 6.5 -10 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 671 14 6 13 3.4 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)cc1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
46874525 203936 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 436 4 4 10 -0.6 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4cccc(C=O)c4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL605055 203936 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 436 4 4 10 -0.6 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4cccc(C=O)c4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
118734349 118677 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 556 9 5 14 -0.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc([N+](=O)[O-])cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416784 118677 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 556 9 5 14 -0.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc([N+](=O)[O-])cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
11811574 79428 None 0 Human Functional pEC50 = 5.4 5.4 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 405 6 3 9 1.7 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CSC(C)C)[C@@H](O)[C@H]3O)c2n1 10.1021/jm010952v
CHEMBL2113601 79428 None 0 Human Functional pEC50 = 5.4 5.4 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 405 6 3 9 1.7 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CSC(C)C)[C@@H](O)[C@H]3O)c2n1 10.1021/jm010952v
168286257 191705 None 0 Human Functional pEC50 = 6.4 6.4 -6 4
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 863 14 6 13 6.3 Nc1sc(-c2ccc(C(=O)NCCc3ccc(CCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5195260 191705 None 0 Human Functional pEC50 = 6.4 6.4 -6 4
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 863 14 6 13 6.3 Nc1sc(-c2ccc(C(=O)NCCc3ccc(CCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
137634444 156254 None 0 Human Functional pEC50 = 5.4 5.4 -57 3
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 801 14 6 13 5.7 Nc1sc(-c2ccc(C(=O)NCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4063841 156254 None 0 Human Functional pEC50 = 5.4 5.4 -57 3
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 801 14 6 13 5.7 Nc1sc(-c2ccc(C(=O)NCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
57384543 75513 None 0 Human Functional pEC50 = 6.4 6.4 3 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 838 14 6 11 7.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)cc(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042308 75513 None 0 Human Functional pEC50 = 6.4 6.4 3 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 838 14 6 11 7.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)cc(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
168272212 190540 None 0 Human Functional pEC50 = 7.4 7.4 2 4
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 518 10 5 10 1.9 O=C(NCCCCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5178142 190540 None 0 Human Functional pEC50 = 7.4 7.4 2 4
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 518 10 5 10 1.9 O=C(NCCCCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccccc1 10.1021/acs.jmedchem.2c00320
148938245 185160 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Antagonist activity at human A2A receptor on T-cells assessed as increase of IL-2 production preincubated for 1 hr followed by addition of T-cell activator CD3/CD28 and measured after 1 hr by plate reader methodAntagonist activity at human A2A receptor on T-cells assessed as increase of IL-2 production preincubated for 1 hr followed by addition of T-cell activator CD3/CD28 and measured after 1 hr by plate reader method
ChEMBL 338 1 1 4 3.9 Nc1nc(-c2cccc(Br)c2)cn2c1nc1ccccc12 10.1016/j.ejmech.2020.113040
CHEMBL4855390 185160 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Antagonist activity at human A2A receptor on T-cells assessed as increase of IL-2 production preincubated for 1 hr followed by addition of T-cell activator CD3/CD28 and measured after 1 hr by plate reader methodAntagonist activity at human A2A receptor on T-cells assessed as increase of IL-2 production preincubated for 1 hr followed by addition of T-cell activator CD3/CD28 and measured after 1 hr by plate reader method
ChEMBL 338 1 1 4 3.9 Nc1nc(-c2cccc(Br)c2)cn2c1nc1ccccc12 10.1016/j.ejmech.2020.113040
118734362 118559 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 579 8 5 12 0.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(Cl)c(Cl)c5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3414573 118559 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 579 8 5 12 0.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(Cl)c(Cl)c5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
118734353 118681 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 555 9 6 13 -0.9 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(C(=O)O)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416788 118681 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 555 9 6 13 -0.9 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(C(=O)O)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
118734374 118699 None 0 Human Functional pEC50 = 7.4 7.4 22 2
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 642 8 4 12 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCc6ccc(C(F)(F)F)cc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416808 118699 None 0 Human Functional pEC50 = 7.4 7.4 22 2
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 642 8 4 12 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCc6ccc(C(F)(F)F)cc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
137650221 157347 None 0 Human Functional pEC50 = 7.4 7.4 1 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 463 6 3 13 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4076561 157347 None 0 Human Functional pEC50 = 7.4 7.4 1 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 463 6 3 13 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
71657835 159831 None 4 Human Functional pEC50 = 6.4 6.4 -7 4
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL4104819 159831 None 4 Human Functional pEC50 = 6.4 6.4 -7 4
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
16203542 85232 None 0 Human Functional pEC50 = 7.4 7.4 3 2
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 504 6 5 10 0.9 Nc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL225459 85232 None 0 Human Functional pEC50 = 7.4 7.4 3 2
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 504 6 5 10 0.9 Nc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
118734360 118688 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 541 9 5 13 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccccc5OC)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416795 118688 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 541 9 5 13 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccccc5OC)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
377 2758 None 42 Rat Functional pEC50 = 6.4 6.4 -22 10
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm00009a007
425 2758 None 42 Rat Functional pEC50 = 6.4 6.4 -22 10
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm00009a007
448222 2758 None 42 Rat Functional pEC50 = 6.4 6.4 -22 10
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm00009a007
CHEMBL464859 2758 None 42 Rat Functional pEC50 = 6.4 6.4 -22 10
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm00009a007
377 2758 None 42 Rat Functional pEC50 = 6.4 6.4 -22 10
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm00018a017
425 2758 None 42 Rat Functional pEC50 = 6.4 6.4 -22 10
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm00018a017
448222 2758 None 42 Rat Functional pEC50 = 6.4 6.4 -22 10
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm00018a017
CHEMBL464859 2758 None 42 Rat Functional pEC50 = 6.4 6.4 -22 10
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm00018a017
377 2758 None 42 Rat Functional pEC50 = 6.4 6.4 -22 10
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm960376g
425 2758 None 42 Rat Functional pEC50 = 6.4 6.4 -22 10
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm960376g
448222 2758 None 42 Rat Functional pEC50 = 6.4 6.4 -22 10
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm960376g
CHEMBL464859 2758 None 42 Rat Functional pEC50 = 6.4 6.4 -22 10
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm960376g
76336527 106119 None 0 Human Functional pEC50 = 6.4 6.4 -630 4
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 433 5 5 10 0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(Cl)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133161 106119 None 0 Human Functional pEC50 = 6.4 6.4 -630 4
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 433 5 5 10 0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(Cl)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
76314797 106105 None 0 Human Functional pEC50 = 5.4 5.4 -39 3
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 391 5 5 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(NC)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133081 106105 None 0 Human Functional pEC50 = 5.4 5.4 -39 3
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 391 5 5 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(NC)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
70689262 78006 None 0 Rat Functional pEC50 = 8.4 8.4 -1 3
Efficacy against phenylephrine precontracted tissue relaxation in rat aortaEfficacy against phenylephrine precontracted tissue relaxation in rat aorta
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL2096798 78006 None 0 Rat Functional pEC50 = 8.4 8.4 -1 3
Efficacy against phenylephrine precontracted tissue relaxation in rat aortaEfficacy against phenylephrine precontracted tissue relaxation in rat aorta
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
155553962 175557 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 509 8 5 12 1.2 Nc1nc(N/N=C/c2ccc(OCc3ccc(F)cc3)cc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.ejmech.2019.06.050
CHEMBL4576915 175557 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 509 8 5 12 1.2 Nc1nc(N/N=C/c2ccc(OCc3ccc(F)cc3)cc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.ejmech.2019.06.050
127041420 136898 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(NC(C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
CHEMBL3741543 136898 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(NC(C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
88448936 169962 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 377 5 5 11 -0.4 Nc1nc(N/N=C/C2CCCC2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.ejmech.2019.06.050
CHEMBL4440214 169962 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 377 5 5 11 -0.4 Nc1nc(N/N=C/C2CCCC2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.ejmech.2019.06.050
1511731 38104 None 12 Human Functional pEC50 = 8.4 8.4 -2 4
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 337 3 1 6 2.9 COc1ccc(C(=O)Nc2nc(C)c3cc4c(cc3n2)OCO4)cc1 10.1016/j.ejmech.2023.115419
CHEMBL1460863 38104 None 12 Human Functional pEC50 = 8.4 8.4 -2 4
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 337 3 1 6 2.9 COc1ccc(C(=O)Nc2nc(C)c3cc4c(cc3n2)OCO4)cc1 10.1016/j.ejmech.2023.115419
137647420 157793 None 0 Human Functional pEC50 = 8.4 8.4 -2 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 501 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4081876 157793 None 0 Human Functional pEC50 = 8.4 8.4 -2 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 501 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
136707040 196261 None 2 Human Functional pEC50 = 8.4 8.4 -2 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 330 3 1 4 1.8 O=C(CC1CCCC1)N1CCc2c(nc(N3CCCC3)[nH]c2=O)C1 10.1016/j.ejmech.2023.115419
CHEMBL5419943 196261 None 2 Human Functional pEC50 = 8.4 8.4 -2 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 330 3 1 4 1.8 O=C(CC1CCCC1)N1CCc2c(nc(N3CCCC3)[nH]c2=O)C1 10.1016/j.ejmech.2023.115419
2917099 52161 None 8 Human Functional pEC50 = 8.3 8.3 -2 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 315 3 1 5 3.0 CC(C)C(=O)Nc1ncc2c(n1)CC(c1cccs1)CC2=O 10.1016/j.ejmech.2023.115419
CHEMBL1587915 52161 None 8 Human Functional pEC50 = 8.3 8.3 -2 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 315 3 1 5 3.0 CC(C)C(=O)Nc1ncc2c(n1)CC(c1cccs1)CC2=O 10.1016/j.ejmech.2023.115419
56720528 195296 None 5 Human Functional pEC50 = 8.3 8.3 -1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 295 2 1 5 2.4 Cc1ccc2nc(C(=O)Nc3cnc4n3CCCC4)cn2c1 10.1016/j.ejmech.2023.115419
CHEMBL5400258 195296 None 5 Human Functional pEC50 = 8.3 8.3 -1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 295 2 1 5 2.4 Cc1ccc2nc(C(=O)Nc3cnc4n3CCCC4)cn2c1 10.1016/j.ejmech.2023.115419
56751513 195991 None 5 Human Functional pEC50 = 8.3 8.3 -1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 316 2 1 6 2.2 O=C(Nc1cnc2n1CCCC2)c1cn2cc(Cl)cnc2n1 10.1016/j.ejmech.2023.115419
CHEMBL5414806 195991 None 5 Human Functional pEC50 = 8.3 8.3 -1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 316 2 1 6 2.2 O=C(Nc1cnc2n1CCCC2)c1cn2cc(Cl)cnc2n1 10.1016/j.ejmech.2023.115419
24241730 196416 None 3 Human Functional pEC50 = 8.3 8.3 -1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 275 5 1 4 3.3 CC(Sc1nnc(C(C)C)[nH]1)C(=O)c1ccccc1 10.1016/j.ejmech.2023.115419
CHEMBL5423524 196416 None 3 Human Functional pEC50 = 8.3 8.3 -1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 275 5 1 4 3.3 CC(Sc1nnc(C(C)C)[nH]1)C(=O)c1ccccc1 10.1016/j.ejmech.2023.115419
45216745 196544 None 5 Human Functional pEC50 = 8.3 8.3 -1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 278 6 2 8 0.0 COCC(O)CNc1ncc(C)c(-c2ncnn2C)n1 10.1016/j.ejmech.2023.115419
CHEMBL5426384 196544 None 5 Human Functional pEC50 = 8.3 8.3 -1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 278 6 2 8 0.0 COCC(O)CNc1ncc(C)c(-c2ncnn2C)n1 10.1016/j.ejmech.2023.115419
155524113 170974 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 420 5 5 12 -0.5 Nc1nc(N/N=C/c2cccnc2Cl)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.ejmech.2019.06.050
CHEMBL4454157 170974 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 420 5 5 12 -0.5 Nc1nc(N/N=C/c2cccnc2Cl)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.ejmech.2019.06.050
377 2758 None 42 Human Functional pEC50 = 8.3 8.3 -6 10
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
425 2758 None 42 Human Functional pEC50 = 8.3 8.3 -6 10
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
448222 2758 None 42 Human Functional pEC50 = 8.3 8.3 -6 10
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
CHEMBL464859 2758 None 42 Human Functional pEC50 = 8.3 8.3 -6 10
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
118734365 118692 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 563 8 5 12 0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(Cl)cc5F)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416799 118692 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 563 8 5 12 0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(Cl)cc5F)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
377 2758 None 42 Human Functional pEC50 = 7.4 7.4 -6 10
G-protein activation in human Adenosine A2A receptor expressing CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressing CHO cells using cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm010952v
425 2758 None 42 Human Functional pEC50 = 7.4 7.4 -6 10
G-protein activation in human Adenosine A2A receptor expressing CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressing CHO cells using cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm010952v
448222 2758 None 42 Human Functional pEC50 = 7.4 7.4 -6 10
G-protein activation in human Adenosine A2A receptor expressing CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressing CHO cells using cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm010952v
CHEMBL464859 2758 None 42 Human Functional pEC50 = 7.4 7.4 -6 10
G-protein activation in human Adenosine A2A receptor expressing CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressing CHO cells using cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm010952v
137657841 159664 None 0 Human Functional pEC50 = 7.4 7.4 -1 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4102750 159664 None 0 Human Functional pEC50 = 7.4 7.4 -1 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
46874521 203898 None 0 Rat Functional pEC50 = 6.4 6.4 -2 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 422 4 4 9 -0.2 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#CCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL604851 203898 None 0 Rat Functional pEC50 = 6.4 6.4 -2 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 422 4 4 9 -0.2 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#CCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
46874626 203742 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 423 3 5 10 -0.9 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(N)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL604023 203742 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 423 3 5 10 -0.9 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(N)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
46874556 203703 None 0 Rat Functional pEC50 = 6.4 6.4 2 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 444 4 4 11 -2.2 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#CCN4CCN(C)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL603809 203703 None 0 Rat Functional pEC50 = 6.4 6.4 2 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 444 4 4 11 -2.2 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#CCN4CCN(C)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
118734361 118689 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 563 8 5 12 0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(F)c(Cl)c5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416796 118689 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 563 8 5 12 0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(F)c(Cl)c5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
57387825 75505 None 0 Human Functional pEC50 = 7.4 7.4 6 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 505 7 5 10 0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(Br)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042300 75505 None 0 Human Functional pEC50 = 7.4 7.4 6 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 505 7 5 10 0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(Br)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
118734346 118674 None 0 Human Functional pEC50 = 7.4 7.4 218 2
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 589 8 5 12 0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(Br)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416781 118674 None 0 Human Functional pEC50 = 7.4 7.4 218 2
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 589 8 5 12 0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(Br)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
118734373 118698 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 592 8 4 12 1.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCc6ccc(F)cc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416807 118698 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 592 8 4 12 1.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCc6ccc(F)cc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
14969715 206252 None 1 Human Functional pEC50 = 4.4 4.4 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 208 3 2 4 0.2 CCCCn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm00100a008
CHEMBL68278 206252 None 1 Human Functional pEC50 = 4.4 4.4 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 208 3 2 4 0.2 CCCCn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm00100a008
137649841 157522 None 0 Human Functional pEC50 = 6.4 6.4 -3 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 656 14 5 12 3.8 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cc(C(=O)c3ccccc3)cs2)c1 10.1021/acs.jmedchem.8b00047
CHEMBL4078771 157522 None 0 Human Functional pEC50 = 6.4 6.4 -3 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 656 14 5 12 3.8 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cc(C(=O)c3ccccc3)cs2)c1 10.1021/acs.jmedchem.8b00047
118734341 118669 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 525 9 5 12 -0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCCN4CCN(c5ccccc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416776 118669 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 525 9 5 12 -0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCCN4CCN(c5ccccc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL5093654 217928 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Partial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based AssayPartial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based Assay
ChEMBL None None None N#Cc1c(SCc2ncc[nH]2)nc(N)nc1-c1ccccc1 10.1021/acs.jmedchem.0c01856
9996838 79278 None 0 Rat Functional pEC50 = 6.4 6.4 -2 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 332 3 4 9 -1.9 C#Cc1nc(N)c2ncn([C@@H]3O[C@H](C(=O)NCC)[C@@H](O)[C@H]3O)c2n1 10.1021/jm00009a007
CHEMBL2113449 79278 None 0 Rat Functional pEC50 = 6.4 6.4 -2 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 332 3 4 9 -1.9 C#Cc1nc(N)c2ncn([C@@H]3O[C@H](C(=O)NCC)[C@@H](O)[C@H]3O)c2n1 10.1021/jm00009a007
57384287 75506 None 0 Human Functional pEC50 = 7.4 7.4 33 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 658 9 6 11 3.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)cc(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042301 75506 None 0 Human Functional pEC50 = 7.4 7.4 33 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 658 9 6 11 3.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)cc(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
377 2758 None 42 Human Functional pEC50 = 7.4 7.4 -6 10
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C5MD00086F
425 2758 None 42 Human Functional pEC50 = 7.4 7.4 -6 10
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C5MD00086F
448222 2758 None 42 Human Functional pEC50 = 7.4 7.4 -6 10
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C5MD00086F
CHEMBL464859 2758 None 42 Human Functional pEC50 = 7.4 7.4 -6 10
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C5MD00086F
118734355 118683 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 545 8 5 12 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5cccc(Cl)c5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416790 118683 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 545 8 5 12 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5cccc(Cl)c5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
46893147 141252 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine receptor A2a expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation measured as NECA EC50 at 5 uM incubated for 15 mins in presence of [3H]cAMP by liquid scintillation counting (Rvb = 68 nM)Antagonist activity at human adenosine receptor A2a expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation measured as NECA EC50 at 5 uM incubated for 15 mins in presence of [3H]cAMP by liquid scintillation counting (Rvb = 68 nM)
ChEMBL 454 9 0 9 1.6 CCN(CC)CCOc1ccc(CCN2CCCn3c2nc2c3c(=O)n(C)c(=O)n2C)cc1 10.1016/j.bmc.2016.07.028
CHEMBL3827859 141252 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine receptor A2a expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation measured as NECA EC50 at 5 uM incubated for 15 mins in presence of [3H]cAMP by liquid scintillation counting (Rvb = 68 nM)Antagonist activity at human adenosine receptor A2a expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation measured as NECA EC50 at 5 uM incubated for 15 mins in presence of [3H]cAMP by liquid scintillation counting (Rvb = 68 nM)
ChEMBL 454 9 0 9 1.6 CCN(CC)CCOc1ccc(CCN2CCCn3c2nc2c3c(=O)n(C)c(=O)n2C)cc1 10.1016/j.bmc.2016.07.028
46874581 203938 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 458 3 4 9 0.7 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4cccc5ccccc45)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL605057 203938 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 458 3 4 9 0.7 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4cccc5ccccc45)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
118734348 118676 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 579 8 5 12 0.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(C(F)(F)F)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416783 118676 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 579 8 5 12 0.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(C(F)(F)F)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
16389231 196198 None 3 Human Functional pEC50 = 7.3 7.3 -1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 289 2 1 4 3.5 N#CC1(C(=O)Nc2nc3ccc(F)cc3s2)CCCC1 10.1016/j.ejmech.2023.115419
CHEMBL5418682 196198 None 3 Human Functional pEC50 = 7.3 7.3 -1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 289 2 1 4 3.5 N#CC1(C(=O)Nc2nc3ccc(F)cc3s2)CCCC1 10.1016/j.ejmech.2023.115419
15931309 115323 None 7 Human Functional pEC50 = 5.3 5.3 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 194 1 1 5 -0.6 CCn1c(=O)n(C)c(=O)c2[nH]cnc21 10.1021/jm00100a008
CHEMBL334813 115323 None 7 Human Functional pEC50 = 5.3 5.3 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 194 1 1 5 -0.6 CCn1c(=O)n(C)c(=O)c2[nH]cnc21 10.1021/jm00100a008
118734366 118693 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 647 10 6 13 -0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(CC(=O)O)cc5Br)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416800 118693 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 647 10 6 13 -0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(CC(=O)O)cc5Br)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
127038339 136885 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 400 6 5 10 0.1 CC(Cc1ccccc1)Nc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1039/C5MD00086F
CHEMBL3741393 136885 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 400 6 5 10 0.1 CC(Cc1ccccc1)Nc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1039/C5MD00086F
10434186 79386 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 456 7 5 13 0.0 Nc1nc(N/N=C/C=C/c2ccc([N+](=O)[O-])cc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm00018a017
CHEMBL2113556 79386 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 456 7 5 13 0.0 Nc1nc(N/N=C/C=C/c2ccc([N+](=O)[O-])cc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm00018a017
137652475 157237 None 0 Human Functional pEC50 = 5.3 5.3 -72 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 829 16 6 13 6.5 Nc1sc(-c2ccc(C(=O)NCCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4075186 157237 None 0 Human Functional pEC50 = 5.3 5.3 -72 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 829 16 6 13 6.5 Nc1sc(-c2ccc(C(=O)NCCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
46874622 203704 None 0 Rat Functional pEC50 = 6.3 6.3 -1 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 409 3 4 10 -1.0 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4cccnc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL603812 203704 None 0 Rat Functional pEC50 = 6.3 6.3 -1 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 409 3 4 10 -1.0 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4cccnc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
10251529 87218 None 0 Human Functional pEC50 = 6.3 6.3 28 2
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation countingAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation counting
ChEMBL 419 5 5 11 0.1 Nc1nc(N/N=C/c2ccc(Cl)cc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.bmc.2012.11.021
CHEMBL2326842 87218 None 0 Human Functional pEC50 = 6.3 6.3 28 2
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation countingAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation counting
ChEMBL 419 5 5 11 0.1 Nc1nc(N/N=C/c2ccc(Cl)cc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.bmc.2012.11.021
10478926 79279 None 0 Rat Functional pEC50 = 6.3 6.3 12 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 450 6 4 9 0.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#CCCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL2113450 79279 None 0 Rat Functional pEC50 = 6.3 6.3 12 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 450 6 4 9 0.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#CCCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
10478926 79279 None 0 Rat Functional pEC50 = 6.3 6.3 12 2
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 450 6 4 9 0.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#CCCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm960376g
CHEMBL2113450 79279 None 0 Rat Functional pEC50 = 6.3 6.3 12 2
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 450 6 4 9 0.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#CCCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm960376g
118732975 118580 None 0 Human Functional pEC50 = 8.3 8.3 -2 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414941 118580 None 0 Human Functional pEC50 = 8.3 8.3 -2 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
45803129 195879 None 4 Human Functional pEC50 = 8.3 8.3 -2 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 345 6 2 5 2.9 CC(=O)NC(CC(=O)Nc1nc(C(C)=O)cs1)c1ccc(C)cc1 10.1016/j.ejmech.2023.115419
CHEMBL5412498 195879 None 4 Human Functional pEC50 = 8.3 8.3 -2 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 345 6 2 5 2.9 CC(=O)NC(CC(=O)Nc1nc(C(C)=O)cs1)c1ccc(C)cc1 10.1016/j.ejmech.2023.115419
127038752 136832 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 466 7 4 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(NC(C)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
CHEMBL3740959 136832 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 466 7 4 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(NC(C)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
155526752 171252 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 436 5 5 12 0.0 Nc1nc(N/N=C/c2ccc3ncccc3c2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.ejmech.2019.06.050
CHEMBL4458638 171252 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 436 5 5 12 0.0 Nc1nc(N/N=C/c2ccc3ncccc3c2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.ejmech.2019.06.050
57387337 75502 None 0 Human Functional pEC50 = 8.3 8.3 -15 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 326 3 4 9 -1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042297 75502 None 0 Human Functional pEC50 = 8.3 8.3 -15 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 326 3 4 9 -1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
155559963 175000 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 461 6 5 11 1.1 Nc1nc(N/N=C/c2ccc(-c3ccccc3)cc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.ejmech.2019.06.050
CHEMBL4564192 175000 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 461 6 5 11 1.1 Nc1nc(N/N=C/c2ccc(-c3ccccc3)cc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.ejmech.2019.06.050
118714540 114575 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human adenosine A2a receptor expressed in CHO cells assessed as stimulation of cAMP formation after 24 hrsAgonist activity at human adenosine A2a receptor expressed in CHO cells assessed as stimulation of cAMP formation after 24 hrs
ChEMBL 677 13 6 15 1.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(CCC(=O)Nc5ccc(OC(C)=O)c([N+](=O)[O-])c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/ml5002486
CHEMBL3335523 114575 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human adenosine A2a receptor expressed in CHO cells assessed as stimulation of cAMP formation after 24 hrsAgonist activity at human adenosine A2a receptor expressed in CHO cells assessed as stimulation of cAMP formation after 24 hrs
ChEMBL 677 13 6 15 1.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(CCC(=O)Nc5ccc(OC(C)=O)c([N+](=O)[O-])c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/ml5002486
377 2758 None 42 Human Functional pEC50 = 7.3 7.3 -6 10
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
425 2758 None 42 Human Functional pEC50 = 7.3 7.3 -6 10
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
448222 2758 None 42 Human Functional pEC50 = 7.3 7.3 -6 10
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
CHEMBL464859 2758 None 42 Human Functional pEC50 = 7.3 7.3 -6 10
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
169317 1201 None 26 Human Functional pEC50 = 7.3 7.3 30 2
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 10.1021/jm00100a008
427 1201 None 26 Human Functional pEC50 = 7.3 7.3 30 2
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 10.1021/jm00100a008
CHEMBL157655 1201 None 26 Human Functional pEC50 = 7.3 7.3 30 2
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 10.1021/jm00100a008
11047444 79432 None 0 Human Functional pEC50 = 6.3 6.3 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 391 6 3 9 1.3 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CSCC)[C@@H](O)[C@H]3O)c2n1 10.1021/jm010952v
CHEMBL2113605 79432 None 0 Human Functional pEC50 = 6.3 6.3 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 391 6 3 9 1.3 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CSCC)[C@@H](O)[C@H]3O)c2n1 10.1021/jm010952v
11025671 79414 None 0 Human Functional pEC50 = 5.3 5.3 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 395 7 4 11 0.8 CSC[C@H]1O[C@@H](n2cnc3c(N)nc(N/N=C/CC(C)C)nc32)[C@H](O)[C@@H]1O 10.1021/jm010952v
CHEMBL2113588 79414 None 0 Human Functional pEC50 = 5.3 5.3 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 395 7 4 11 0.8 CSC[C@H]1O[C@@H](n2cnc3c(N)nc(N/N=C/CC(C)C)nc32)[C@H](O)[C@@H]1O 10.1021/jm010952v
10377425 99395 None 2 Human Functional pEC50 = 5.3 5.3 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 250 4 0 6 0.7 CCCn1cnc2c1c(=O)n(C)c(=O)n2CCC 10.1021/jm00100a008
CHEMBL282310 99395 None 2 Human Functional pEC50 = 5.3 5.3 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 250 4 0 6 0.7 CCCn1cnc2c1c(=O)n(C)c(=O)n2CCC 10.1021/jm00100a008
76329264 106109 None 0 Human Functional pEC50 = 6.3 6.3 -12 3
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 405 6 5 10 -0.0 CCNc1nc(NC2CCCC2)c2ncn([C@@H]3O[C@H](C(=O)NC)[C@@H](O)[C@H]3O)c2n1 10.1039/C3MD00364G
CHEMBL3133151 106109 None 0 Human Functional pEC50 = 6.3 6.3 -12 3
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 405 6 5 10 -0.0 CCNc1nc(NC2CCCC2)c2ncn([C@@H]3O[C@H](C(=O)NC)[C@@H](O)[C@H]3O)c2n1 10.1039/C3MD00364G
76325693 106106 None 0 Human Functional pEC50 = 5.3 5.3 -7 2
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 405 5 4 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N(C)C)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133082 106106 None 0 Human Functional pEC50 = 5.3 5.3 -7 2
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 405 5 4 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N(C)C)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
118734372 118697 None 0 Human Functional pEC50 = 7.3 7.3 17 2
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 608 8 4 12 1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCc6ccc(Cl)cc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416806 118697 None 0 Human Functional pEC50 = 7.3 7.3 17 2
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 608 8 4 12 1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCc6ccc(Cl)cc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
147996856 185619 None 0 Human Functional pEC50 = 6.3 6.3 4 2
Antagonist activity at human A2A receptor on T-cells assessed as increase of IL-2 production preincubated for 1 hr followed by addition of T-cell activator CD3/CD28 and measured after 1 hr by plate reader methodAntagonist activity at human A2A receptor on T-cells assessed as increase of IL-2 production preincubated for 1 hr followed by addition of T-cell activator CD3/CD28 and measured after 1 hr by plate reader method
ChEMBL 326 2 1 5 3.4 COc1cccc(-c2cn3c(nc4cc(F)c(F)cc43)c(N)n2)c1 10.1016/j.ejmech.2020.113040
CHEMBL4862573 185619 None 0 Human Functional pEC50 = 6.3 6.3 4 2
Antagonist activity at human A2A receptor on T-cells assessed as increase of IL-2 production preincubated for 1 hr followed by addition of T-cell activator CD3/CD28 and measured after 1 hr by plate reader methodAntagonist activity at human A2A receptor on T-cells assessed as increase of IL-2 production preincubated for 1 hr followed by addition of T-cell activator CD3/CD28 and measured after 1 hr by plate reader method
ChEMBL 326 2 1 5 3.4 COc1cccc(-c2cn3c(nc4cc(F)c(F)cc43)c(N)n2)c1 10.1016/j.ejmech.2020.113040
10048927 79384 None 0 Rat Functional pEC50 = 6.3 6.3 3 2
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 441 7 5 12 0.1 COc1ccccc1/C=C/C=N/Nc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm00018a017
CHEMBL2113554 79384 None 0 Rat Functional pEC50 = 6.3 6.3 3 2
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 441 7 5 12 0.1 COc1ccccc1/C=C/C=N/Nc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm00018a017
118734363 118690 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 579 8 5 12 0.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5cc(Cl)cc(Cl)c5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416797 118690 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 579 8 5 12 0.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5cc(Cl)cc(Cl)c5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
46874569 203816 None 0 Rat Functional pEC50 = 6.3 6.3 -1 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 431 4 4 11 -2.2 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#CCN4CCOCC4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL604440 203816 None 0 Rat Functional pEC50 = 6.3 6.3 -1 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 431 4 4 11 -2.2 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#CCN4CCOCC4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
137650899 157295 None 0 Human Functional pEC50 = 7.3 7.3 2 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 413 6 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4076003 157295 None 0 Human Functional pEC50 = 7.3 7.3 2 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 413 6 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
169662 79349 None 53 Human Functional pEC50 = 5.3 5.3 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 393 2 4 9 -1.4 Nc1nc(I)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm010952v
CHEMBL2113519 79349 None 53 Human Functional pEC50 = 5.3 5.3 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 393 2 4 9 -1.4 Nc1nc(I)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm010952v
168297825 192392 None 0 Human Functional pEC50 = 6.3 6.3 -891 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5205907 192392 None 0 Human Functional pEC50 = 6.3 6.3 -891 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
137646828 158098 None 0 Human Functional pEC50 = 7.3 7.3 1 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 856 16 6 13 6.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCCCNC(=O)c4ccc(-c5sc(N)c(C(=O)c6ccccc6)c5-c5cccc(C(F)(F)F)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.8b00047
CHEMBL4085418 158098 None 0 Human Functional pEC50 = 7.3 7.3 1 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 856 16 6 13 6.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCCCNC(=O)c4ccc(-c5sc(N)c(C(=O)c6ccccc6)c5-c5cccc(C(F)(F)F)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.8b00047
168292290 192074 None 0 Human Functional pEC50 = 5.2 5.2 -10964 2
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 457 7 4 11 0.9 COc1cccc(O[C@@H]2CCC[C@H]2Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c1 10.1021/acs.jmedchem.2c01414
CHEMBL5201013 192074 None 0 Human Functional pEC50 = 5.2 5.2 -10964 2
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 457 7 4 11 0.9 COc1cccc(O[C@@H]2CCC[C@H]2Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c1 10.1021/acs.jmedchem.2c01414
10503806 86032 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 452 8 4 9 1.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(/C=C/CCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm960376g
CHEMBL2304158 86032 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 452 8 4 9 1.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(/C=C/CCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm960376g
75398270 196724 None 3 Human Functional pEC50 = 7.2 7.2 -2 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 294 4 1 5 2.5 COc1cccc(C(=O)Nc2cnn(-c3ccccc3)n2)c1 10.1016/j.ejmech.2023.115419
CHEMBL5430803 196724 None 3 Human Functional pEC50 = 7.2 7.2 -2 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 294 4 1 5 2.5 COc1cccc(C(=O)Nc2cnn(-c3ccccc3)n2)c1 10.1016/j.ejmech.2023.115419
10243194 99580 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 236 3 0 6 0.3 CCCn1c(=O)n(C)c(=O)c2c1ncn2CC 10.1021/jm00100a008
CHEMBL283412 99580 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 236 3 0 6 0.3 CCCn1c(=O)n(C)c(=O)c2c1ncn2CC 10.1021/jm00100a008
9977702 79357 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 390 7 4 9 0.4 CCCC/C=C/c1nc(N)c2ncn([C@@H]3O[C@H](C(=O)NCC)[C@@H](O)[C@H]3O)c2n1 10.1021/jm960376g
CHEMBL2113528 79357 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 390 7 4 9 0.4 CCCC/C=C/c1nc(N)c2ncn([C@@H]3O[C@H](C(=O)NCC)[C@@H](O)[C@H]3O)c2n1 10.1021/jm960376g
164437 64 None 20 Rat Functional pEC50 = 6.2 6.2 7 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 388 5 4 9 -0.3 CCCCC#Cc1nc(N)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)C(=O)NCC 10.1021/jm00009a007
373 64 None 20 Rat Functional pEC50 = 6.2 6.2 7 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 388 5 4 9 -0.3 CCCCC#Cc1nc(N)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)C(=O)NCC 10.1021/jm00009a007
CHEMBL410873 64 None 20 Rat Functional pEC50 = 6.2 6.2 7 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 388 5 4 9 -0.3 CCCCC#Cc1nc(N)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)C(=O)NCC 10.1021/jm00009a007
164437 64 None 20 Rat Functional pEC50 = 6.2 6.2 7 2
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 388 5 4 9 -0.3 CCCCC#Cc1nc(N)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)C(=O)NCC 10.1021/jm960376g
373 64 None 20 Rat Functional pEC50 = 6.2 6.2 7 2
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 388 5 4 9 -0.3 CCCCC#Cc1nc(N)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)C(=O)NCC 10.1021/jm960376g
CHEMBL410873 64 None 20 Rat Functional pEC50 = 6.2 6.2 7 2
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 388 5 4 9 -0.3 CCCCC#Cc1nc(N)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)C(=O)NCC 10.1021/jm960376g
40149613 197019 None 3 Human Functional pEC50 = 8.2 8.2 -1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 277 4 2 4 2.3 O=C(Nc1nc2ccccc2s1)N(CCO)C1CC1 10.1016/j.ejmech.2023.115419
CHEMBL5436964 197019 None 3 Human Functional pEC50 = 8.2 8.2 -1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 277 4 2 4 2.3 O=C(Nc1nc2ccccc2s1)N(CCO)C1CC1 10.1016/j.ejmech.2023.115419
57388055 75511 None 0 Human Functional pEC50 = 8.2 8.2 5 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 622 12 6 11 3.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(N)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042306 75511 None 0 Human Functional pEC50 = 8.2 8.2 5 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 622 12 6 11 3.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(N)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
57384289 75508 None 0 Human Functional pEC50 = 8.2 8.2 18 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 630 13 6 13 2.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)CCCC[C@H]5CCSS5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042303 75508 None 0 Human Functional pEC50 = 8.2 8.2 18 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 630 13 6 13 2.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)CCCC[C@H]5CCSS5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
11157262 123707 None 0 Rat Functional pEC50 = 8.2 8.2 -4 3
Efficacy against phenylephrine precontracted tissue relaxation in rat aortaEfficacy against phenylephrine precontracted tissue relaxation in rat aorta
ChEMBL 560 8 5 14 0.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Br)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL361925 123707 None 0 Rat Functional pEC50 = 8.2 8.2 -4 3
Efficacy against phenylephrine precontracted tissue relaxation in rat aortaEfficacy against phenylephrine precontracted tissue relaxation in rat aorta
ChEMBL 560 8 5 14 0.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Br)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
137638080 156927 None 0 Human Functional pEC50 = 8.2 8.2 -3 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 457 6 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4071338 156927 None 0 Human Functional pEC50 = 8.2 8.2 -3 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 457 6 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
135629993 195205 None 7 Human Functional pEC50 = 8.2 8.2 1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 322 3 1 5 3.1 O=c1[nH]c(N2CCCCC2)nc2nccc(/C=C/c3ccco3)c12 10.1016/j.ejmech.2023.115419
CHEMBL5398733 195205 None 7 Human Functional pEC50 = 8.2 8.2 1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 322 3 1 5 3.1 O=c1[nH]c(N2CCCCC2)nc2nccc(/C=C/c3ccco3)c12 10.1016/j.ejmech.2023.115419
246396 195457 None 5 Human Functional pEC50 = 8.2 8.2 2 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 283 5 3 8 -2.2 Cn1c(=O)c2[nH]c(N(CCO)CCO)nc2n(C)c1=O 10.1016/j.ejmech.2023.115419
CHEMBL5404183 195457 None 5 Human Functional pEC50 = 8.2 8.2 2 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 283 5 3 8 -2.2 Cn1c(=O)c2[nH]c(N(CCO)CCO)nc2n(C)c1=O 10.1016/j.ejmech.2023.115419
137641990 158171 None 0 Human Functional pEC50 = 7.2 7.2 -1 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 447 6 3 13 0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4086325 158171 None 0 Human Functional pEC50 = 7.2 7.2 -1 4
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 447 6 3 13 0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
161713 98844 None 45 Human Functional pEC50 = 6.2 6.2 33 2
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 250 4 0 6 0.7 CCCn1c(=O)c2c(ncn2C)n(CCC)c1=O 10.1021/jm00100a008
CHEMBL278332 98844 None 45 Human Functional pEC50 = 6.2 6.2 33 2
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 250 4 0 6 0.7 CCCn1c(=O)c2c(ncn2C)n(CCC)c1=O 10.1021/jm00100a008
118734351 118679 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 541 9 5 13 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(OC)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416786 118679 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 541 9 5 13 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(OC)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
128525 154814 None 5 Human Functional pEC50 = 4.2 4.2 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm00100a008
CHEMBL39986 154814 None 5 Human Functional pEC50 = 4.2 4.2 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm00100a008
45503815 196995 None 3 Human Functional pEC50 = 7.2 7.2 1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 314 2 1 6 3.1 Cc1nnsc1C(=O)Nc1nc2c(s1)Cc1ccccc1-2 10.1016/j.ejmech.2023.115419
CHEMBL5436271 196995 None 3 Human Functional pEC50 = 7.2 7.2 1 2
Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)Antagonist activity at human A2AR expressed in Flp-In-CHO cells assessed as NECA-mediated cAMP accumulation incubated for 30 to 60 mins followed by NECA addition measured after 30 mins by LANCE cAMP assay (Rvb = 8.38 +/- 0.03 No_unit)
ChEMBL 314 2 1 6 3.1 Cc1nnsc1C(=O)Nc1nc2c(s1)Cc1ccccc1-2 10.1016/j.ejmech.2023.115419
168283120 191170 None 0 Human Functional pEC50 = 5.2 5.2 -47863 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 498 8 4 11 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(OC)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5187330 191170 None 0 Human Functional pEC50 = 5.2 5.2 -47863 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 498 8 4 11 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(OC)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
10411731 79388 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 456 7 5 13 0.0 Nc1nc(N/N=C/C=C/c2ccccc2[N+](=O)[O-])nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm00018a017
CHEMBL2113558 79388 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 456 7 5 13 0.0 Nc1nc(N/N=C/C=C/c2ccccc2[N+](=O)[O-])nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm00018a017
46874544 204155 None 0 Rat Functional pEC50 = 5.2 5.2 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 451 4 5 10 -1.3 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(C(N)=O)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL606315 204155 None 0 Rat Functional pEC50 = 5.2 5.2 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 451 4 5 10 -1.3 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(C(N)=O)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
137641858 158399 None 0 Human Functional pEC50 = 6.2 6.2 -7 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 696 13 5 11 5.3 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccc(-c2sccc2-c2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.8b00047
CHEMBL4089092 158399 None 0 Human Functional pEC50 = 6.2 6.2 -7 4
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 696 13 5 11 5.3 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccc(-c2sccc2-c2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.8b00047
162645916 179602 None 0 Human Functional pEC50 = 6.2 6.2 -8 4
Irreversible agonist activity at human adenosine A2A 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 A2A receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 414 6 4 11 0.8 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccc(CN=C=S)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.6b01561
CHEMBL4741079 179602 None 0 Human Functional pEC50 = 6.2 6.2 -8 4
Irreversible agonist activity at human adenosine A2A 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 A2A receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 414 6 4 11 0.8 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccc(CN=C=S)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.6b01561
46874586 203978 None 0 Rat Functional pEC50 = 5.2 5.2 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 447 4 4 10 -0.4 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(CC#N)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL605264 203978 None 0 Rat Functional pEC50 = 5.2 5.2 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 447 4 4 10 -0.4 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(CC#N)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
57388054 75510 None 0 Human Functional pEC50 = 7.2 7.2 1 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 607 12 5 10 3.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042305 75510 None 0 Human Functional pEC50 = 7.2 7.2 1 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 607 12 5 10 3.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
46874620 203670 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 424 3 5 10 -0.7 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(O)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL603602 203670 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 424 3 5 10 -0.7 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#Cc4ccc(O)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
132991434 180064 None 0 Human Functional pEC50 = 7.2 7.2 -7 4
Irreversible agonist activity at human adenosine A2A 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 A2A receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 564 8 6 12 2.4 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccc(CNC(=S)Nc5ccc(N=C=S)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.6b01561
CHEMBL4746617 180064 None 0 Human Functional pEC50 = 7.2 7.2 -7 4
Irreversible agonist activity at human adenosine A2A 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 A2A receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 564 8 6 12 2.4 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccc(CNC(=S)Nc5ccc(N=C=S)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.6b01561
132991435 180904 None 0 Human Functional pEC50 = 7.2 7.2 -70 4
Irreversible agonist activity at human adenosine A2A 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 A2A receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 558 8 5 12 0.8 O=C(NCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccc(S(=O)(=O)F)cc1 10.1021/acs.jmedchem.6b01561
CHEMBL4756472 180904 None 0 Human Functional pEC50 = 7.2 7.2 -70 4
Irreversible agonist activity at human adenosine A2A 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 A2A receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 558 8 5 12 0.8 O=C(NCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccc(S(=O)(=O)F)cc1 10.1021/acs.jmedchem.6b01561
46875672 204932 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 390 7 4 9 0.4 CCCC/C=C\c1nc(N)c2ncn(C3O[C@H](C(=O)NCC)[C@@H](O)[C@H]3O)c2n1 10.1021/jm960376g
CHEMBL611256 204932 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 390 7 4 9 0.4 CCCC/C=C\c1nc(N)c2ncn(C3O[C@H](C(=O)NCC)[C@@H](O)[C@H]3O)c2n1 10.1021/jm960376g
168290340 192002 None 0 Human Functional pEC50 = 5.2 5.2 -1995 3
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 475 7 4 10 1.6 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5199871 192002 None 0 Human Functional pEC50 = 5.2 5.2 -1995 3
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 475 7 4 10 1.6 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
10048928 79390 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 441 7 5 12 0.1 COc1ccc(/C=C/C=N/Nc2nc(N)c3ncn([C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)cc1 10.1021/jm00018a017
CHEMBL2113560 79390 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 441 7 5 12 0.1 COc1ccc(/C=C/C=N/Nc2nc(N)c3ncn([C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)cc1 10.1021/jm00018a017
350737 21051 None 22 Human Functional pEC50 = 4.2 4.2 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 180 1 2 4 -0.6 CCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1021/jm00100a008
CHEMBL131181 21051 None 22 Human Functional pEC50 = 4.2 4.2 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 180 1 2 4 -0.6 CCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1021/jm00100a008
118732976 118581 None 0 Human Functional pEC50 = 8.1 8.1 -1 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 427 5 3 12 0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N[C@H]5C[C@@H]6CC[C@@H]5C6)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414942 118581 None 0 Human Functional pEC50 = 8.1 8.1 -1 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 427 5 3 12 0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N[C@H]5C[C@@H]6CC[C@@H]5C6)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
2844 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO cellsAgonist activity at human adenosine A2A receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
60961 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO cellsAgonist activity at human adenosine A2A receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
60961.0 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO cellsAgonist activity at human adenosine A2A receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
90 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO cellsAgonist activity at human adenosine A2A receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
CHEMBL477 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO cellsAgonist activity at human adenosine A2A receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
DB00640 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO cellsAgonist activity at human adenosine A2A receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
2844 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
60961 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
60961.0 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
90 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
CHEMBL477 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
DB00640 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
2844 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human recombinant adenosine receptor A2a by cAMP assayAgonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
60961 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human recombinant adenosine receptor A2a by cAMP assayAgonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
60961.0 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human recombinant adenosine receptor A2a by cAMP assayAgonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
90 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human recombinant adenosine receptor A2a by cAMP assayAgonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
CHEMBL477 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human recombinant adenosine receptor A2a by cAMP assayAgonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
DB00640 283 None 61 Human Functional pEC50 = 6.2 6.2 -7 5
Agonist activity at human recombinant adenosine receptor A2a by cAMP assayAgonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
11728558 79421 None 0 Human Functional pEC50 = 6.2 6.2 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 377 5 3 9 0.9 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CSC)[C@@H](O)[C@H]3O)c2n1 10.1021/jm010952v
CHEMBL2113595 79421 None 0 Human Functional pEC50 = 6.2 6.2 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 377 5 3 9 0.9 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CSC)[C@@H](O)[C@H]3O)c2n1 10.1021/jm010952v
10005682 79382 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 487 7 5 11 1.6 Nc1nc(N/N=C/C=C(c2ccccc2)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm00018a017
CHEMBL2113552 79382 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 487 7 5 11 1.6 Nc1nc(N/N=C/C=C(c2ccccc2)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm00018a017
57384544 75514 None 0 Human Functional pEC50 = 6.2 6.2 1 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 854 14 7 12 7.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042309 75514 None 0 Human Functional pEC50 = 6.2 6.2 1 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 854 14 7 12 7.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
168278159 190469 None 0 Human Functional pEC50 = 7.1 7.1 -23 4
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 839 15 5 15 6.6 Nc1sc(-c2ccc(-c3cn(CCCCCCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)nn3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5177040 190469 None 0 Human Functional pEC50 = 7.1 7.1 -23 4
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 839 15 5 15 6.6 Nc1sc(-c2ccc(-c3cn(CCCCCCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)nn3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
1676 99038 None 41 Human Functional pEC50 = 5.1 5.1 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1021/jm00100a008
CHEMBL279898 99038 None 41 Human Functional pEC50 = 5.1 5.1 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1021/jm00100a008
11153 2008 None 42 Human Functional pEC50 = 6.1 6.1 - 1
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISAAntagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
ChEMBL 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 10.1021/acs.jmedchem.2c00101
86676119 2008 None 42 Human Functional pEC50 = 6.1 6.1 - 1
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISAAntagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
ChEMBL 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 10.1021/acs.jmedchem.2c00101
CHEMBL4594442 2008 None 42 Human Functional pEC50 = 6.1 6.1 - 1
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISAAntagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
ChEMBL 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 10.1021/acs.jmedchem.2c00101
DB16192 2008 None 42 Human Functional pEC50 = 6.1 6.1 - 1
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISAAntagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
ChEMBL 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 10.1021/acs.jmedchem.2c00101
10456627 79383 None 0 Rat Functional pEC50 = 6.1 6.1 1 2
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 454 7 5 12 0.2 CN(C)c1ccc(/C=C/C=N/Nc2nc(N)c3ncn([C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)cc1 10.1021/jm00018a017
CHEMBL2113553 79383 None 0 Rat Functional pEC50 = 6.1 6.1 1 2
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 454 7 5 12 0.2 CN(C)c1ccc(/C=C/C=N/Nc2nc(N)c3ncn([C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)cc1 10.1021/jm00018a017
2844 283 None 61 Human Functional pEC50 = 6.1 6.1 -7 5
Agonist activity at human adenosine A2A receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2A receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
60961 283 None 61 Human Functional pEC50 = 6.1 6.1 -7 5
Agonist activity at human adenosine A2A receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2A receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
60961.0 283 None 61 Human Functional pEC50 = 6.1 6.1 -7 5
Agonist activity at human adenosine A2A receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2A receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
90 283 None 61 Human Functional pEC50 = 6.1 6.1 -7 5
Agonist activity at human adenosine A2A receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2A receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
CHEMBL477 283 None 61 Human Functional pEC50 = 6.1 6.1 -7 5
Agonist activity at human adenosine A2A receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2A receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
DB00640 283 None 61 Human Functional pEC50 = 6.1 6.1 -7 5
Agonist activity at human adenosine A2A receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2A receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
118734377 118703 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 570 9 4 14 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCC(=O)OCC)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416811 118703 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 570 9 4 14 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCC(=O)OCC)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
168290627 192112 None 0 Human Functional pEC50 = 6.1 6.1 -5 4
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 859 11 6 13 6.6 Nc1sc(-c2ccc(C(=O)NCCC#Cc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5201533 192112 None 0 Human Functional pEC50 = 6.1 6.1 -5 4
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 859 11 6 13 6.6 Nc1sc(-c2ccc(C(=O)NCCC#Cc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
46876053 204985 None 0 Rat Functional pEC50 = 6.1 6.1 53 2
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 399 5 5 11 -0.2 Cc1ccc(/C=N/Nc2nc(N)c3ncn(C4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)cc1 10.1021/jm00018a017
CHEMBL611571 204985 None 0 Rat Functional pEC50 = 6.1 6.1 53 2
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 399 5 5 11 -0.2 Cc1ccc(/C=N/Nc2nc(N)c3ncn(C4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)cc1 10.1021/jm00018a017
10431643 79406 None 0 Human Functional pEC50 = 5.1 5.1 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 409 8 4 11 1.2 CCSC[C@H]1O[C@@H](n2cnc3c(N)nc(N/N=C/CC(C)C)nc32)[C@H](O)[C@@H]1O 10.1021/jm010952v
CHEMBL2113580 79406 None 0 Human Functional pEC50 = 5.1 5.1 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 409 8 4 11 1.2 CCSC[C@H]1O[C@@H](n2cnc3c(N)nc(N/N=C/CC(C)C)nc32)[C@H](O)[C@@H]1O 10.1021/jm010952v
46874604 204157 None 0 Rat Functional pEC50 = 6.1 6.1 4 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 412 4 4 11 -1.6 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#CCn4ccnc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
CHEMBL606319 204157 None 0 Rat Functional pEC50 = 6.1 6.1 4 2
Functional activity against adenosine A2a receptor from rat aorta.Functional activity against adenosine A2a receptor from rat aorta.
ChEMBL 412 4 4 11 -1.6 CCNC(=O)[C@H]1OC(n2cnc3c(N)nc(C#CCn4ccnc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm00009a007
137634052 156736 None 0 Human Functional pEC50 = 6.1 6.1 -7 3
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 830 15 7 14 5.7 Nc1nc(NCCCCCCNC(=O)c2ccc(-c3sc(N)c(C(=O)c4ccccc4)c3-c3cccc(C(F)(F)F)c3)cc2)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/acs.jmedchem.8b00047
CHEMBL4069296 156736 None 0 Human Functional pEC50 = 6.1 6.1 -7 3
Agonist activity at human A2A-AR 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 A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 830 15 7 14 5.7 Nc1nc(NCCCCCCNC(=O)c2ccc(-c3sc(N)c(C(=O)c4ccccc4)c3-c3cccc(C(F)(F)F)c3)cc2)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/acs.jmedchem.8b00047
80220 16887 None 65 Human Functional pEC50 = 4.1 4.1 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 166 0 2 4 -1.1 Cn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm00100a008
CHEMBL1250 16887 None 65 Human Functional pEC50 = 4.1 4.1 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 166 0 2 4 -1.1 Cn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm00100a008
12905389 20215 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 222 3 1 5 0.2 CCCCn1c(=O)c2nc[nH]c2n(C)c1=O 10.1021/jm00100a008
CHEMBL130503 20215 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 222 3 1 5 0.2 CCCCn1c(=O)c2nc[nH]c2n(C)c1=O 10.1021/jm00100a008
10037104 21947 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 236 3 0 6 0.3 CCCn1c(=O)n(CC)c(=O)c2c1ncn2C 10.1021/jm00100a008
CHEMBL132052 21947 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 236 3 0 6 0.3 CCCn1c(=O)n(CC)c(=O)c2c1ncn2C 10.1021/jm00100a008
10020580 108029 None 3 Rat Functional pEC50 = 7.1 7.1 -7 4
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 347 4 4 9 -0.4 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm960376g
CHEMBL319387 108029 None 3 Rat Functional pEC50 = 7.1 7.1 -7 4
Vasorelaxation as Adenosine A2A receptor activity in rat aortaVasorelaxation as Adenosine A2A receptor activity in rat aorta
ChEMBL 347 4 4 9 -0.4 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm960376g
123683 3121 None 46 Human Functional pEC50 = 7.1 7.1 -169 5
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
422 3121 None 46 Human Functional pEC50 = 7.1 7.1 -169 5
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
CHEMBL119709 3121 None 46 Human Functional pEC50 = 7.1 7.1 -169 5
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
DB05511 3121 None 46 Human Functional pEC50 = 7.1 7.1 -169 5
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
76329263 106103 None 0 Human Functional pEC50 = 7.1 7.1 -19 4
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 413 6 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133079 106103 None 0 Human Functional pEC50 = 7.1 7.1 -19 4
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 413 6 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
76322076 106104 None 0 Human Functional pEC50 = 6.1 6.1 -158 4
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 489 7 5 10 1.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133080 106104 None 0 Human Functional pEC50 = 6.1 6.1 -158 4
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 489 7 5 10 1.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
76325694 106117 None 0 Human Functional pEC50 = 6.1 6.1 -12 4
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 391 4 5 10 -0.5 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133159 106117 None 0 Human Functional pEC50 = 6.1 6.1 -12 4
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 391 4 5 10 -0.5 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
11352497 123033 None 0 Human Functional pEC50 = 8.1 8.1 -2 3
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 498 8 6 15 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(O)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL360837 123033 None 0 Human Functional pEC50 = 8.1 8.1 -2 3
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 498 8 6 15 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(O)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
118732980 118585 None 0 Human Functional pEC50 = 8.1 8.1 1 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 461 5 3 12 1.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414946 118585 None 0 Human Functional pEC50 = 8.1 8.1 1 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 461 5 3 12 1.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
155533388 171919 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 374 5 6 11 -1.2 Nc1nc(N/N=C/c2ccc[nH]2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.ejmech.2019.06.050
CHEMBL4468448 171919 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysisAgonist activity at human adenosine receptor A2A expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by Eu-cAMP tracer-based Envision plate reader analysis
ChEMBL 374 5 6 11 -1.2 Nc1nc(N/N=C/c2ccc[nH]2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1016/j.ejmech.2019.06.050
9869857 66851 None 12 Human Functional pEC50 = 8.1 8.1 1 5
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL186113 66851 None 12 Human Functional pEC50 = 8.1 8.1 1 5
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
56945639 70427 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as induction of cAMP production after 30 mins by immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as induction of cAMP production after 30 mins by immunoassay
ChEMBL 317 3 3 8 0.2 CCCCC#Cc1nc(N)c2ncn([C@@H]3OC[C@@H](O)[C@H]3O)c2n1 10.1021/jm201229j
CHEMBL1945563 70427 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as induction of cAMP production after 30 mins by immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as induction of cAMP production after 30 mins by immunoassay
ChEMBL 317 3 3 8 0.2 CCCCC#Cc1nc(N)c2ncn([C@@H]3OC[C@@H](O)[C@H]3O)c2n1 10.1021/jm201229j
10046591 79385 None 0 Rat Functional pEC50 = 6.1 6.1 5 2
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 401 6 5 12 -0.3 Nc1nc(N/N=C/C=C/c2ccco2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm00018a017
CHEMBL2113555 79385 None 0 Rat Functional pEC50 = 6.1 6.1 5 2
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aortaFunctional activity at Adenosine A2A receptor as vasorelaxation of rat aorta
ChEMBL 401 6 5 12 -0.3 Nc1nc(N/N=C/C=C/c2ccco2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm00018a017
10884004 79431 None 0 Human Functional pEC50 = 6.1 6.1 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 405 7 3 9 1.7 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CSCCC)[C@@H](O)[C@H]3O)c2n1 10.1021/jm010952v
CHEMBL2113604 79431 None 0 Human Functional pEC50 = 6.1 6.1 - 1
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assayG-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
ChEMBL 405 7 3 9 1.7 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CSCCC)[C@@H](O)[C@H]3O)c2n1 10.1021/jm010952v
372 58 None 56 Guinea pig Functional pEC50 = 5.1 5.1 -213 5
Antagonism of cyclic [3H]AMP accumulation elicited by 15 uM 2-chloroadenosine in [3H]adenine-labeled guinea pig cerebral cortical slices at A2 receptorAntagonism of cyclic [3H]AMP accumulation elicited by 15 uM 2-chloroadenosine in [3H]adenine-labeled guinea pig cerebral cortical slices at A2 receptor
ChEMBL 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10.1021/jm00382a018
8974 58 None 56 Guinea pig Functional pEC50 = 5.1 5.1 -213 5
Antagonism of cyclic [3H]AMP accumulation elicited by 15 uM 2-chloroadenosine in [3H]adenine-labeled guinea pig cerebral cortical slices at A2 receptorAntagonism of cyclic [3H]AMP accumulation elicited by 15 uM 2-chloroadenosine in [3H]adenine-labeled guinea pig cerebral cortical slices at A2 receptor
ChEMBL 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10.1021/jm00382a018
CHEMBL285819 58 None 56 Guinea pig Functional pEC50 = 5.1 5.1 -213 5
Antagonism of cyclic [3H]AMP accumulation elicited by 15 uM 2-chloroadenosine in [3H]adenine-labeled guinea pig cerebral cortical slices at A2 receptorAntagonism of cyclic [3H]AMP accumulation elicited by 15 uM 2-chloroadenosine in [3H]adenine-labeled guinea pig cerebral cortical slices at A2 receptor
ChEMBL 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10.1021/jm00382a018
CHEMBL5091876 217822 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Partial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based AssayPartial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based Assay
ChEMBL None None None Nc1nc(SCc2ncc[nH]2)nc(-c2ccccc2)n1 10.1021/acs.jmedchem.0c01856
218667 115330 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 208 3 2 4 0.2 CCCCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1021/jm00100a008
CHEMBL334849 115330 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 208 3 2 4 0.2 CCCCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1021/jm00100a008
10376254 116714 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 222 3 1 5 0.3 CCCn1c(=O)[nH]c(=O)c2c1ncn2CC 10.1021/jm00100a008
CHEMBL337001 116714 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 222 3 1 5 0.3 CCCn1c(=O)[nH]c(=O)c2c1ncn2CC 10.1021/jm00100a008
118734352 118680 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 585 12 5 14 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(OCCOC)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416787 118680 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 585 12 5 14 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(OCCOC)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
118734342 118670 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 525 9 5 12 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(Cc5ccccc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416777 118670 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 525 9 5 12 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(Cc5ccccc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
57385043 75515 None 0 Human Functional pEC50 = 7.1 7.1 1 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 810 18 6 13 6.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)CCCC[C@H]5CCSS5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042310 75515 None 0 Human Functional pEC50 = 7.1 7.1 1 4
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 810 18 6 13 6.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)CCCC[C@H]5CCSS5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
9869857 66851 None 12 Human Functional pEC50 = 8.1 8.1 1 5
Agonist activity at adenosine receptor A2a (unknown origin) assessed as cAMP formationAgonist activity at adenosine receptor A2a (unknown origin) assessed as cAMP formation
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm4011669
CHEMBL186113 66851 None 12 Human Functional pEC50 = 8.1 8.1 1 5
Agonist activity at adenosine receptor A2a (unknown origin) assessed as cAMP formationAgonist activity at adenosine receptor A2a (unknown origin) assessed as cAMP formation
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm4011669
118732982 118587 None 0 Human Functional pEC50 = 8.0 8.0 1 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 583 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccccc5I)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414948 118587 None 0 Human Functional pEC50 = 8.0 8.0 1 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 583 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccccc5I)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
127038754 136778 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 484 7 4 13 0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(NC(C)Cc5ccc(F)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
CHEMBL3740436 136778 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay
ChEMBL 484 7 4 13 0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(NC(C)Cc5ccc(F)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
118732974 118579 None 0 Human Functional pEC50 = 8.0 8.0 -1 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414940 118579 None 0 Human Functional pEC50 = 8.0 8.0 -1 4
Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
11174953 16769 None 1 Human Functional pEC50 = 8.0 8.0 1 2
Partial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based AssayPartial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based Assay
ChEMBL 332 4 2 6 3.1 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccccc1 10.1021/acs.jmedchem.0c01856
CHEMBL124345 16769 None 1 Human Functional pEC50 = 8.0 8.0 1 2
Partial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based AssayPartial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based Assay
ChEMBL 332 4 2 6 3.1 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccccc1 10.1021/acs.jmedchem.0c01856
118734340 118668 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 511 8 5 12 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccccc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416775 118668 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 511 8 5 12 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccccc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
168283013 190984 None 0 Human Functional pEC50 = 5.0 5.0 -1778 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 516 8 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5184828 190984 None 0 Human Functional pEC50 = 5.0 5.0 -1778 4
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 516 8 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
118734356 118684 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 555 9 6 13 -0.9 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5cccc(C(=O)O)c5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416791 118684 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 555 9 6 13 -0.9 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5cccc(C(=O)O)c5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
137661670 159430 None 0 Human Functional pEC50 = 7.0 7.0 1 3
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 509 6 3 12 1.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4100130 159430 None 0 Human Functional pEC50 = 7.0 7.0 1 3
Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 509 6 3 12 1.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
174907 9564 None 2 Human Functional pEC50 = 5.0 5.0 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 208 2 1 5 -0.2 CCCn1c(=O)c2nc[nH]c2n(C)c1=O 10.1021/jm00100a008
CHEMBL112369 9564 None 2 Human Functional pEC50 = 5.0 5.0 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 208 2 1 5 -0.2 CCCn1c(=O)c2nc[nH]c2n(C)c1=O 10.1021/jm00100a008
15931307 18421 None 3 Human Functional pEC50 = 4.0 4.0 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 180 1 2 4 -0.6 CCn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm00100a008
CHEMBL127167 18421 None 3 Human Functional pEC50 = 4.0 4.0 - 1
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
ChEMBL 180 1 2 4 -0.6 CCn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm00100a008
10256007 122995 None 0 Human Functional pEC50 = 7.0 7.0 47 2
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 516 8 5 14 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Cl)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL360646 122995 None 0 Human Functional pEC50 = 7.0 7.0 47 2
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptorPotency against cAMP formation in CHO cells expressing recombinant human A2A receptor
ChEMBL 516 8 5 14 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Cl)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
145436767 162573 None 0 Human Functional pIC50 = 11.0 11.0 4365 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2cccnc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4167125 162573 None 0 Human Functional pIC50 = 11.0 11.0 4365 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2cccnc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
145436760 162236 None 0 Human Functional pIC50 = 10.4 10.4 2089 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 329 4 2 8 3.6 Nc1nc(NCc2cccs2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4161758 162236 None 0 Human Functional pIC50 = 10.4 10.4 2089 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 329 4 2 8 3.6 Nc1nc(NCc2cccs2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
168274325 190811 None 0 Human Functional pIC50 = 10.4 10.4 - 1
Inverse agonist activity at human A2A receptor assessed as inhibition of selective agonist-induced cAMP productionInverse agonist activity at human A2A receptor assessed as inhibition of selective agonist-induced cAMP production
ChEMBL 324 4 2 8 3.0 Nc1nc(Nc2ccco2)nc2sc(Cc3cccnc3)nc12 10.1016/j.ejmech.2021.113907
CHEMBL5182250 190811 None 0 Human Functional pIC50 = 10.4 10.4 - 1
Inverse agonist activity at human A2A receptor assessed as inhibition of selective agonist-induced cAMP productionInverse agonist activity at human A2A receptor assessed as inhibition of selective agonist-induced cAMP production
ChEMBL 324 4 2 8 3.0 Nc1nc(Nc2ccco2)nc2sc(Cc3cccnc3)nc12 10.1016/j.ejmech.2021.113907
145436769 162899 None 0 Human Functional pIC50 = 10.4 10.4 2041 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 313 4 2 8 3.1 Nc1nc(NCc2ccco2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4172399 162899 None 0 Human Functional pIC50 = 10.4 10.4 2041 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 313 4 2 8 3.1 Nc1nc(NCc2ccco2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
145436765 162890 None 0 Human Functional pIC50 = 10.4 10.4 2511 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 343 5 2 8 3.6 Nc1nc(NCCc2cccs2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4172264 162890 None 0 Human Functional pIC50 = 10.4 10.4 2511 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 343 5 2 8 3.6 Nc1nc(NCCc2cccs2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
132991405 151152 None 3 Human Functional pIC50 = 10.3 10.3 6165 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1ccccc1CNc1nc(N)c2nc(-c3ccco3)sc2n1 10.1021/acs.jmedchem.6b01068
CHEMBL3958838 151152 None 3 Human Functional pIC50 = 10.3 10.3 6165 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1ccccc1CNc1nc(N)c2nc(-c3ccco3)sc2n1 10.1021/acs.jmedchem.6b01068
145436767 162573 None 0 Human Functional pIC50 = 10.2 10.2 4365 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2cccnc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4167125 162573 None 0 Human Functional pIC50 = 10.2 10.2 4365 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2cccnc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
132991406 144301 None 0 Human Functional pIC50 = 10.0 10.0 4786 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1cccc(CNc2nc(N)c3nc(-c4ccco4)sc3n2)c1 10.1021/acs.jmedchem.6b01068
CHEMBL3904408 144301 None 0 Human Functional pIC50 = 10.0 10.0 4786 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1cccc(CNc2nc(N)c3nc(-c4ccco4)sc3n2)c1 10.1021/acs.jmedchem.6b01068
156821369 185729 None 2 Human Functional pIC50 = 9.5 9.5 14 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 447 4 2 7 3.5 Nc1nc(-c2ccccc2)c(-c2ccc(=O)[nH]c2)c2nc(Cc3ncc(F)cc3Cl)nn12 10.1021/acsmedchemlett.1c00620
CHEMBL4864129 185729 None 2 Human Functional pIC50 = 9.5 9.5 14 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 447 4 2 7 3.5 Nc1nc(-c2ccccc2)c(-c2ccc(=O)[nH]c2)c2nc(Cc3ncc(F)cc3Cl)nn12 10.1021/acsmedchemlett.1c00620
145436763 162291 None 0 Human Functional pIC50 = 9.5 9.5 13 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 338 5 2 8 3.0 Nc1nc(NCCc2cccnc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4162638 162291 None 0 Human Functional pIC50 = 9.5 9.5 13 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 338 5 2 8 3.0 Nc1nc(NCCc2cccnc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
156821390 185342 None 0 Human Functional pIC50 = 9.5 9.5 30 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 431 4 2 7 3.0 Nc1nc(-c2ccc(F)cc2)c(-c2ccc(=O)[nH]c2)c2nc(Cc3ccc(F)cn3)nn12 10.1021/acsmedchemlett.1c00620
CHEMBL4858144 185342 None 0 Human Functional pIC50 = 9.5 9.5 30 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 431 4 2 7 3.0 Nc1nc(-c2ccc(F)cc2)c(-c2ccc(=O)[nH]c2)c2nc(Cc3ccc(F)cn3)nn12 10.1021/acsmedchemlett.1c00620
145436763 162291 None 0 Human Functional pIC50 = 9.5 9.5 13 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 338 5 2 8 3.0 Nc1nc(NCCc2cccnc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4162638 162291 None 0 Human Functional pIC50 = 9.5 9.5 13 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 338 5 2 8 3.0 Nc1nc(NCCc2cccnc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
145436764 162081 None 0 Human Functional pIC50 = 9.4 9.4 22 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 329 4 2 8 3.6 Nc1nc(NCc2ccsc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4159215 162081 None 0 Human Functional pIC50 = 9.4 9.4 22 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 329 4 2 8 3.6 Nc1nc(NCc2ccsc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
10305890 8684 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 751 15 8 12 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCc4ccc(C(=O)O)cc4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
CHEMBL1095604 8684 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 751 15 8 12 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCc4ccc(C(=O)O)cc4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
9869857 66851 None 12 Human Functional pIC50 = 9.4 9.4 1 5
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1016/j.bmcl.2009.11.131
CHEMBL186113 66851 None 12 Human Functional pIC50 = 9.4 9.4 1 5
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1016/j.bmcl.2009.11.131
145436764 162081 None 0 Human Functional pIC50 = 9.4 9.4 22 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 329 4 2 8 3.6 Nc1nc(NCc2ccsc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4159215 162081 None 0 Human Functional pIC50 = 9.4 9.4 22 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 329 4 2 8 3.6 Nc1nc(NCc2ccsc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
162645933 179652 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by 3 nM A2A agonist NECA addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by 3 nM A2A agonist NECA addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assay
ChEMBL 555 7 2 12 1.5 NC(=O)Cc1cc(N2CCN(CCn3c(=O)sc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)cc1F 10.1021/acs.jmedchem.0c00237
CHEMBL4741609 179652 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by 3 nM A2A agonist NECA addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by 3 nM A2A agonist NECA addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assay
ChEMBL 555 7 2 12 1.5 NC(=O)Cc1cc(N2CCN(CCn3c(=O)sc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)cc1F 10.1021/acs.jmedchem.0c00237
156821421 186325 None 0 Human Functional pIC50 = 9.3 9.3 16 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 443 4 2 9 2.4 Cn1cc(-c2c(-c3ccccc3)nc(N)n3nc([C@H](O)c4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
CHEMBL4873266 186325 None 0 Human Functional pIC50 = 9.3 9.3 16 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 443 4 2 9 2.4 Cn1cc(-c2c(-c3ccccc3)nc(N)n3nc([C@H](O)c4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
156821433 186100 None 0 Human Functional pIC50 = 9.2 9.2 12 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 427 4 1 8 2.9 Cn1cc(-c2c(-c3ccccc3)nc(N)n3nc(Cc4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
CHEMBL4870159 186100 None 0 Human Functional pIC50 = 9.2 9.2 12 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 427 4 1 8 2.9 Cn1cc(-c2c(-c3ccccc3)nc(N)n3nc(Cc4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
135346979 181265 None 9 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by 3 nM A2A agonist NECA addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by 3 nM A2A agonist NECA addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assay
ChEMBL 604 9 1 13 2.2 C[S+]([O-])CCOc1cc(N2CCN(CCn3c(=O)sc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)cc1F 10.1021/acs.jmedchem.0c00237
CHEMBL4760867 181265 None 9 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by 3 nM A2A agonist NECA addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by 3 nM A2A agonist NECA addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assay
ChEMBL 604 9 1 13 2.2 C[S+]([O-])CCOc1cc(N2CCN(CCn3c(=O)sc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)cc1F 10.1021/acs.jmedchem.0c00237
176407 4148 None 56 Human Functional pIC50 = 9.2 9.2 13 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.6b01068
405 4148 None 56 Human Functional pIC50 = 9.2 9.2 13 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.6b01068
CHEMBL113142 4148 None 56 Human Functional pIC50 = 9.2 9.2 13 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.6b01068
DB08770 4148 None 56 Human Functional pIC50 = 9.2 9.2 13 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.6b01068
145436766 162622 None 0 Human Functional pIC50 = 9.2 9.2 102 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2ccccn2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4167813 162622 None 0 Human Functional pIC50 = 9.2 9.2 102 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2ccccn2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
164611330 185190 None 0 Human Functional pIC50 = 9.1 9.1 380 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 418 4 2 6 3.4 Nc1nc(-c2ccc(F)cc2)c(-c2ccc(=O)[nH]c2)c2nc(CCC(F)(F)F)nn12 10.1021/acsmedchemlett.1c00620
CHEMBL4855908 185190 None 0 Human Functional pIC50 = 9.1 9.1 380 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 418 4 2 6 3.4 Nc1nc(-c2ccc(F)cc2)c(-c2ccc(=O)[nH]c2)c2nc(CCC(F)(F)F)nn12 10.1021/acsmedchemlett.1c00620
67364057 74315 None 0 Human Functional pIC50 = 9.1 9.1 2 2
Antagonist activity at human adenosine 2A receptor expressed in CHO-K1 cells assessed as reduction in cAMP level in presence of 0.1 uM adenosine by fluorescent AssayAntagonist activity at human adenosine 2A receptor expressed in CHO-K1 cells assessed as reduction in cAMP level in presence of 0.1 uM adenosine by fluorescent Assay
ChEMBL 295 2 1 5 2.9 Cc1cc(-c2nnc(N)nc2-c2ccc(F)cc2)cc(C)n1 10.1021/acs.jmedchem.0c00237
CHEMBL2024116 74315 None 0 Human Functional pIC50 = 9.1 9.1 2 2
Antagonist activity at human adenosine 2A receptor expressed in CHO-K1 cells assessed as reduction in cAMP level in presence of 0.1 uM adenosine by fluorescent AssayAntagonist activity at human adenosine 2A receptor expressed in CHO-K1 cells assessed as reduction in cAMP level in presence of 0.1 uM adenosine by fluorescent Assay
ChEMBL 295 2 1 5 2.9 Cc1cc(-c2nnc(N)nc2-c2ccc(F)cc2)cc(C)n1 10.1021/acs.jmedchem.0c00237
176407 4148 None 56 Human Functional pIC50 = 9.1 9.1 13 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2018.06.020
405 4148 None 56 Human Functional pIC50 = 9.1 9.1 13 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2018.06.020
CHEMBL113142 4148 None 56 Human Functional pIC50 = 9.1 9.1 13 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2018.06.020
DB08770 4148 None 56 Human Functional pIC50 = 9.1 9.1 13 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2018.06.020
176407 4148 None 56 Human Functional pIC50 = 8.9 8.9 13 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2018.06.020
405 4148 None 56 Human Functional pIC50 = 8.9 8.9 13 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2018.06.020
CHEMBL113142 4148 None 56 Human Functional pIC50 = 8.9 8.9 13 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2018.06.020
DB08770 4148 None 56 Human Functional pIC50 = 8.9 8.9 13 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2018.06.020
145436766 162622 None 0 Human Functional pIC50 = 8.9 8.9 102 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2ccccn2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4167813 162622 None 0 Human Functional pIC50 = 8.9 8.9 102 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2ccccn2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
176407 4148 None 56 Human Functional pIC50 = 8.8 8.8 13 2
Inverse agonist activity at human A2A receptor assessed as inhibition of cAMP accumulationInverse agonist activity at human A2A receptor assessed as inhibition of cAMP accumulation
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2021.113907
405 4148 None 56 Human Functional pIC50 = 8.8 8.8 13 2
Inverse agonist activity at human A2A receptor assessed as inhibition of cAMP accumulationInverse agonist activity at human A2A receptor assessed as inhibition of cAMP accumulation
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2021.113907
CHEMBL113142 4148 None 56 Human Functional pIC50 = 8.8 8.8 13 2
Inverse agonist activity at human A2A receptor assessed as inhibition of cAMP accumulationInverse agonist activity at human A2A receptor assessed as inhibition of cAMP accumulation
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2021.113907
DB08770 4148 None 56 Human Functional pIC50 = 8.8 8.8 13 2
Inverse agonist activity at human A2A receptor assessed as inhibition of cAMP accumulationInverse agonist activity at human A2A receptor assessed as inhibition of cAMP accumulation
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2021.113907
176407 4148 None 56 Human Functional pIC50 = 8.8 8.8 13 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.6b01068
405 4148 None 56 Human Functional pIC50 = 8.8 8.8 13 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.6b01068
CHEMBL113142 4148 None 56 Human Functional pIC50 = 8.8 8.8 13 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.6b01068
DB08770 4148 None 56 Human Functional pIC50 = 8.8 8.8 13 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.6b01068
176407 4148 None 56 Human Functional pIC50 = 8.8 8.8 13 2
Antagonist activity at human adenosine A2A receptor expressed in HEK293T cells assessed as inhibition of NECA-induced Gs short protein activation by TRUPATH assayAntagonist activity at human adenosine A2A receptor expressed in HEK293T cells assessed as inhibition of NECA-induced Gs short protein activation by TRUPATH assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acsmedchemlett.2c00099
405 4148 None 56 Human Functional pIC50 = 8.8 8.8 13 2
Antagonist activity at human adenosine A2A receptor expressed in HEK293T cells assessed as inhibition of NECA-induced Gs short protein activation by TRUPATH assayAntagonist activity at human adenosine A2A receptor expressed in HEK293T cells assessed as inhibition of NECA-induced Gs short protein activation by TRUPATH assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acsmedchemlett.2c00099
CHEMBL113142 4148 None 56 Human Functional pIC50 = 8.8 8.8 13 2
Antagonist activity at human adenosine A2A receptor expressed in HEK293T cells assessed as inhibition of NECA-induced Gs short protein activation by TRUPATH assayAntagonist activity at human adenosine A2A receptor expressed in HEK293T cells assessed as inhibition of NECA-induced Gs short protein activation by TRUPATH assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acsmedchemlett.2c00099
DB08770 4148 None 56 Human Functional pIC50 = 8.8 8.8 13 2
Antagonist activity at human adenosine A2A receptor expressed in HEK293T cells assessed as inhibition of NECA-induced Gs short protein activation by TRUPATH assayAntagonist activity at human adenosine A2A receptor expressed in HEK293T cells assessed as inhibition of NECA-induced Gs short protein activation by TRUPATH assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acsmedchemlett.2c00099
46886593 8835 None 0 Human Functional pIC50 = 8 8.0 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 776 15 7 12 1.9 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCCN4CCc5ccccc5C4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
CHEMBL1096890 8835 None 0 Human Functional pIC50 = 8 8.0 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 776 15 7 12 1.9 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCCN4CCc5ccccc5C4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
46886595 8837 None 0 Human Functional pIC50 = 8 8.0 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 721 15 7 11 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
CHEMBL1096892 8837 None 0 Human Functional pIC50 = 8 8.0 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 721 15 7 11 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
10362099 206068 None 17 Human Functional pIC50 = 8 8.0 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 375 5 2 9 2.7 Nc1nc2c(cnn2CCCc2ccc(O)cc2)c2nc(-c3ccco3)nn12 10.1021/jm9708689
CHEMBL67026 206068 None 17 Human Functional pIC50 = 8 8.0 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 375 5 2 9 2.7 Nc1nc2c(cnn2CCCc2ccc(O)cc2)c2nc(-c3ccco3)nn12 10.1021/jm9708689
171485733 197030 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 454 5 1 7 4.4 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(C(C)(C)F)n3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5437168 197030 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 454 5 1 7 4.4 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(C(C)(C)F)n3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
163215620 190452 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assayAntagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assay
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5176737 190452 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assayAntagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assay
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5203105 190452 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assayAntagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assay
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
127046495 139882 None 0 Human Functional pIC50 = 8.0 8.0 13 2
Antagonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 305 3 1 6 3.0 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4)cc3n2)o1 10.1016/j.bmc.2016.04.048
CHEMBL3798754 139882 None 0 Human Functional pIC50 = 8.0 8.0 13 2
Antagonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 305 3 1 6 3.0 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4)cc3n2)o1 10.1016/j.bmc.2016.04.048
9851062 155121 None 0 Human Functional pIC50 = 7 7.0 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 572 11 4 10 3.8 COC[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(CNC4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
CHEMBL401571 155121 None 0 Human Functional pIC50 = 7 7.0 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 572 11 4 10 3.8 COC[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(CNC4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
25110821 97618 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells by cAMP assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells by cAMP assay
ChEMBL 462 6 1 8 2.9 Cc1cc(C)n(-c2cc(NC(=O)Cc3ccc(S(C)(=O)=O)cc3)nc(-c3ccccn3)n2)n1 10.1016/j.bmcl.2008.01.036
CHEMBL270654 97618 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells by cAMP assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells by cAMP assay
ChEMBL 462 6 1 8 2.9 Cc1cc(C)n(-c2cc(NC(=O)Cc3ccc(S(C)(=O)=O)cc3)nc(-c3ccccn3)n2)n1 10.1016/j.bmcl.2008.01.036
44454230 155589 None 0 Human Functional pIC50 = 6 6.0 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 613 12 5 10 4.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCC4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
CHEMBL404123 155589 None 0 Human Functional pIC50 = 6 6.0 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 613 12 5 10 4.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCC4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
24989636 189872 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human adenosine A2A receptor assessed as inhibition of CGS-21680-stimulated cAMP productionAntagonist activity at human adenosine A2A receptor assessed as inhibition of CGS-21680-stimulated cAMP production
ChEMBL 314 3 1 6 1.4 CC(=O)Nc1cc(N2CCCC2=O)nc(-n2nc(C)cc2C)n1 10.1021/jm800908d
CHEMBL515992 189872 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human adenosine A2A receptor assessed as inhibition of CGS-21680-stimulated cAMP productionAntagonist activity at human adenosine A2A receptor assessed as inhibition of CGS-21680-stimulated cAMP production
ChEMBL 314 3 1 6 1.4 CC(=O)Nc1cc(N2CCCC2=O)nc(-n2nc(C)cc2C)n1 10.1021/jm800908d
46230245 203398 None 0 Human Functional pIC50 = 7 7.0 - 1
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 648 12 4 14 3.7 Cc1nnnn1[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4cn(C(C)C)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL601732 203398 None 0 Human Functional pIC50 = 7 7.0 - 1
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 648 12 4 14 3.7 Cc1nnnn1[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4cn(C(C)C)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
44454231 155688 None 0 Human Functional pIC50 = 6 6.0 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 586 12 4 10 4.7 COC[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCC4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
CHEMBL404521 155688 None 0 Human Functional pIC50 = 6 6.0 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 586 12 4 10 4.7 COC[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCC4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
CHEMBL5093127 217898 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CC2CC2)o1 10.1021/acs.jmedchem.1c02199
CHEMBL5089248 217689 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1ccccc1Cn1c(=O)cnc2c(-c3ccc(C)o3)nc(N)nc21 10.1021/acs.jmedchem.1c02199
145962529 161485 None 0 Human Functional pIC50 = 7.0 7.0 1 3
Antagonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 291 4 2 7 2.7 Cc1nc2c(N)nc(NCCc3cccs3)nc2s1 10.1016/j.bmc.2018.05.048
CHEMBL4126427 161485 None 0 Human Functional pIC50 = 7.0 7.0 1 3
Antagonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 291 4 2 7 2.7 Cc1nc2c(N)nc(NCCc3cccs3)nc2s1 10.1016/j.bmc.2018.05.048
24768400 153936 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2A receptor by cAMP assayAntagonist activity at human adenosine A2A receptor by cAMP assay
ChEMBL 384 5 1 8 2.0 CN1CCN(CC(=O)Nc2cc(-c3nccs3)nc(-c3ccco3)n2)CC1 10.1021/jm701185v
CHEMBL398272 153936 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2A receptor by cAMP assayAntagonist activity at human adenosine A2A receptor by cAMP assay
ChEMBL 384 5 1 8 2.0 CN1CCN(CC(=O)Nc2cc(-c3nccs3)nc(-c3ccco3)n2)CC1 10.1021/jm701185v
CHEMBL5074910 216828 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2[nH]c(=O)n3Cc2ccccc2)o1 10.1021/acs.jmedchem.1c02199
168276863 190297 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assayAntagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assay
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccncc2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5174275 190297 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assayAntagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assay
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccncc2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
118726003 120948 None 0 Human Functional pIC50 = 6.0 6.0 1 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 878 31 5 13 7.1 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394259 120948 None 0 Human Functional pIC50 = 6.0 6.0 1 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 878 31 5 13 7.1 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3559207 120948 None 0 Human Functional pIC50 = 6.0 6.0 1 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 878 31 5 13 7.1 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
118726003 120948 None 0 Human Functional pIC50 = 6.0 6.0 1 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 878 31 5 13 7.1 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394259 120948 None 0 Human Functional pIC50 = 6.0 6.0 1 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 878 31 5 13 7.1 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3559207 120948 None 0 Human Functional pIC50 = 6.0 6.0 1 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 878 31 5 13 7.1 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
46883041 5735 None 0 Human Functional pIC50 = 6.0 6.0 -2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 379 5 1 6 5.5 Cc1ccc(C(=O)c2nc(NC(C)c3ccccc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078347 5735 None 0 Human Functional pIC50 = 6.0 6.0 -2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 379 5 1 6 5.5 Cc1ccc(C(=O)c2nc(NC(C)c3ccccc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
118726000 117268 None 0 Human Functional pIC50 = 7.0 7.0 7 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 765 23 5 13 4.0 CCCN(CCCNC(=O)CCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394257 117268 None 0 Human Functional pIC50 = 7.0 7.0 7 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 765 23 5 13 4.0 CCCN(CCCNC(=O)CCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
171485730 196377 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 407 4 1 6 4.1 Cc1ccccc1Cn1ccc(-c2cc(-c3cccc(C#N)c3C)nc(N)n2)cc1=O 10.1021/acs.jmedchem.2c01860
CHEMBL5422530 196377 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 407 4 1 6 4.1 Cc1ccccc1Cn1ccc(-c2cc(-c3cccc(C#N)c3C)nc(N)n2)cc1=O 10.1021/acs.jmedchem.2c01860
71625116 90121 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 583 16 1 11 3.1 CCn1c(=O)c2c(nc(/C=C/c3ccc(OCCCC(=O)NCCCCCC(=O)OC)c(OC)c3)n2C)n(CC)c1=O 10.1016/j.bmcl.2013.03.070
CHEMBL2381768 90121 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 583 16 1 11 3.1 CCn1c(=O)c2c(nc(/C=C/c3ccc(OCCCC(=O)NCCCCCC(=O)OC)c(OC)c3)n2C)n(CC)c1=O 10.1016/j.bmcl.2013.03.070
10122714 95527 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 687 15 6 11 2.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(CNC(=O)NCCN(C(C)C)C(C)C)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
CHEMBL257213 95527 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 687 15 6 11 2.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(CNC(=O)NCCN(C(C)C)C(C)C)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
145436761 162932 None 0 Human Functional pIC50 = 8.0 8.0 1 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 325 4 2 9 2.3 Nc1nc(NCc2cnccn2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4172818 162932 None 0 Human Functional pIC50 = 8.0 8.0 1 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 325 4 2 9 2.3 Nc1nc(NCc2cnccn2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL5091888 217823 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCN2CCN(c3ccccc3F)CC2)o1 10.1021/acs.jmedchem.1c02199
118726000 117268 None 0 Human Functional pIC50 = 7.0 7.0 7 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 765 23 5 13 4.0 CCCN(CCCNC(=O)CCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394257 117268 None 0 Human Functional pIC50 = 7.0 7.0 7 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 765 23 5 13 4.0 CCCN(CCCNC(=O)CCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
118726009 117273 None 0 Human Functional pIC50 = 6.0 6.0 -2 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 447 9 3 10 1.8 CN(CCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394264 117273 None 0 Human Functional pIC50 = 6.0 6.0 -2 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 447 9 3 10 1.8 CN(CCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
118726009 117273 None 0 Human Functional pIC50 = 6.0 6.0 -2 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 447 9 3 10 1.8 CN(CCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394264 117273 None 0 Human Functional pIC50 = 6.0 6.0 -2 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 447 9 3 10 1.8 CN(CCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
172450291 196076 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 451 5 1 8 3.6 COC(=O)c1cccc(Cn2ccc(-c3cc(-c4cccc(C#N)c4C)nc(N)n3)cc2=O)c1 10.1021/acs.jmedchem.2c01860
CHEMBL5416491 196076 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 451 5 1 8 3.6 COC(=O)c1cccc(Cn2ccc(-c3cc(-c4cccc(C#N)c4C)nc(N)n3)cc2=O)c1 10.1021/acs.jmedchem.2c01860
172445196 195465 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 481 7 1 9 3.3 COC(=O)COc1cccc(Cn2ccc(-c3cc(-c4cccc(C#N)c4C)nc(N)n3)cc2=O)c1 10.1021/acs.jmedchem.2c01860
CHEMBL5404268 195465 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 481 7 1 9 3.3 COC(=O)COc1cccc(Cn2ccc(-c3cc(-c4cccc(C#N)c4C)nc(N)n3)cc2=O)c1 10.1021/acs.jmedchem.2c01860
155519986 170500 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 550 11 2 10 4.3 Nc1nc(-c2ccc(OCCNC(=O)CCCCC3CCSS3)cc2)cn2c(=O)n(-c3ccccc3)nc12 10.1021/acs.jmedchem.9b00778
CHEMBL4447993 170500 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 550 11 2 10 4.3 Nc1nc(-c2ccc(OCCNC(=O)CCCCC3CCSS3)cc2)cn2c(=O)n(-c3ccccc3)nc12 10.1021/acs.jmedchem.9b00778
46883070 5682 None 0 Human Functional pIC50 = 6.9 6.9 -1 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 5 1 8 3.7 Cc1ccc(C(=O)c2nc(NCc3ccncn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1077902 5682 None 0 Human Functional pIC50 = 6.9 6.9 -1 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 5 1 8 3.7 Cc1ccc(C(=O)c2nc(NCc3ccncn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
46883206 6319 None 0 Human Functional pIC50 = 5.9 5.9 -10 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 347 5 1 7 3.3 O=C(c1cccnc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1081873 6319 None 0 Human Functional pIC50 = 5.9 5.9 -10 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 347 5 1 7 3.3 O=C(c1cccnc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
46883106 5685 None 0 Human Functional pIC50 = 6.9 6.9 -6 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 1 7 4.9 Cc1ccc(C(=O)c2nc(NC(C)c3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1077915 5685 None 0 Human Functional pIC50 = 6.9 6.9 -6 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 1 7 4.9 Cc1ccc(C(=O)c2nc(NC(C)c3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
11574573 201970 None 0 Human Functional pIC50 = 7.9 7.9 8 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 386 5 4 8 0.5 CCCCC#Cc1nc(N)c2ncn([C@@H]3C[C@H](NC(=O)CC)[C@@H](O)[C@H]3O)c2n1 10.1016/j.bmcl.2009.11.131
CHEMBL591999 201970 None 0 Human Functional pIC50 = 7.9 7.9 8 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 386 5 4 8 0.5 CCCCC#Cc1nc(N)c2ncn([C@@H]3C[C@H](NC(=O)CC)[C@@H](O)[C@H]3O)c2n1 10.1016/j.bmcl.2009.11.131
2690 903 None 44 Human Functional pIC50 = 7.9 7.9 -3 5
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm9708689
384 903 None 44 Human Functional pIC50 = 7.9 7.9 -3 5
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm9708689
CHEMBL16687 903 None 44 Human Functional pIC50 = 7.9 7.9 -3 5
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm9708689
176408 3557 None 55 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/jm9708689
403 3557 None 55 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/jm9708689
431 3557 None 55 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/jm9708689
CHEMBL17127 3557 None 55 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/jm9708689
118726007 120747 None 0 Human Functional pIC50 = 6.9 6.9 2 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 774 18 4 17 4.1 CCCN(CCCNc1nc(Oc2ccc(CCNc3nc(N)n4nc(-c5ccco5)nc4n3)cc2)nc(N2CCOCC2)n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394262 120747 None 0 Human Functional pIC50 = 6.9 6.9 2 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 774 18 4 17 4.1 CCCN(CCCNc1nc(Oc2ccc(CCNc3nc(N)n4nc(-c5ccco5)nc4n3)cc2)nc(N2CCOCC2)n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3547017 120747 None 0 Human Functional pIC50 = 6.9 6.9 2 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 774 18 4 17 4.1 CCCN(CCCNc1nc(Oc2ccc(CCNc3nc(N)n4nc(-c5ccco5)nc4n3)cc2)nc(N2CCOCC2)n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL5075499 216865 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCN2CCN(c3ccc(OC(F)(F)F)cc3)CC2)o1 10.1021/acs.jmedchem.1c02199
118726007 120747 None 0 Human Functional pIC50 = 6.9 6.9 2 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 774 18 4 17 4.1 CCCN(CCCNc1nc(Oc2ccc(CCNc3nc(N)n4nc(-c5ccco5)nc4n3)cc2)nc(N2CCOCC2)n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394262 120747 None 0 Human Functional pIC50 = 6.9 6.9 2 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 774 18 4 17 4.1 CCCN(CCCNc1nc(Oc2ccc(CCNc3nc(N)n4nc(-c5ccco5)nc4n3)cc2)nc(N2CCOCC2)n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3547017 120747 None 0 Human Functional pIC50 = 6.9 6.9 2 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 774 18 4 17 4.1 CCCN(CCCNc1nc(Oc2ccc(CCNc3nc(N)n4nc(-c5ccco5)nc4n3)cc2)nc(N2CCOCC2)n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
135665340 90119 None 18 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 370 5 1 8 1.8 CCn1c(=O)c2c(nc(/C=C/c3ccc(O)c(OC)c3)n2C)n(CC)c1=O 10.1016/j.bmcl.2013.03.070
CHEMBL2381766 90119 None 18 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 370 5 1 8 1.8 CCn1c(=O)c2c(nc(/C=C/c3ccc(O)c(OC)c3)n2C)n(CC)c1=O 10.1016/j.bmcl.2013.03.070
134138961 147712 None 0 Human Functional pIC50 = 6.9 6.9 1 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1ccc(CNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1 10.1021/acs.jmedchem.6b01068
CHEMBL3931329 147712 None 0 Human Functional pIC50 = 6.9 6.9 1 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1ccc(CNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1 10.1021/acs.jmedchem.6b01068
46883109 5836 None 0 Human Functional pIC50 = 5.9 5.9 -2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 350 5 1 7 3.8 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)o1 10.1016/j.bmcl.2009.08.040
CHEMBL1079117 5836 None 0 Human Functional pIC50 = 5.9 5.9 -2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 350 5 1 7 3.8 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)o1 10.1016/j.bmcl.2009.08.040
46882998 5643 None 0 Human Functional pIC50 = 6.9 6.9 10 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 303 4 1 6 3.7 CCNc1nc(C(=O)c2ccc(C)s2)c2sccc2n1 10.1016/j.bmcl.2009.08.040
CHEMBL1077752 5643 None 0 Human Functional pIC50 = 6.9 6.9 10 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 303 4 1 6 3.7 CCNc1nc(C(=O)c2ccc(C)s2)c2sccc2n1 10.1016/j.bmcl.2009.08.040
171485731 195334 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 411 4 1 6 3.9 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(F)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5401410 195334 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 411 4 1 6 3.9 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(F)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
25069914 192155 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 393 4 1 8 2.1 CC(=O)Nc1cc(-c2cccc(N3CCOCC3)n2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
CHEMBL520229 192155 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 393 4 1 8 2.1 CC(=O)Nc1cc(-c2cccc(N3CCOCC3)n2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
145954098 162634 None 0 Human Functional pIC50 = 7.9 7.9 35 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 345 4 2 8 4.1 Nc1nc(NCc2cccs2)nc2sc(-c3cccs3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4168016 162634 None 0 Human Functional pIC50 = 7.9 7.9 35 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 345 4 2 8 4.1 Nc1nc(NCc2cccs2)nc2sc(-c3cccs3)nc12 10.1016/j.ejmech.2018.06.020
171485690 196384 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 471 5 1 8 3.2 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(S(C)(=O)=O)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5422621 196384 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 471 5 1 8 3.2 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(S(C)(=O)=O)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
1329 1472 None 53 Human Functional pIC50 = 6.9 6.9 -147 8
Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assayAntagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.9b00106
386 1472 None 53 Human Functional pIC50 = 6.9 6.9 -147 8
Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assayAntagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.9b00106
CHEMBL183 1472 None 53 Human Functional pIC50 = 6.9 6.9 -147 8
Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assayAntagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.9b00106
DB12946 1472 None 53 Human Functional pIC50 = 6.9 6.9 -147 8
Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assayAntagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.9b00106
171485701 195201 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 427 4 1 6 4.4 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(Cl)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5398651 195201 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 427 4 1 6 4.4 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(Cl)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
118726005 117271 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 535 8 2 14 2.5 Nc1nc(NCCc2ccc(Oc3nc(Cl)nc(N4CCOCC4)n3)cc2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
CHEMBL3394261 117271 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 535 8 2 14 2.5 Nc1nc(NCCc2ccc(Oc3nc(Cl)nc(N4CCOCC4)n3)cc2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
118726005 117271 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 535 8 2 14 2.5 Nc1nc(NCCc2ccc(Oc3nc(Cl)nc(N4CCOCC4)n3)cc2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
CHEMBL3394261 117271 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 535 8 2 14 2.5 Nc1nc(NCCc2ccc(Oc3nc(Cl)nc(N4CCOCC4)n3)cc2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
168007153 196461 None 3 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human adenosine A2A receptor in presence of 2000 nM NECAAntagonist activity at human adenosine A2A receptor in presence of 2000 nM NECA
ChEMBL 451 5 2 7 4.0 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(C(C)(C)O)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5424461 196461 None 3 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human adenosine A2A receptor in presence of 2000 nM NECAAntagonist activity at human adenosine A2A receptor in presence of 2000 nM NECA
ChEMBL 451 5 2 7 4.0 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(C(C)(C)O)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
172466841 196659 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 437 6 1 7 3.9 COCc1cccc(Cn2ccc(-c3cc(-c4cccc(C#N)c4C)nc(N)n3)cc2=O)c1 10.1021/acs.jmedchem.2c01860
CHEMBL5429151 196659 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 437 6 1 7 3.9 COCc1cccc(Cn2ccc(-c3cc(-c4cccc(C#N)c4C)nc(N)n3)cc2=O)c1 10.1021/acs.jmedchem.2c01860
10689930 206220 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 361 4 2 9 2.3 Nc1nc2c(cnn2CCc2ccc(O)cc2)c2nc(-c3ccco3)nn12 10.1021/jm9708689
CHEMBL67994 206220 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 361 4 2 9 2.3 Nc1nc2c(cnn2CCc2ccc(O)cc2)c2nc(-c3ccco3)nn12 10.1021/jm9708689
10065148 99169 None 0 Human Functional pIC50 = 7.8 7.8 57 2
Antagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECA
ChEMBL 329 4 1 9 2.4 CCCSc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL280888 99169 None 0 Human Functional pIC50 = 7.8 7.8 57 2
Antagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECA
ChEMBL 329 4 1 9 2.4 CCCSc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
25230949 6007 None 0 Human Functional pIC50 = 5.9 5.9 -95 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 367 5 2 8 3.6 Nc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL1080241 6007 None 0 Human Functional pIC50 = 5.9 5.9 -95 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 367 5 2 8 3.6 Nc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
25230881 6179 None 0 Human Functional pIC50 = 5.9 5.9 -42 4
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 395 6 1 8 4.1 CN(C)c1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
CHEMBL1081160 6179 None 0 Human Functional pIC50 = 5.9 5.9 -42 4
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 395 6 1 8 4.1 CN(C)c1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
67364057 74315 None 0 Human Functional pIC50 = 6.8 6.8 2 2
Antagonist activity at human adenosine 2A receptor expressed in CHO-K1 cells assessed as reduction in cAMP level in presence of 10 uM adenosine by fluorescent AssayAntagonist activity at human adenosine 2A receptor expressed in CHO-K1 cells assessed as reduction in cAMP level in presence of 10 uM adenosine by fluorescent Assay
ChEMBL 295 2 1 5 2.9 Cc1cc(-c2nnc(N)nc2-c2ccc(F)cc2)cc(C)n1 10.1021/acs.jmedchem.0c00237
CHEMBL2024116 74315 None 0 Human Functional pIC50 = 6.8 6.8 2 2
Antagonist activity at human adenosine 2A receptor expressed in CHO-K1 cells assessed as reduction in cAMP level in presence of 10 uM adenosine by fluorescent AssayAntagonist activity at human adenosine 2A receptor expressed in CHO-K1 cells assessed as reduction in cAMP level in presence of 10 uM adenosine by fluorescent Assay
ChEMBL 295 2 1 5 2.9 Cc1cc(-c2nnc(N)nc2-c2ccc(F)cc2)cc(C)n1 10.1021/acs.jmedchem.0c00237
171485694 196036 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 379 4 1 6 3.5 N#Cc1cccc(-c2cc(-c3ccn(Cc4ccccc4)c(=O)c3)nc(N)n2)c1 10.1021/acs.jmedchem.2c01860
CHEMBL5415529 196036 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 379 4 1 6 3.5 N#Cc1cccc(-c2cc(-c3ccn(Cc4ccccc4)c(=O)c3)nc(N)n2)c1 10.1021/acs.jmedchem.2c01860
118726023 120951 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 459 5 2 10 1.6 Nc1nc(N2CCCN(CCc3cccc4c3CC(=O)N4)CC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
CHEMBL3394277 120951 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 459 5 2 10 1.6 Nc1nc(N2CCCN(CCc3cccc4c3CC(=O)N4)CC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
CHEMBL3559212 120951 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 459 5 2 10 1.6 Nc1nc(N2CCCN(CCc3cccc4c3CC(=O)N4)CC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
118726023 120951 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 459 5 2 10 1.6 Nc1nc(N2CCCN(CCc3cccc4c3CC(=O)N4)CC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
CHEMBL3394277 120951 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 459 5 2 10 1.6 Nc1nc(N2CCCN(CCc3cccc4c3CC(=O)N4)CC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
CHEMBL3559212 120951 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 459 5 2 10 1.6 Nc1nc(N2CCCN(CCc3cccc4c3CC(=O)N4)CC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
10831497 162554 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 347 3 2 9 2.1 Nc1nc2c(cnn2Cc2ccc(O)cc2)c2nc(-c3ccco3)nn12 10.1021/jm9708689
CHEMBL416684 162554 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 347 3 2 9 2.1 Nc1nc2c(cnn2Cc2ccc(O)cc2)c2nc(-c3ccco3)nn12 10.1021/jm9708689
25110630 189322 None 0 Rat Functional pIC50 = 7.8 7.8 - 1
Activity at adenosine A2A receptor in rat PC12 cells assessed as intracellular cAMP accumulationActivity at adenosine A2A receptor in rat PC12 cells assessed as intracellular cAMP accumulation
ChEMBL 424 5 1 7 3.1 CC(=O)Nc1cc(-c2cc(F)cc(O[C@H]3CCN(C)C3)c2)nc(-n2nc(C)cc2C)n1 10.1016/j.bmcl.2008.09.048
CHEMBL511440 189322 None 0 Rat Functional pIC50 = 7.8 7.8 - 1
Activity at adenosine A2A receptor in rat PC12 cells assessed as intracellular cAMP accumulationActivity at adenosine A2A receptor in rat PC12 cells assessed as intracellular cAMP accumulation
ChEMBL 424 5 1 7 3.1 CC(=O)Nc1cc(-c2cc(F)cc(O[C@H]3CCN(C)C3)c2)nc(-n2nc(C)cc2C)n1 10.1016/j.bmcl.2008.09.048
168278866 191040 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inverse agonist activity at human adenosine A2A receptor transfected in CHO cell membranes and measured by AlphaScreencAMP assayInverse agonist activity at human adenosine A2A receptor transfected in CHO cell membranes and measured by AlphaScreencAMP assay
ChEMBL 489 6 2 9 4.5 Nc1nc(NC2CCN(C3CCCN(Cc4ccccc4)C3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2021.113907
CHEMBL5185537 191040 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inverse agonist activity at human adenosine A2A receptor transfected in CHO cell membranes and measured by AlphaScreencAMP assayInverse agonist activity at human adenosine A2A receptor transfected in CHO cell membranes and measured by AlphaScreencAMP assay
ChEMBL 489 6 2 9 4.5 Nc1nc(NC2CCN(C3CCCN(Cc4ccccc4)C3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2021.113907
145971923 163113 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2ccncc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4175676 163113 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2ccncc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
118726016 117279 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 459 6 3 10 2.0 Nc1nc(NC2CCN(CCc3cccc4c3CC(=O)N4)CC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
CHEMBL3394271 117279 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 459 6 3 10 2.0 Nc1nc(NC2CCN(CCc3cccc4c3CC(=O)N4)CC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
118726016 117279 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 459 6 3 10 2.0 Nc1nc(NC2CCN(CCc3cccc4c3CC(=O)N4)CC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
CHEMBL3394271 117279 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 459 6 3 10 2.0 Nc1nc(NC2CCN(CCc3cccc4c3CC(=O)N4)CC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
46883108 5835 None 0 Human Functional pIC50 = 5.8 5.8 -3 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 386 5 1 7 4.6 O=C(c1ccc(Cl)s1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079116 5835 None 0 Human Functional pIC50 = 5.8 5.8 -3 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 386 5 1 7 4.6 O=C(c1ccc(Cl)s1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
25138086 186494 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 351 4 1 7 2.4 CC(=O)Nc1cc(-c2cccc(N(C)C)n2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
CHEMBL487572 186494 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 351 4 1 7 2.4 CC(=O)Nc1cc(-c2cccc(N(C)C)n2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
155564753 175645 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 358 4 1 8 2.0 N#CCOc1ccc(-c2cn3c(=O)n(-c4ccccc4)nc3c(N)n2)cc1 10.1021/acs.jmedchem.9b00778
CHEMBL4578482 175645 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 358 4 1 8 2.0 N#CCOc1ccc(-c2cn3c(=O)n(-c4ccccc4)nc3c(N)n2)cc1 10.1021/acs.jmedchem.9b00778
171485725 195302 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 469 5 2 7 4.1 Cc1c(C#N)cccc1-c1nc(N)nc(-c2ccn(Cc3cccc(C(C)(C)O)c3)c(=O)c2)c1F 10.1021/acs.jmedchem.2c01860
CHEMBL5400341 195302 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 469 5 2 7 4.1 Cc1c(C#N)cccc1-c1nc(N)nc(-c2ccn(Cc3cccc(C(C)(C)O)c3)c(=O)c2)c1F 10.1021/acs.jmedchem.2c01860
377 2758 None 42 Human Functional pIC50 = 7.8 7.8 -6 10
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2009.11.131
425 2758 None 42 Human Functional pIC50 = 7.8 7.8 -6 10
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2009.11.131
448222 2758 None 42 Human Functional pIC50 = 7.8 7.8 -6 10
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2009.11.131
CHEMBL464859 2758 None 42 Human Functional pIC50 = 7.8 7.8 -6 10
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2009.11.131
134149255 148252 None 0 Human Functional pIC50 = 7.8 7.8 16 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 2 7 3.6 Nc1nc(NCCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3935610 148252 None 0 Human Functional pIC50 = 7.8 7.8 16 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 2 7 3.6 Nc1nc(NCCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
46230104 201799 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 651 14 5 11 4.5 CCCC(=O)N[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4cn(C(C)C)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL590718 201799 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 651 14 5 11 4.5 CCCC(=O)N[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4cn(C(C)C)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
46883071 5695 None 0 Human Functional pIC50 = 6.8 6.8 1 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 4 1 7 3.9 Cc1ccc(C(=O)c2nc(NC(=O)c3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078001 5695 None 0 Human Functional pIC50 = 6.8 6.8 1 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 4 1 7 3.9 Cc1ccc(C(=O)c2nc(NC(=O)c3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
172454743 196100 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 451 5 1 8 3.6 COC(=O)c1ccccc1Cn1ccc(-c2cc(-c3cccc(C#N)c3C)nc(N)n2)cc1=O 10.1021/acs.jmedchem.2c01860
CHEMBL5416911 196100 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 451 5 1 8 3.6 COC(=O)c1ccccc1Cn1ccc(-c2cc(-c3cccc(C#N)c3C)nc(N)n2)cc1=O 10.1021/acs.jmedchem.2c01860
46883158 5840 None 0 Human Functional pIC50 = 5.8 5.8 -3 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 346 5 1 6 3.9 O=C(c1ccccc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079141 5840 None 0 Human Functional pIC50 = 5.8 5.8 -3 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 346 5 1 6 3.9 O=C(c1ccccc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
155514463 169954 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced increase in cAMP accumulation preincubated for 10 mins followed by NECA addition by GloSensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced increase in cAMP accumulation preincubated for 10 mins followed by NECA addition by GloSensor cAMP assay
ChEMBL 294 2 1 6 3.6 Nc1nc(-c2ccco2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmcl.2018.12.062
CHEMBL4440137 169954 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced increase in cAMP accumulation preincubated for 10 mins followed by NECA addition by GloSensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced increase in cAMP accumulation preincubated for 10 mins followed by NECA addition by GloSensor cAMP assay
ChEMBL 294 2 1 6 3.6 Nc1nc(-c2ccco2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmcl.2018.12.062
CHEMBL4550896 216469 None 2 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293T cells assessed as inhibition of NECA-induced Gs short protein activation by TRUPATH assayAntagonist activity at human adenosine A2A receptor expressed in HEK293T cells assessed as inhibition of NECA-induced Gs short protein activation by TRUPATH assay
ChEMBL None None None O=C(Nc1ccc2ccccc2n1)c1ccco1 10.1021/acsmedchemlett.2c00099
25138083 191721 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 354 4 1 8 2.5 COC(=O)Nc1cc(-c2cncc(OC)c2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
CHEMBL519549 191721 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 354 4 1 8 2.5 COC(=O)Nc1cc(-c2cncc(OC)c2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
50783701 192465 None 1 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 394 6 1 4 5.2 CN(Cc1ccccc1)C(=O)c1cccc(Nc2cc(-c3ccccc3)ncn2)c1 10.1016/j.ejmech.2021.113907
CHEMBL5207175 192465 None 1 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 394 6 1 4 5.2 CN(Cc1ccccc1)C(=O)c1cccc(Nc2cc(-c3ccccc3)ncn2)c1 10.1016/j.ejmech.2021.113907
171485698 197149 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 407 5 1 6 4.0 Cc1c(C#N)cccc1-c1cc(-c2ccn(CCc3ccccc3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5439885 197149 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 407 5 1 6 4.0 Cc1c(C#N)cccc1-c1cc(-c2ccn(CCc3ccccc3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
46230246 202691 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 550 13 4 12 3.2 CCc1cnn([C@H]2C[C@@H](n3cnc4c(NCC(CC)CC)nc(NCCc5cn(CC)cn5)nc43)[C@H](O)[C@@H]2O)c1 10.1016/j.bmcl.2009.11.131
CHEMBL596904 202691 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 550 13 4 12 3.2 CCc1cnn([C@H]2C[C@@H](n3cnc4c(NCC(CC)CC)nc(NCCc5cn(CC)cn5)nc43)[C@H](O)[C@@H]2O)c1 10.1016/j.bmcl.2009.11.131
10305241 155188 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 671 13 6 11 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(CNC(=O)NCCN4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
CHEMBL401914 155188 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 671 13 6 11 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(CNC(=O)NCCN4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
10305241 155188 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 671 13 6 11 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(CNC(=O)NCCN4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
CHEMBL401914 155188 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 671 13 6 11 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(CNC(=O)NCCN4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
162650047 180174 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at adenosine 2A receptor in human whole blood assessed as reduction in phosphorylated CREB level preincubated for 20 mins followed by adenosine receptor agonist NECA addition and measured after 30 mins by flow cytometric analysisAntagonist activity at adenosine 2A receptor in human whole blood assessed as reduction in phosphorylated CREB level preincubated for 20 mins followed by adenosine receptor agonist NECA addition and measured after 30 mins by flow cytometric analysis
ChEMBL 393 5 2 7 3.0 COc1nc(-c2ncco2)nc(N)c1C(=O)NCc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.0c00237
CHEMBL4747929 180174 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at adenosine 2A receptor in human whole blood assessed as reduction in phosphorylated CREB level preincubated for 20 mins followed by adenosine receptor agonist NECA addition and measured after 30 mins by flow cytometric analysisAntagonist activity at adenosine 2A receptor in human whole blood assessed as reduction in phosphorylated CREB level preincubated for 20 mins followed by adenosine receptor agonist NECA addition and measured after 30 mins by flow cytometric analysis
ChEMBL 393 5 2 7 3.0 COc1nc(-c2ncco2)nc(N)c1C(=O)NCc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.0c00237
10190 935 None 41 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP by immunoassayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP by immunoassay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.0c00237
44537963 935 None 41 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP by immunoassayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP by immunoassay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.0c00237
44537963.0 935 None 41 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP by immunoassayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP by immunoassay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.0c00237
CHEMBL4297184 935 None 41 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP by immunoassayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP by immunoassay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.0c00237
DB16125 935 None 41 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP by immunoassayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP by immunoassay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.0c00237
25138077 186489 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 367 5 1 7 2.9 COc1cc(OC)cc(-c2cc(NC(C)=O)nc(-n3nc(C)cc3C)n2)c1 10.1021/jm800851u
CHEMBL487569 186489 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 367 5 1 7 2.9 COc1cc(OC)cc(-c2cc(NC(C)=O)nc(-n3nc(C)cc3C)n2)c1 10.1021/jm800851u
10874051 84284 None 0 Human Functional pIC50 = 7.8 7.8 46 2
Antagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECA
ChEMBL 450 5 2 10 3.6 COc1ccc(NC(=O)Nc2nc3nn(C)c(SC)c3c3nc(-c4ccco4)nn23)cc1 10.1021/jm021023m
CHEMBL22113 84284 None 0 Human Functional pIC50 = 7.8 7.8 46 2
Antagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECA
ChEMBL 450 5 2 10 3.6 COc1ccc(NC(=O)Nc2nc3nn(C)c(SC)c3c3nc(-c4ccco4)nn23)cc1 10.1021/jm021023m
145954098 162634 None 0 Human Functional pIC50 = 7.8 7.8 35 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 345 4 2 8 4.1 Nc1nc(NCc2cccs2)nc2sc(-c3cccs3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4168016 162634 None 0 Human Functional pIC50 = 7.8 7.8 35 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 345 4 2 8 4.1 Nc1nc(NCc2cccs2)nc2sc(-c3cccs3)nc12 10.1016/j.ejmech.2018.06.020
168297484 192554 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assayAntagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assay
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2cccnc2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5208415 192554 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assayAntagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assay
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2cccnc2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
46883157 5824 None 0 Human Functional pIC50 = 5.8 5.8 -11 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 5 1 8 3.4 O=C(c1cncs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079044 5824 None 0 Human Functional pIC50 = 5.8 5.8 -11 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 5 1 8 3.4 O=C(c1cncs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
118726012 117276 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 400 3 2 10 2.2 CC(C)(C)OC(=O)N1CCC(Nc2nc(N)n3nc(-c4ccco4)nc3n2)CC1 10.1021/jm501254d
CHEMBL3394267 117276 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 400 3 2 10 2.2 CC(C)(C)OC(=O)N1CCC(Nc2nc(N)n3nc(-c4ccco4)nc3n2)CC1 10.1021/jm501254d
118726012 117276 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 400 3 2 10 2.2 CC(C)(C)OC(=O)N1CCC(Nc2nc(N)n3nc(-c4ccco4)nc3n2)CC1 10.1021/jm501254d
CHEMBL3394267 117276 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 400 3 2 10 2.2 CC(C)(C)OC(=O)N1CCC(Nc2nc(N)n3nc(-c4ccco4)nc3n2)CC1 10.1021/jm501254d
CHEMBL5075711 216881 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCN2CCN(c3ccc(C(F)(F)F)cc3)CC2)o1 10.1021/acs.jmedchem.1c02199
46883073 5706 None 0 Human Functional pIC50 = 6.8 6.8 2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 6 1 7 4.3 Cc1ccc(C(=O)c2nc(NCCc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078086 5706 None 0 Human Functional pIC50 = 6.8 6.8 2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 6 1 7 4.3 Cc1ccc(C(=O)c2nc(NCCc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
118726011 117275 None 0 Human Functional pIC50 = 5.8 5.8 -46 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 517 14 3 10 3.8 CCCN(CCCCCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394266 117275 None 0 Human Functional pIC50 = 5.8 5.8 -46 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 517 14 3 10 3.8 CCCN(CCCCCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
118726011 117275 None 0 Human Functional pIC50 = 5.8 5.8 -46 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 517 14 3 10 3.8 CCCN(CCCCCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394266 117275 None 0 Human Functional pIC50 = 5.8 5.8 -46 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 517 14 3 10 3.8 CCCN(CCCCCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
155558941 174888 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 375 2 2 7 3.1 CC(C)(C)c1cc(-c2cn3c(=O)n(-c4ccccc4)nc3c(N)n2)ccc1O 10.1021/acs.jmedchem.9b00778
CHEMBL4561681 174888 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 375 2 2 7 3.1 CC(C)(C)c1cc(-c2cn3c(=O)n(-c4ccccc4)nc3c(N)n2)ccc1O 10.1021/acs.jmedchem.9b00778
CHEMBL5090017 217727 None 3 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 1 uM NECA by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 1 uM NECA by ultra LANCE cAMP detection assay
ChEMBL None None None COc1ccc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)[C@@H](C)C2)c(F)c1 10.1021/acs.jmedchem.1c02199
134147788 150079 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 323 4 2 7 3.5 Nc1nc(NCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3950142 150079 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 323 4 2 7 3.5 Nc1nc(NCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
25138091 186477 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 393 5 1 8 2.1 COC1CN(c2cccc(-c3cc(NC(C)=O)nc(-n4nc(C)cc4C)n3)n2)C1 10.1021/jm800851u
CHEMBL487554 186477 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 393 5 1 8 2.1 COC1CN(c2cccc(-c3cc(NC(C)=O)nc(-n4nc(C)cc4C)n3)n2)C1 10.1021/jm800851u
9798914 59469 None 4 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 359 5 1 8 2.9 Nc1nc2c(cnn2CCCc2ccccc2)c2nc(-c3ccco3)nn12 10.1021/jm9708689
CHEMBL17121 59469 None 4 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 359 5 1 8 2.9 Nc1nc2c(cnn2CCCc2ccccc2)c2nc(-c3ccco3)nn12 10.1021/jm9708689
118725999 120952 None 0 Human Functional pIC50 = 7.8 7.8 11 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 680 19 4 12 4.1 CCCN(CCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394256 120952 None 0 Human Functional pIC50 = 7.8 7.8 11 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 680 19 4 12 4.1 CCCN(CCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3559222 120952 None 0 Human Functional pIC50 = 7.8 7.8 11 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 680 19 4 12 4.1 CCCN(CCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
118725999 120952 None 0 Human Functional pIC50 = 7.7 7.7 11 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 680 19 4 12 4.1 CCCN(CCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394256 120952 None 0 Human Functional pIC50 = 7.7 7.7 11 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 680 19 4 12 4.1 CCCN(CCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3559222 120952 None 0 Human Functional pIC50 = 7.7 7.7 11 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 680 19 4 12 4.1 CCCN(CCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
145971923 163113 None 0 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2ccncc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4175676 163113 None 0 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2ccncc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
137651319 157565 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine receptor A2A expressed in CHO cell membranes assessed as inhibition of NECA-induced increase of cAMP accumulation preincubated for 10 mins followed by NECA addition measured after 10 mins by GloSensor cAMP assayAntagonist activity at human adenosine receptor A2A expressed in CHO cell membranes assessed as inhibition of NECA-induced increase of cAMP accumulation preincubated for 10 mins followed by NECA addition measured after 10 mins by GloSensor cAMP assay
ChEMBL 333 3 1 7 2.1 COc1ccc(-c2cn3c(=O)n(-c4ccccc4)nc3c(N)n2)cc1 10.1021/acs.jmedchem.7b00457
CHEMBL4079360 157565 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine receptor A2A expressed in CHO cell membranes assessed as inhibition of NECA-induced increase of cAMP accumulation preincubated for 10 mins followed by NECA addition measured after 10 mins by GloSensor cAMP assayAntagonist activity at human adenosine receptor A2A expressed in CHO cell membranes assessed as inhibition of NECA-induced increase of cAMP accumulation preincubated for 10 mins followed by NECA addition measured after 10 mins by GloSensor cAMP assay
ChEMBL 333 3 1 7 2.1 COc1ccc(-c2cn3c(=O)n(-c4ccccc4)nc3c(N)n2)cc1 10.1021/acs.jmedchem.7b00457
17016836 191591 None 8 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 450 8 2 7 4.9 Cc1ccc(Nc2nc(N(CCO)Cc3ccccc3)nc3c2cnn3-c2ccccc2)cc1 10.1016/j.ejmech.2021.113907
CHEMBL5193510 191591 None 8 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 450 8 2 7 4.9 Cc1ccc(Nc2nc(N(CCO)Cc3ccccc3)nc3c2cnn3-c2ccccc2)cc1 10.1016/j.ejmech.2021.113907
71625253 90111 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 491 14 2 10 5.1 CCCCCCCCCC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.bmcl.2013.03.070
CHEMBL2381757 90111 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 491 14 2 10 5.1 CCCCCCCCCC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.bmcl.2013.03.070
71624864 90114 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 399 5 2 8 2.8 Nc1nc(NCCc2ccc(Br)cc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmcl.2013.03.070
CHEMBL2381760 90114 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 399 5 2 8 2.8 Nc1nc(NCCc2ccc(Br)cc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmcl.2013.03.070
71625253 90111 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 491 14 2 10 5.1 CCCCCCCCCC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.bmcl.2013.03.070
CHEMBL2381757 90111 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 491 14 2 10 5.1 CCCCCCCCCC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.bmcl.2013.03.070
71624864 90114 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 399 5 2 8 2.8 Nc1nc(NCCc2ccc(Br)cc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmcl.2013.03.070
CHEMBL2381760 90114 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 399 5 2 8 2.8 Nc1nc(NCCc2ccc(Br)cc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmcl.2013.03.070
172451563 195779 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 423 5 1 7 3.8 COc1cccc(Cn2ccc(-c3cc(-c4cccc(C#N)c4C)nc(N)n3)cc2=O)c1 10.1021/acs.jmedchem.2c01860
CHEMBL5410668 195779 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 423 5 1 7 3.8 COc1cccc(Cn2ccc(-c3cc(-c4cccc(C#N)c4C)nc(N)n3)cc2=O)c1 10.1021/acs.jmedchem.2c01860
46883042 5736 None 0 Human Functional pIC50 = 6.7 6.7 -4 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 366 5 1 7 4.3 Cc1ccc(C(=O)c2nc(NCc3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078348 5736 None 0 Human Functional pIC50 = 6.7 6.7 -4 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 366 5 1 7 4.3 Cc1ccc(C(=O)c2nc(NCc3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
134138961 147712 None 0 Human Functional pIC50 = 6.7 6.7 1 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1ccc(CNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1 10.1021/acs.jmedchem.6b01068
CHEMBL3931329 147712 None 0 Human Functional pIC50 = 6.7 6.7 1 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1ccc(CNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1 10.1021/acs.jmedchem.6b01068
CHEMBL5083172 217337 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CC2CCCCC2)o1 10.1021/acs.jmedchem.1c02199
3086599 904 None 36 Human Functional pIC50 = 7.7 7.7 1 6
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1016/j.bmcl.2009.11.131
375 904 None 36 Human Functional pIC50 = 7.7 7.7 1 6
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1016/j.bmcl.2009.11.131
424 904 None 36 Human Functional pIC50 = 7.7 7.7 1 6
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1016/j.bmcl.2009.11.131
CHEMBL331372 904 None 36 Human Functional pIC50 = 7.7 7.7 1 6
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1016/j.bmcl.2009.11.131
46883207 5981 None 0 Human Functional pIC50 = 5.7 5.7 -2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 347 5 1 7 3.3 O=C(c1ccncc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1080067 5981 None 0 Human Functional pIC50 = 5.7 5.7 -2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 347 5 1 7 3.3 O=C(c1ccncc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
171485672 196872 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 418 4 1 7 3.7 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(C#N)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5433808 196872 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 418 4 1 7 3.7 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(C#N)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
25138084 185298 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 368 5 1 8 2.9 CCOC(=O)Nc1cc(-c2cncc(OC)c2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
CHEMBL485752 185298 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 368 5 1 8 2.9 CCOC(=O)Nc1cc(-c2cncc(OC)c2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
162645933 179652 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by 5 nM A2A agonist NECA addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by 5 nM A2A agonist NECA addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assay
ChEMBL 555 7 2 12 1.5 NC(=O)Cc1cc(N2CCN(CCn3c(=O)sc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)cc1F 10.1021/acs.jmedchem.0c00237
CHEMBL4741609 179652 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by 5 nM A2A agonist NECA addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by 5 nM A2A agonist NECA addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assay
ChEMBL 555 7 2 12 1.5 NC(=O)Cc1cc(N2CCN(CCn3c(=O)sc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)cc1F 10.1021/acs.jmedchem.0c00237
135346979 181265 None 9 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by 5 nM A2A agonist NECA addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by 5 nM A2A agonist NECA addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assay
ChEMBL 604 9 1 13 2.2 C[S+]([O-])CCOc1cc(N2CCN(CCn3c(=O)sc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)cc1F 10.1021/acs.jmedchem.0c00237
CHEMBL4760867 181265 None 9 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by 5 nM A2A agonist NECA addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by 5 nM A2A agonist NECA addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assay
ChEMBL 604 9 1 13 2.2 C[S+]([O-])CCOc1cc(N2CCN(CCn3c(=O)sc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)cc1F 10.1021/acs.jmedchem.0c00237
11533614 202039 None 0 Human Functional pIC50 = 8.6 8.6 602 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 513 12 5 11 1.9 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NC(CC)CC)nc(NCCc4cn(CC)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL592541 202039 None 0 Human Functional pIC50 = 8.6 8.6 602 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 513 12 5 11 1.9 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NC(CC)CC)nc(NCCc4cn(CC)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
145436762 162605 None 0 Human Functional pIC50 = 8.5 8.5 3 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 327 5 2 8 3.2 Nc1nc(NCCc2ccco2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4167557 162605 None 0 Human Functional pIC50 = 8.5 8.5 3 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 327 5 2 8 3.2 Nc1nc(NCCc2ccco2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
162645933 179652 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at adenosine 2A receptor in human peripheral blood lymphocytes assessed as reduction in NECA-stimulated CREB phosphorylation by flow cytometric analysisAntagonist activity at adenosine 2A receptor in human peripheral blood lymphocytes assessed as reduction in NECA-stimulated CREB phosphorylation by flow cytometric analysis
ChEMBL 555 7 2 12 1.5 NC(=O)Cc1cc(N2CCN(CCn3c(=O)sc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)cc1F 10.1021/acs.jmedchem.0c00237
CHEMBL4741609 179652 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at adenosine 2A receptor in human peripheral blood lymphocytes assessed as reduction in NECA-stimulated CREB phosphorylation by flow cytometric analysisAntagonist activity at adenosine 2A receptor in human peripheral blood lymphocytes assessed as reduction in NECA-stimulated CREB phosphorylation by flow cytometric analysis
ChEMBL 555 7 2 12 1.5 NC(=O)Cc1cc(N2CCN(CCn3c(=O)sc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)cc1F 10.1021/acs.jmedchem.0c00237
10645750 206489 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 419 7 1 10 3.0 COc1ccc(CCCn2ncc3c2nc(N)n2nc(-c4ccco4)nc32)cc1OC 10.1021/jm9708689
CHEMBL69794 206489 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 419 7 1 10 3.0 COc1ccc(CCCn2ncc3c2nc(N)n2nc(-c4ccco4)nc32)cc1OC 10.1021/jm9708689
117996795 197180 None 14 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity against human A2A receptorAntagonist activity against human A2A receptor
ChEMBL 569 7 2 7 4.8 CCN1CCN(Cc2ccc3cc(C(=O)Nc4cc(NC(=O)c5ccc6c(c5)OCCO6)ccc4F)ccc3n2)CC1 10.1021/acs.jmedchem.3c00156
CHEMBL5440545 197180 None 14 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity against human A2A receptorAntagonist activity against human A2A receptor
ChEMBL 569 7 2 7 4.8 CCN1CCN(Cc2ccc3cc(C(=O)Nc4cc(NC(=O)c5ccc6c(c5)OCCO6)ccc4F)ccc3n2)CC1 10.1021/acs.jmedchem.3c00156
CHEMBL5088038 217623 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1ccc(N2C[C@H](C)N(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)C[C@H]2C)cc1 10.1021/acs.jmedchem.1c02199
172463471 196537 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 467 7 2 8 3.2 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(OCC(=O)O)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5426226 196537 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 467 7 2 8 3.2 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(OCC(=O)O)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5081105 217209 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCc2ccccc2)o1 10.1021/acs.jmedchem.1c02199
134132684 144808 None 0 Human Functional pIC50 = 7.7 7.7 20 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 3 8 3.3 Nc1nc(NCCc2ccc(O)cc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3908770 144808 None 0 Human Functional pIC50 = 7.7 7.7 20 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 3 8 3.3 Nc1nc(NCCc2ccc(O)cc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL5089845 217719 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCN2CCN(c3ccc(OC(F)F)cc3F)CC2)o1 10.1021/acs.jmedchem.1c02199
10917575 81175 None 0 Human Functional pIC50 = 7.7 7.7 21 2
Antagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECA
ChEMBL 463 5 1 11 2.9 CSc1c2c(nc(NC(=O)Cc3ccc4c(c3)OCO4)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL21572 81175 None 0 Human Functional pIC50 = 7.7 7.7 21 2
Antagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECA
ChEMBL 463 5 1 11 2.9 CSc1c2c(nc(NC(=O)Cc3ccc4c(c3)OCO4)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
46912311 91176 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA additionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
ChEMBL 288 5 2 9 -0.2 Cn1c(-n2nccn2)nc2c(N)nc(CCCCO)nc21 10.1021/jm400491x
CHEMBL2398485 91176 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA additionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
ChEMBL 288 5 2 9 -0.2 Cn1c(-n2nccn2)nc2c(N)nc(CCCCO)nc21 10.1021/jm400491x
CHEMBL5079711 217123 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1ccc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)CC2)nc1 10.1021/acs.jmedchem.1c02199
25074313 192645 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 393 4 1 8 2.1 CC(=O)Nc1cc(-c2cncc(N3CCOCC3)c2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
CHEMBL521029 192645 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 393 4 1 8 2.1 CC(=O)Nc1cc(-c2cncc(N3CCOCC3)c2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
CHEMBL5076939 216958 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3Cc2ccco2)o1 10.1021/acs.jmedchem.1c02199
134138275 147841 None 0 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 339 4 3 8 3.2 Nc1nc(NCc2cccc(O)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3932413 147841 None 0 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 339 4 3 8 3.2 Nc1nc(NCc2cccc(O)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
155554464 174706 None 0 Human Functional pIC50 = 7.7 7.7 -4 3
Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assayAntagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay
ChEMBL 362 5 2 7 3.5 N#Cc1c(N)nc(SCc2cccc(CO)c2)c(C#N)c1-c1ccco1 10.1021/acs.jmedchem.9b00106
CHEMBL4557250 174706 None 0 Human Functional pIC50 = 7.7 7.7 -4 3
Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assayAntagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay
ChEMBL 362 5 2 7 3.5 N#Cc1c(N)nc(SCc2cccc(CO)c2)c(C#N)c1-c1ccco1 10.1021/acs.jmedchem.9b00106
CHEMBL5084222 217392 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1ccc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)CC2)cc1 10.1021/acs.jmedchem.1c02199
25138092 192666 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 407 4 2 8 2.3 CC(=O)Nc1cc(-c2cccc(N3CCC(O)CC3)n2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
CHEMBL521223 192666 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 407 4 2 8 2.3 CC(=O)Nc1cc(-c2cccc(N3CCC(O)CC3)n2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
46882997 5642 None 0 Human Functional pIC50 = 6.7 6.7 3 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 275 2 1 6 2.9 Cc1ccc(C(=O)c2nc(N)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1077751 5642 None 0 Human Functional pIC50 = 6.7 6.7 3 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 275 2 1 6 2.9 Cc1ccc(C(=O)c2nc(N)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL5082528 217297 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1ccc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)C[C@@H]2C)cc1 10.1021/acs.jmedchem.1c02199
46883074 5707 None 0 Human Functional pIC50 = 5.6 5.6 1 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 0 7 4.3 Cc1ccc(C(=O)c2nc(N(C)Cc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078087 5707 None 0 Human Functional pIC50 = 5.6 5.6 1 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 0 7 4.3 Cc1ccc(C(=O)c2nc(N(C)Cc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL5085213 217446 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COCCOc1ccc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)CC2)cc1 10.1021/acs.jmedchem.1c02199
46912313 91171 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA additionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
ChEMBL 288 4 2 9 0.4 CCCC(O)c1nc(N)c2nc(-n3nccn3)n(C)c2n1 10.1021/jm400491x
CHEMBL2398480 91171 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA additionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
ChEMBL 288 4 2 9 0.4 CCCC(O)c1nc(N)c2nc(-n3nccn3)n(C)c2n1 10.1021/jm400491x
25231166 6355 None 0 Human Functional pIC50 = 5.6 5.6 -181 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 CC(Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
CHEMBL1082064 6355 None 0 Human Functional pIC50 = 5.6 5.6 -181 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 CC(Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
25230948 6037 None 0 Human Functional pIC50 = 5.6 5.6 -117 4
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 395 7 2 8 4.4 CCNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
CHEMBL1080421 6037 None 0 Human Functional pIC50 = 5.6 5.6 -117 4
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 395 7 2 8 4.4 CCNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
10193 3010 None 42 Human Functional pIC50 = 7.6 7.6 56 2
Antagonist activity at adenosine 2A receptor (unknown origin) expressed in CHO cells assessed as reduction in intracellular cAMP level preincubated for 15 mins followed by NECA addition and measured after 15 mins by immunoassay methodAntagonist activity at adenosine 2A receptor (unknown origin) expressed in CHO cells assessed as reduction in intracellular cAMP level preincubated for 15 mins followed by NECA addition and measured after 15 mins by immunoassay method
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 10.1021/acs.jmedchem.0c00237
53466958 3010 None 42 Human Functional pIC50 = 7.6 7.6 56 2
Antagonist activity at adenosine 2A receptor (unknown origin) expressed in CHO cells assessed as reduction in intracellular cAMP level preincubated for 15 mins followed by NECA addition and measured after 15 mins by immunoassay methodAntagonist activity at adenosine 2A receptor (unknown origin) expressed in CHO cells assessed as reduction in intracellular cAMP level preincubated for 15 mins followed by NECA addition and measured after 15 mins by immunoassay method
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 10.1021/acs.jmedchem.0c00237
53466958.0 3010 None 42 Human Functional pIC50 = 7.6 7.6 56 2
Antagonist activity at adenosine 2A receptor (unknown origin) expressed in CHO cells assessed as reduction in intracellular cAMP level preincubated for 15 mins followed by NECA addition and measured after 15 mins by immunoassay methodAntagonist activity at adenosine 2A receptor (unknown origin) expressed in CHO cells assessed as reduction in intracellular cAMP level preincubated for 15 mins followed by NECA addition and measured after 15 mins by immunoassay method
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 10.1021/acs.jmedchem.0c00237
CHEMBL3638684 3010 None 42 Human Functional pIC50 = 7.6 7.6 56 2
Antagonist activity at adenosine 2A receptor (unknown origin) expressed in CHO cells assessed as reduction in intracellular cAMP level preincubated for 15 mins followed by NECA addition and measured after 15 mins by immunoassay methodAntagonist activity at adenosine 2A receptor (unknown origin) expressed in CHO cells assessed as reduction in intracellular cAMP level preincubated for 15 mins followed by NECA addition and measured after 15 mins by immunoassay method
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 10.1021/acs.jmedchem.0c00237
CHEMBL3694769 3010 None 42 Human Functional pIC50 = 7.6 7.6 56 2
Antagonist activity at adenosine 2A receptor (unknown origin) expressed in CHO cells assessed as reduction in intracellular cAMP level preincubated for 15 mins followed by NECA addition and measured after 15 mins by immunoassay methodAntagonist activity at adenosine 2A receptor (unknown origin) expressed in CHO cells assessed as reduction in intracellular cAMP level preincubated for 15 mins followed by NECA addition and measured after 15 mins by immunoassay method
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 10.1021/acs.jmedchem.0c00237
135346979 181265 None 9 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by adenosine addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by adenosine addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assay
ChEMBL 604 9 1 13 2.2 C[S+]([O-])CCOc1cc(N2CCN(CCn3c(=O)sc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)cc1F 10.1021/acs.jmedchem.0c00237
CHEMBL4760867 181265 None 9 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by adenosine addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by adenosine addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assay
ChEMBL 604 9 1 13 2.2 C[S+]([O-])CCOc1cc(N2CCN(CCn3c(=O)sc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)cc1F 10.1021/acs.jmedchem.0c00237
134132684 144808 None 0 Human Functional pIC50 = 7.6 7.6 20 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 3 8 3.3 Nc1nc(NCCc2ccc(O)cc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3908770 144808 None 0 Human Functional pIC50 = 7.6 7.6 20 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 3 8 3.3 Nc1nc(NCCc2ccc(O)cc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
145991447 166882 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting methodAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting method
ChEMBL 340 4 2 6 3.1 Nc1cc(NC(=O)CN2CCCCC2)cc2nc(-c3ccco3)oc12 10.1016/j.ejmech.2017.12.007
CHEMBL4284097 166882 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting methodAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting method
ChEMBL 340 4 2 6 3.1 Nc1cc(NC(=O)CN2CCCCC2)cc2nc(-c3ccco3)oc12 10.1016/j.ejmech.2017.12.007
25231167 6219 None 0 Human Functional pIC50 = 5.6 5.6 -20 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 313 5 2 6 2.4 CCNC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1081335 6219 None 0 Human Functional pIC50 = 5.6 5.6 -20 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 313 5 2 6 2.4 CCNC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
71625119 90124 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 451 11 3 11 2.9 CCOC(=O)CCCNc1nc(NCCc2ccc(O)cc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmcl.2013.03.070
CHEMBL2381771 90124 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 451 11 3 11 2.9 CCOC(=O)CCCNc1nc(NCCc2ccc(O)cc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmcl.2013.03.070
46912312 91174 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA additionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
ChEMBL 288 4 2 9 -0.2 C[C@H](O)CCc1nc(N)c2nc(-n3nccn3)n(C)c2n1 10.1021/jm400491x
CHEMBL2398483 91174 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA additionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
ChEMBL 288 4 2 9 -0.2 C[C@H](O)CCc1nc(N)c2nc(-n3nccn3)n(C)c2n1 10.1021/jm400491x
25231170 5517 None 0 Human Functional pIC50 = 5.6 5.6 -8 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 327 5 2 6 2.8 CC(C)NC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1076504 5517 None 0 Human Functional pIC50 = 5.6 5.6 -8 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 327 5 2 6 2.8 CC(C)NC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
155567003 176000 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 621 7 4 9 5.2 CC(C)(C)c1cc(C(=O)NCCC(=O)Nc2ccc(-c3cn4c(=O)n(-c5ccccc5)nc4c(N)n3)cc2)cc(C(C)(C)C)c1O 10.1021/acs.jmedchem.9b00778
CHEMBL4586743 176000 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 621 7 4 9 5.2 CC(C)(C)c1cc(C(=O)NCCC(=O)Nc2ccc(-c3cn4c(=O)n(-c5ccccc5)nc4c(N)n3)cc2)cc(C(C)(C)C)c1O 10.1021/acs.jmedchem.9b00778
71624865 90116 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 350 5 3 8 2.6 Cn1c(-c2ccco2)nc2c(N)nc(NCCc3ccc(O)cc3)nc21 10.1016/j.bmcl.2013.03.070
CHEMBL2381762 90116 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 350 5 3 8 2.6 Cn1c(-c2ccco2)nc2c(N)nc(NCCc3ccc(O)cc3)nc21 10.1016/j.bmcl.2013.03.070
71624865 90116 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 350 5 3 8 2.6 Cn1c(-c2ccco2)nc2c(N)nc(NCCc3ccc(O)cc3)nc21 10.1016/j.bmcl.2013.03.070
CHEMBL2381762 90116 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 350 5 3 8 2.6 Cn1c(-c2ccco2)nc2c(N)nc(NCCc3ccc(O)cc3)nc21 10.1016/j.bmcl.2013.03.070
134138275 147841 None 0 Human Functional pIC50 = 7.6 7.6 1 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 339 4 3 8 3.2 Nc1nc(NCc2cccc(O)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3932413 147841 None 0 Human Functional pIC50 = 7.6 7.6 1 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 339 4 3 8 3.2 Nc1nc(NCc2cccc(O)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
25207803 5687 None 0 Human Functional pIC50 = 6.6 6.6 -234 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL1077943 5687 None 0 Human Functional pIC50 = 6.6 6.6 -234 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL5088993 217678 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCC2CCN(c3ccccc3)CC2)o1 10.1021/acs.jmedchem.1c02199
9851372 95574 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 586 12 4 10 3.8 COC[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(CCNC4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
CHEMBL257429 95574 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 586 12 4 10 3.8 COC[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(CCNC4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
CHEMBL5079580 217111 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2n(C)c(=O)n3Cc2ccccc2)o1 10.1021/acs.jmedchem.1c02199
25138077 186489 None 0 Rat Functional pIC50 = 7.5 7.5 -1 2
Activity at adenosine A2A receptor in rat PC12 cells assessed as intracellular cAMP accumulationActivity at adenosine A2A receptor in rat PC12 cells assessed as intracellular cAMP accumulation
ChEMBL 367 5 1 7 2.9 COc1cc(OC)cc(-c2cc(NC(C)=O)nc(-n3nc(C)cc3C)n2)c1 10.1016/j.bmcl.2008.09.048
CHEMBL487569 186489 None 0 Rat Functional pIC50 = 7.5 7.5 -1 2
Activity at adenosine A2A receptor in rat PC12 cells assessed as intracellular cAMP accumulationActivity at adenosine A2A receptor in rat PC12 cells assessed as intracellular cAMP accumulation
ChEMBL 367 5 1 7 2.9 COc1cc(OC)cc(-c2cc(NC(C)=O)nc(-n3nc(C)cc3C)n2)c1 10.1016/j.bmcl.2008.09.048
134147788 150079 None 0 Human Functional pIC50 = 7.5 7.5 1 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 323 4 2 7 3.5 Nc1nc(NCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3950142 150079 None 0 Human Functional pIC50 = 7.5 7.5 1 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 323 4 2 7 3.5 Nc1nc(NCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
168007153 196461 None 3 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 451 5 2 7 4.0 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(C(C)(C)O)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5424461 196461 None 3 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 451 5 2 7 4.0 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(C(C)(C)O)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5093742 217931 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1ccc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)CC2)cn1 10.1021/acs.jmedchem.1c02199
60167948 90126 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 407 8 2 10 2.7 CCCC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.bmcl.2013.03.070
CHEMBL2381774 90126 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 407 8 2 10 2.7 CCCC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.bmcl.2013.03.070
155522875 170840 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 577 11 3 10 4.3 Nc1nc(-c2ccc(NC(=O)CCNC(=O)CCCCC3CCSS3)cc2)cn2c(=O)n(-c3ccccc3)nc12 10.1021/acs.jmedchem.9b00778
CHEMBL4452288 170840 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 577 11 3 10 4.3 Nc1nc(-c2ccc(NC(=O)CCNC(=O)CCCCC3CCSS3)cc2)cn2c(=O)n(-c3ccccc3)nc12 10.1021/acs.jmedchem.9b00778
CHEMBL5091663 217810 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1ccc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)[C@H](C)C2)cc1 10.1021/acs.jmedchem.1c02199
11153 2008 None 42 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assayAntagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assay
ChEMBL 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 10.1021/acs.jmedchem.2c00101
86676119 2008 None 42 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assayAntagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assay
ChEMBL 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 10.1021/acs.jmedchem.2c00101
CHEMBL4594442 2008 None 42 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assayAntagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assay
ChEMBL 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 10.1021/acs.jmedchem.2c00101
DB16192 2008 None 42 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assayAntagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assay
ChEMBL 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 10.1021/acs.jmedchem.2c00101
145958464 162253 None 0 Human Functional pIC50 = 8.5 8.5 1174 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 369 5 2 8 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3cccs3)sc2n1 10.1016/j.ejmech.2018.06.020
CHEMBL4162037 162253 None 0 Human Functional pIC50 = 8.5 8.5 1174 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 369 5 2 8 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3cccs3)sc2n1 10.1016/j.ejmech.2018.06.020
60167948 90126 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 407 8 2 10 2.7 CCCC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.bmcl.2013.03.070
CHEMBL2381774 90126 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 407 8 2 10 2.7 CCCC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.bmcl.2013.03.070
10528161 165516 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 465 8 1 9 4.5 Nc1nc2c(cnn2CCCc2ccc(OCc3ccccc3)cc2)c2nc(-c3ccco3)nn12 10.1021/jm9708689
CHEMBL423852 165516 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 465 8 1 9 4.5 Nc1nc2c(cnn2CCCc2ccc(OCc3ccccc3)cc2)c2nc(-c3ccco3)nn12 10.1021/jm9708689
155510489 174816 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced increase in cAMP accumulation preincubated for 10 mins followed by NECA addition by GloSensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced increase in cAMP accumulation preincubated for 10 mins followed by NECA addition by GloSensor cAMP assay
ChEMBL 284 2 1 7 3.2 Nc1nc(-c2ccco2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2018.12.062
CHEMBL4559969 174816 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced increase in cAMP accumulation preincubated for 10 mins followed by NECA addition by GloSensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced increase in cAMP accumulation preincubated for 10 mins followed by NECA addition by GloSensor cAMP assay
ChEMBL 284 2 1 7 3.2 Nc1nc(-c2ccco2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2018.12.062
46886594 8836 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 742 15 6 12 1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCN(C)C(=O)NCCN4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
CHEMBL1096891 8836 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 742 15 6 12 1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCN(C)C(=O)NCCN4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
25230100 6354 None 0 Human Functional pIC50 = 5.5 5.5 -5 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 5 2 6 3.8 O=C(NC1CCCCC1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1082063 6354 None 0 Human Functional pIC50 = 5.5 5.5 -5 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 5 2 6 3.8 O=C(NC1CCCCC1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
134138322 148127 None 0 Human Functional pIC50 = 7.5 7.5 15 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 6 2 8 3.6 COc1ccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1 10.1021/acs.jmedchem.6b01068
CHEMBL3934626 148127 None 0 Human Functional pIC50 = 7.5 7.5 15 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 6 2 8 3.6 COc1ccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1 10.1021/acs.jmedchem.6b01068
164617261 184774 None 1 Human Functional pIC50 = 7.5 7.5 20 2
Antagonist activity at human A2A expressed in human HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by NECA stimulation and measured after 30 mins by micro plate reader methodAntagonist activity at human A2A expressed in human HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by NECA stimulation and measured after 30 mins by micro plate reader method
ChEMBL 274 2 1 4 3.1 Nc1nc(Cc2ccccc2)cn2c1nc1ccccc12 10.1016/j.ejmech.2020.113040
CHEMBL4849795 184774 None 1 Human Functional pIC50 = 7.5 7.5 20 2
Antagonist activity at human A2A expressed in human HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by NECA stimulation and measured after 30 mins by micro plate reader methodAntagonist activity at human A2A expressed in human HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by NECA stimulation and measured after 30 mins by micro plate reader method
ChEMBL 274 2 1 4 3.1 Nc1nc(Cc2ccccc2)cn2c1nc1ccccc12 10.1016/j.ejmech.2020.113040
25138082 185530 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 352 5 1 7 2.7 CCC(=O)Nc1cc(-c2cncc(OC)c2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
CHEMBL486140 185530 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 352 5 1 7 2.7 CCC(=O)Nc1cc(-c2cncc(OC)c2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
164617261 184774 None 1 Human Functional pIC50 = 7.5 7.5 20 2
Antagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assayAntagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assay
ChEMBL 274 2 1 4 3.1 Nc1nc(Cc2ccccc2)cn2c1nc1ccccc12 10.1016/j.ejmech.2021.113907
CHEMBL4849795 184774 None 1 Human Functional pIC50 = 7.5 7.5 20 2
Antagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assayAntagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assay
ChEMBL 274 2 1 4 3.1 Nc1nc(Cc2ccccc2)cn2c1nc1ccccc12 10.1016/j.ejmech.2021.113907
10443 969 None 0 Human Functional pIC50 = 6.5 6.5 -223 2
Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assayAntagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay
ChEMBL 390 5 1 8 3.7 COC(=O)c1cccc(c1)CSc1nc(N)c(c(c1C#N)c1ccco1)C#N 10.1021/acs.jmedchem.9b00106
139030524 969 None 0 Human Functional pIC50 = 6.5 6.5 -223 2
Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assayAntagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay
ChEMBL 390 5 1 8 3.7 COC(=O)c1cccc(c1)CSc1nc(N)c(c(c1C#N)c1ccco1)C#N 10.1021/acs.jmedchem.9b00106
CHEMBL4448894 969 None 0 Human Functional pIC50 = 6.5 6.5 -223 2
Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assayAntagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay
ChEMBL 390 5 1 8 3.7 COC(=O)c1cccc(c1)CSc1nc(N)c(c(c1C#N)c1ccco1)C#N 10.1021/acs.jmedchem.9b00106
25230881 6179 None 0 Human Functional pIC50 = 6.5 6.5 -42 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 395 6 1 8 4.1 CN(C)c1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL1081160 6179 None 0 Human Functional pIC50 = 6.5 6.5 -42 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 395 6 1 8 4.1 CN(C)c1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
25138076 185933 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 355 4 1 6 3.1 COc1cccc(-c2cc(NC(C)=O)nc(-n3nc(C)cc3C)n2)c1F 10.1021/jm800851u
CHEMBL486745 185933 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 355 4 1 6 3.1 COc1cccc(-c2cc(NC(C)=O)nc(-n3nc(C)cc3C)n2)c1F 10.1021/jm800851u
118726008 117272 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 418 7 2 9 2.3 CCCN(CCc1cccc2c1CC(=O)N2)c1nc(N)n2nc(-c3ccco3)nc2n1 10.1021/jm501254d
CHEMBL3394263 117272 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 418 7 2 9 2.3 CCCN(CCc1cccc2c1CC(=O)N2)c1nc(N)n2nc(-c3ccco3)nc2n1 10.1021/jm501254d
118726008 117272 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 418 7 2 9 2.3 CCCN(CCc1cccc2c1CC(=O)N2)c1nc(N)n2nc(-c3ccco3)nc2n1 10.1021/jm501254d
CHEMBL3394263 117272 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 418 7 2 9 2.3 CCCN(CCc1cccc2c1CC(=O)N2)c1nc(N)n2nc(-c3ccco3)nc2n1 10.1021/jm501254d
168007153 196461 None 3 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2A receptor in presence of 200 nM NECAAntagonist activity at human adenosine A2A receptor in presence of 200 nM NECA
ChEMBL 451 5 2 7 4.0 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(C(C)(C)O)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5424461 196461 None 3 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2A receptor in presence of 200 nM NECAAntagonist activity at human adenosine A2A receptor in presence of 200 nM NECA
ChEMBL 451 5 2 7 4.0 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(C(C)(C)O)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
10234071 95369 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 741 14 6 11 4.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(CNC(=O)NCCN(C4CCCCC4)C(C)(C)C)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
CHEMBL256489 95369 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 741 14 6 11 4.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(CNC(=O)NCCN(C4CCCCC4)C(C)(C)C)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
176407 4148 None 56 Human Functional pIC50 = 7.5 7.5 13 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm501254d
405 4148 None 56 Human Functional pIC50 = 7.5 7.5 13 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm501254d
CHEMBL113142 4148 None 56 Human Functional pIC50 = 7.5 7.5 13 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm501254d
DB08770 4148 None 56 Human Functional pIC50 = 7.5 7.5 13 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm501254d
176407 4148 None 56 Human Functional pIC50 = 7.5 7.5 13 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm501254d
405 4148 None 56 Human Functional pIC50 = 7.5 7.5 13 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm501254d
CHEMBL113142 4148 None 56 Human Functional pIC50 = 7.5 7.5 13 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm501254d
DB08770 4148 None 56 Human Functional pIC50 = 7.5 7.5 13 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm501254d
10190 935 None 41 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 1 uM NECA by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 1 uM NECA by ultra LANCE cAMP detection assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.1c02199
44537963 935 None 41 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 1 uM NECA by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 1 uM NECA by ultra LANCE cAMP detection assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.1c02199
44537963.0 935 None 41 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 1 uM NECA by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 1 uM NECA by ultra LANCE cAMP detection assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.1c02199
CHEMBL4297184 935 None 41 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 1 uM NECA by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 1 uM NECA by ultra LANCE cAMP detection assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.1c02199
DB16125 935 None 41 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 1 uM NECA by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 1 uM NECA by ultra LANCE cAMP detection assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.1c02199
118725995 117265 None 0 Human Functional pIC50 = 7.5 7.5 13 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 708 19 4 13 4.0 CCCN(CCCNC(=O)CCCC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394253 117265 None 0 Human Functional pIC50 = 7.5 7.5 13 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 708 19 4 13 4.0 CCCN(CCCNC(=O)CCCC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
134149255 148252 None 0 Human Functional pIC50 = 7.5 7.5 16 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 2 7 3.6 Nc1nc(NCCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3935610 148252 None 0 Human Functional pIC50 = 7.5 7.5 16 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 2 7 3.6 Nc1nc(NCCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
118725995 117265 None 0 Human Functional pIC50 = 7.5 7.5 13 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 708 19 4 13 4.0 CCCN(CCCNC(=O)CCCC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394253 117265 None 0 Human Functional pIC50 = 7.5 7.5 13 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 708 19 4 13 4.0 CCCN(CCCNC(=O)CCCC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
46883072 5705 None 0 Human Functional pIC50 = 6.5 6.5 2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 6 1 7 4.3 Cc1ccc(C(=O)c2nc(NCCc3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078085 5705 None 0 Human Functional pIC50 = 6.5 6.5 2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 6 1 7 4.3 Cc1ccc(C(=O)c2nc(NCCc3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
172441298 195397 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 451 5 1 8 3.6 COC(=O)c1ccc(Cn2ccc(-c3cc(-c4cccc(C#N)c4C)nc(N)n3)cc2=O)cc1 10.1021/acs.jmedchem.2c01860
CHEMBL5402843 195397 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 451 5 1 8 3.6 COC(=O)c1ccc(Cn2ccc(-c3cc(-c4cccc(C#N)c4C)nc(N)n3)cc2=O)cc1 10.1021/acs.jmedchem.2c01860
145960813 161444 None 0 Human Functional pIC50 = 7.4 7.4 1 3
Inverse agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of basal cAMP level after 30 mins by Alphascreen assayInverse agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of basal cAMP level after 30 mins by Alphascreen assay
ChEMBL 339 4 2 7 4.0 Nc1nc(NCc2cccs2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
CHEMBL4125975 161444 None 0 Human Functional pIC50 = 7.4 7.4 1 3
Inverse agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of basal cAMP level after 30 mins by Alphascreen assayInverse agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of basal cAMP level after 30 mins by Alphascreen assay
ChEMBL 339 4 2 7 4.0 Nc1nc(NCc2cccs2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
CHEMBL5093603 217923 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1ccc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)C[C@H]2C)cc1 10.1021/acs.jmedchem.1c02199
25230951 150387 None 0 Human Functional pIC50 = 5.4 5.4 -100 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 380 6 1 7 4.6 CCc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL3952824 150387 None 0 Human Functional pIC50 = 5.4 5.4 -100 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 380 6 1 7 4.6 CCc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
25230950 152834 None 0 Human Functional pIC50 = 5.4 5.4 -70 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 378 6 1 7 4.6 C=Cc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL3973260 152834 None 0 Human Functional pIC50 = 5.4 5.4 -70 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 378 6 1 7 4.6 C=Cc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
71625252 90125 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 379 6 2 10 1.9 CC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.bmcl.2013.03.070
CHEMBL2381773 90125 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 379 6 2 10 1.9 CC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.bmcl.2013.03.070
CHEMBL5093249 217909 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1ccccc1N1CCN(CCn2c(=O)cnc3c(-c4ccc(C)o4)nc(N)nc32)CC1 10.1021/acs.jmedchem.1c02199
46882996 5641 None 0 Human Functional pIC50 = 5.4 5.4 -1 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 288 3 0 5 3.9 CCc1nc(C(=O)c2ccc(C)s2)c2sccc2n1 10.1016/j.bmcl.2009.08.040
CHEMBL1077750 5641 None 0 Human Functional pIC50 = 5.4 5.4 -1 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 288 3 0 5 3.9 CCc1nc(C(=O)c2ccc(C)s2)c2sccc2n1 10.1016/j.bmcl.2009.08.040
CHEMBL5092671 217870 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCN2CCC(c3ccccc3)CC2)o1 10.1021/acs.jmedchem.1c02199
71625252 90125 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 379 6 2 10 1.9 CC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.bmcl.2013.03.070
CHEMBL2381773 90125 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 379 6 2 10 1.9 CC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.bmcl.2013.03.070
171485671 195665 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 354 4 1 5 3.6 Nc1nc(-c2ccccc2)cc(-c2ccn(Cc3ccccc3)c(=O)c2)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5408468 195665 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 354 4 1 5 3.6 Nc1nc(-c2ccccc2)cc(-c2ccn(Cc3ccccc3)c(=O)c2)n1 10.1021/acs.jmedchem.2c01860
171485693 195259 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 471 4 1 6 4.5 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(Br)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5399566 195259 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 471 4 1 6 4.5 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(Br)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
8420 3936 None 22 Human Functional pIC50 = 8.4 8.4 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 777 14 7 13 1.9 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2NCC(c1ccccc1)c1ccccc1)C(=O)NCCNC(=O)NC1CCN(CC1)c1ccccn1 10.1016/j.bmcl.2009.05.027
9833519 3936 None 22 Human Functional pIC50 = 8.4 8.4 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 777 14 7 13 1.9 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2NCC(c1ccccc1)c1ccccc1)C(=O)NCCNC(=O)NC1CCN(CC1)c1ccccn1 10.1016/j.bmcl.2009.05.027
CHEMBL1096896 3936 None 22 Human Functional pIC50 = 8.4 8.4 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 777 14 7 13 1.9 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2NCC(c1ccccc1)c1ccccc1)C(=O)NCCNC(=O)NC1CCN(CC1)c1ccccn1 10.1016/j.bmcl.2009.05.027
DB12691 3936 None 22 Human Functional pIC50 = 8.4 8.4 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 777 14 7 13 1.9 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2NCC(c1ccccc1)c1ccccc1)C(=O)NCCNC(=O)NC1CCN(CC1)c1ccccn1 10.1016/j.bmcl.2009.05.027
46886597 8839 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 708 14 7 12 1.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCc4ccccn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
CHEMBL1096894 8839 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 708 14 7 12 1.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCc4ccccn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
145436762 162605 None 0 Human Functional pIC50 = 8.4 8.4 3 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 327 5 2 8 3.2 Nc1nc(NCCc2ccco2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4167557 162605 None 0 Human Functional pIC50 = 8.4 8.4 3 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 327 5 2 8 3.2 Nc1nc(NCCc2ccco2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
127046496 139976 None 0 Human Functional pIC50 = 8.4 8.4 4 2
Antagonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 335 4 1 7 3.0 COc1ccccc1Cn1cc2nc(-c3ccc(C)o3)nc(N)c2n1 10.1016/j.bmc.2016.04.048
CHEMBL3799351 139976 None 0 Human Functional pIC50 = 8.4 8.4 4 2
Antagonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 335 4 1 7 3.0 COc1ccccc1Cn1cc2nc(-c3ccc(C)o3)nc(N)c2n1 10.1016/j.bmc.2016.04.048
145958464 162253 None 0 Human Functional pIC50 = 8.4 8.4 1174 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 369 5 2 8 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3cccs3)sc2n1 10.1016/j.ejmech.2018.06.020
CHEMBL4162037 162253 None 0 Human Functional pIC50 = 8.4 8.4 1174 2
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodAntagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 369 5 2 8 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3cccs3)sc2n1 10.1016/j.ejmech.2018.06.020
46230237 201902 None 0 Human Functional pIC50 = 8.3 8.3 8 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 609 12 5 11 3.0 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4cn(C)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL591423 201902 None 0 Human Functional pIC50 = 8.3 8.3 8 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 609 12 5 11 3.0 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4cn(C)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL5071785 216755 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1ccc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)CC2)c(F)c1 10.1021/acs.jmedchem.1c02199
46230240 203362 None 0 Human Functional pIC50 = 7.4 7.4 12 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 663 13 5 11 4.5 CC(C)n1cnc(CCNc2nc(NCC(c3ccccc3)c3ccccc3)c3ncn([C@@H]4C[C@H](NC(=O)C5CCC5)[C@@H](O)[C@H]4O)c3n2)c1 10.1016/j.bmcl.2009.11.131
CHEMBL601515 203362 None 0 Human Functional pIC50 = 7.4 7.4 12 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 663 13 5 11 4.5 CC(C)n1cnc(CCNc2nc(NCC(c3ccccc3)c3ccccc3)c3ncn([C@@H]4C[C@H](NC(=O)C5CCC5)[C@@H](O)[C@H]4O)c3n2)c1 10.1016/j.bmcl.2009.11.131
15729957 90115 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 322 5 1 8 2.0 Nc1nc(OCCc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmcl.2013.03.070
CHEMBL2381761 90115 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 322 5 1 8 2.0 Nc1nc(OCCc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmcl.2013.03.070
118726001 117269 None 0 Human Functional pIC50 = 7.4 7.4 12 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 821 27 5 13 5.6 CCCN(CCCNC(=O)CCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394258 117269 None 0 Human Functional pIC50 = 7.4 7.4 12 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 821 27 5 13 5.6 CCCN(CCCNC(=O)CCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
46883155 5839 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 352 5 1 7 4.0 O=C(c1ccsc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079132 5839 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 352 5 1 7 4.0 O=C(c1ccsc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
15729957 90115 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 322 5 1 8 2.0 Nc1nc(OCCc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmcl.2013.03.070
CHEMBL2381761 90115 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 322 5 1 8 2.0 Nc1nc(OCCc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmcl.2013.03.070
118726001 117269 None 0 Human Functional pIC50 = 7.4 7.4 12 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 821 27 5 13 5.6 CCCN(CCCNC(=O)CCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394258 117269 None 0 Human Functional pIC50 = 7.4 7.4 12 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 821 27 5 13 5.6 CCCN(CCCNC(=O)CCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
176407 4148 None 56 Human Functional pIC50 = 7.4 7.4 13 2
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.bmcl.2013.03.070
405 4148 None 56 Human Functional pIC50 = 7.4 7.4 13 2
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.bmcl.2013.03.070
CHEMBL113142 4148 None 56 Human Functional pIC50 = 7.4 7.4 13 2
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.bmcl.2013.03.070
DB08770 4148 None 56 Human Functional pIC50 = 7.4 7.4 13 2
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.bmcl.2013.03.070
44589891 178934 None 0 Rat Functional pIC50 = 7.4 7.4 - 1
Activity at adenosine A2A receptor in rat PC12 cells assessed as intracellular cAMP accumulationActivity at adenosine A2A receptor in rat PC12 cells assessed as intracellular cAMP accumulation
ChEMBL 406 5 1 7 3.0 CC(=O)Nc1cc(-c2cccc(OC3CCN(C)C3)c2)nc(-n2nc(C)cc2C)n1 10.1016/j.bmcl.2008.09.048
CHEMBL469324 178934 None 0 Rat Functional pIC50 = 7.4 7.4 - 1
Activity at adenosine A2A receptor in rat PC12 cells assessed as intracellular cAMP accumulationActivity at adenosine A2A receptor in rat PC12 cells assessed as intracellular cAMP accumulation
ChEMBL 406 5 1 7 3.0 CC(=O)Nc1cc(-c2cccc(OC3CCN(C)C3)c2)nc(-n2nc(C)cc2C)n1 10.1016/j.bmcl.2008.09.048
176407 4148 None 56 Human Functional pIC50 = 7.4 7.4 13 2
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.bmcl.2013.03.070
405 4148 None 56 Human Functional pIC50 = 7.4 7.4 13 2
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.bmcl.2013.03.070
CHEMBL113142 4148 None 56 Human Functional pIC50 = 7.4 7.4 13 2
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.bmcl.2013.03.070
DB08770 4148 None 56 Human Functional pIC50 = 7.4 7.4 13 2
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.bmcl.2013.03.070
134138322 148127 None 0 Human Functional pIC50 = 7.4 7.4 15 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 6 2 8 3.6 COc1ccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1 10.1021/acs.jmedchem.6b01068
CHEMBL3934626 148127 None 0 Human Functional pIC50 = 7.4 7.4 15 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 6 2 8 3.6 COc1ccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1 10.1021/acs.jmedchem.6b01068
46912315 91175 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA additionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
ChEMBL 288 4 2 9 -0.2 C[C@@H](O)CCc1nc(N)c2nc(-n3nccn3)n(C)c2n1 10.1021/jm400491x
CHEMBL2398484 91175 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA additionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
ChEMBL 288 4 2 9 -0.2 C[C@@H](O)CCc1nc(N)c2nc(-n3nccn3)n(C)c2n1 10.1021/jm400491x
118708234 113427 None 0 Human Functional pIC50 = 6.4 6.4 -10 3
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 329 5 1 5 3.6 Nc1nc(CCCc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
CHEMBL3317574 113427 None 0 Human Functional pIC50 = 6.4 6.4 -10 3
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 329 5 1 5 3.6 Nc1nc(CCCc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
171485670 196154 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 407 4 1 6 4.1 Cc1ccc(Cn2ccc(-c3cc(-c4cccc(C#N)c4C)nc(N)n3)cc2=O)cc1 10.1021/acs.jmedchem.2c01860
CHEMBL5417712 196154 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 407 4 1 6 4.1 Cc1ccc(Cn2ccc(-c3cc(-c4cccc(C#N)c4C)nc(N)n3)cc2=O)cc1 10.1021/acs.jmedchem.2c01860
145960813 161444 None 0 Human Functional pIC50 = 7.4 7.4 1 3
Antagonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 339 4 2 7 4.0 Nc1nc(NCc2cccs2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
CHEMBL4125975 161444 None 0 Human Functional pIC50 = 7.4 7.4 1 3
Antagonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 339 4 2 7 4.0 Nc1nc(NCc2cccs2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
5613 3685 None 30 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA additionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
ChEMBL 272 4 1 8 0.9 CCCCc1nc(N)c2c(n1)n(C)c(n2)n1nccn1 10.1021/jm400491x
9860294 3685 None 30 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA additionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
ChEMBL 272 4 1 8 0.9 CCCCc1nc(N)c2c(n1)n(C)c(n2)n1nccn1 10.1021/jm400491x
CHEMBL197669 3685 None 30 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA additionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
ChEMBL 272 4 1 8 0.9 CCCCc1nc(N)c2c(n1)n(C)c(n2)n1nccn1 10.1021/jm400491x
118726004 117270 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 634 22 3 12 5.4 COC(=O)CCCCCCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1021/jm501254d
CHEMBL3394260 117270 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 634 22 3 12 5.4 COC(=O)CCCCCCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1021/jm501254d
71624992 90120 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 484 11 0 10 2.8 CCOC(=O)CCCOc1ccc(/C=C/c2nc3c(c(=O)n(CC)c(=O)n3CC)n2C)cc1OC 10.1016/j.bmcl.2013.03.070
CHEMBL2381767 90120 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 484 11 0 10 2.8 CCOC(=O)CCCOc1ccc(/C=C/c2nc3c(c(=O)n(CC)c(=O)n3CC)n2C)cc1OC 10.1016/j.bmcl.2013.03.070
118726004 117270 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 634 22 3 12 5.4 COC(=O)CCCCCCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1021/jm501254d
CHEMBL3394260 117270 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 634 22 3 12 5.4 COC(=O)CCCCCCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1021/jm501254d
71624992 90120 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 484 11 0 10 2.8 CCOC(=O)CCCOc1ccc(/C=C/c2nc3c(c(=O)n(CC)c(=O)n3CC)n2C)cc1OC 10.1016/j.bmcl.2013.03.070
CHEMBL2381767 90120 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 484 11 0 10 2.8 CCOC(=O)CCCOc1ccc(/C=C/c2nc3c(c(=O)n(CC)c(=O)n3CC)n2C)cc1OC 10.1016/j.bmcl.2013.03.070
46883159 5841 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 360 5 1 6 4.2 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)cc1 10.1016/j.bmcl.2009.08.040
CHEMBL1079142 5841 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 360 5 1 6 4.2 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)cc1 10.1016/j.bmcl.2009.08.040
46886592 8832 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 687 14 7 12 1.2 O=C(NCCNC(=O)c1nc(NCC(c2ccccc2)c2ccccc2)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1)NCCN1CCCCC1 10.1016/j.bmcl.2009.05.027
CHEMBL1096887 8832 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 687 14 7 12 1.2 O=C(NCCNC(=O)c1nc(NCC(c2ccccc2)c2ccccc2)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1)NCCN1CCCCC1 10.1016/j.bmcl.2009.05.027
CHEMBL5092804 217880 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1cccc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)CC2)c1 10.1021/acs.jmedchem.1c02199
66678431 91173 None 18 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA additionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
ChEMBL 288 4 2 9 -0.2 CC(O)CCc1nc(N)c2nc(-n3nccn3)n(C)c2n1 10.1021/jm400491x
CHEMBL2398482 91173 None 18 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA additionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
ChEMBL 288 4 2 9 -0.2 CC(O)CCc1nc(N)c2nc(-n3nccn3)n(C)c2n1 10.1021/jm400491x
172449577 195664 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 472 5 2 8 2.4 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(S(N)(=O)=O)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5408447 195664 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 472 5 2 8 2.4 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(S(N)(=O)=O)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
25230181 5961 None 0 Human Functional pIC50 = 6.3 6.3 -26 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 C[C@H](Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
CHEMBL1079894 5961 None 0 Human Functional pIC50 = 6.3 6.3 -26 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 C[C@H](Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
CHEMBL5083448 217349 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1cccc(Cn2c(=O)cnc3c(-c4ccc(C)o4)nc(N)nc32)c1 10.1021/acs.jmedchem.1c02199
10859484 77687 None 0 Human Functional pIC50 = 7.3 7.3 2 2
Antagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECA
ChEMBL 298 3 2 9 1.3 CCNc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL20888 77687 None 0 Human Functional pIC50 = 7.3 7.3 2 2
Antagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECA
ChEMBL 298 3 2 9 1.3 CCNc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL544678 77687 None 0 Human Functional pIC50 = 7.3 7.3 2 2
Antagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECA
ChEMBL 298 3 2 9 1.3 CCNc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
145962202 161632 None 0 Human Functional pIC50 = 7.3 7.3 -1 3
Inverse agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of basal cAMP level after 30 mins by Alphascreen assayInverse agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of basal cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 2 7 4.0 COc1cccc(CNc2nc(N)c3nc(-c4ccccc4)sc3n2)c1 10.1016/j.bmc.2018.05.048
CHEMBL4128596 161632 None 0 Human Functional pIC50 = 7.3 7.3 -1 3
Inverse agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of basal cAMP level after 30 mins by Alphascreen assayInverse agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of basal cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 2 7 4.0 COc1cccc(CNc2nc(N)c3nc(-c4ccccc4)sc3n2)c1 10.1016/j.bmc.2018.05.048
CHEMBL5091384 217796 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3Cc2ccccc2)o1 10.1021/acs.jmedchem.1c02199
145990255 167040 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting methodAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting method
ChEMBL 391 5 1 6 4.8 O=C(CN1CCCCC1)Nc1cc(-c2ccco2)c2oc(-c3ccco3)nc2c1 10.1016/j.ejmech.2017.12.007
CHEMBL4287056 167040 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting methodAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting method
ChEMBL 391 5 1 6 4.8 O=C(CN1CCCCC1)Nc1cc(-c2ccco2)c2oc(-c3ccco3)nc2c1 10.1016/j.ejmech.2017.12.007
162645933 179652 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by adenosine addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by adenosine addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assay
ChEMBL 555 7 2 12 1.5 NC(=O)Cc1cc(N2CCN(CCn3c(=O)sc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)cc1F 10.1021/acs.jmedchem.0c00237
CHEMBL4741609 179652 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by adenosine addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assayAntagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by adenosine addition and measured after 30 mins by EU-cAMP tracer based TR-FRET assay
ChEMBL 555 7 2 12 1.5 NC(=O)Cc1cc(N2CCN(CCn3c(=O)sc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)cc1F 10.1021/acs.jmedchem.0c00237
25138081 185525 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 423 6 1 9 1.6 COc1cncc(-c2cc(NC(=O)CN3CCOCC3)nc(-n3nc(C)cc3C)n2)c1 10.1021/jm800851u
CHEMBL486131 185525 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 423 6 1 9 1.6 COc1cncc(-c2cc(NC(=O)CN3CCOCC3)nc(-n3nc(C)cc3C)n2)c1 10.1021/jm800851u
CHEMBL5075272 216851 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCN2CCN(c3ccccc3)CC2)o1 10.1021/acs.jmedchem.1c02199
10146937 8831 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 728 15 7 12 1.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCCN4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
CHEMBL1096886 8831 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 728 15 7 12 1.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCCN4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
10169297 8834 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 744 17 7 12 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCCN(C(C)C)C(C)C)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
CHEMBL1096889 8834 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 744 17 7 12 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCCN(C(C)C)C(C)C)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
46886598 8840 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 792 18 7 12 2.9 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCc4ccc(CN(CC)CC)cc4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
CHEMBL1096895 8840 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 792 18 7 12 2.9 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCc4ccc(CN(CC)CC)cc4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
46230236 201895 None 0 Human Functional pIC50 = 8.3 8.3 8 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 623 13 5 11 3.5 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4cn(CC)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL591356 201895 None 0 Human Functional pIC50 = 8.3 8.3 8 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 623 13 5 11 3.5 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4cn(CC)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
46230290 203847 None 0 Human Functional pIC50 = 8.3 8.3 151 3
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 552 13 5 13 2.1 CCC(CC)CNc1nc(NCCc2cn(CC)cn2)nc2c1ncn2[C@@H]1C[C@H](n2cc(CO)cn2)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL604591 203847 None 0 Human Functional pIC50 = 8.3 8.3 151 3
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 552 13 5 13 2.1 CCC(CC)CNc1nc(NCCc2cn(CC)cn2)nc2c1ncn2[C@@H]1C[C@H](n2cc(CO)cn2)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2009.11.131
145962355 161530 None 0 Human Functional pIC50 = 8.3 8.3 2 3
Inverse agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of basal cAMP level after 30 mins by Alphascreen assayInverse agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of basal cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 2 7 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3ccccc3)sc2n1 10.1016/j.bmc.2018.05.048
CHEMBL4127213 161530 None 0 Human Functional pIC50 = 8.3 8.3 2 3
Inverse agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of basal cAMP level after 30 mins by Alphascreen assayInverse agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of basal cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 2 7 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3ccccc3)sc2n1 10.1016/j.bmc.2018.05.048
CHEMBL5085803 217479 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1cnc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)CC2)c(F)c1 10.1021/acs.jmedchem.1c02199
164627235 186519 None 0 Human Functional pIC50 = 8.2 8.2 22 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 433 4 2 7 3.2 Cc1cc(-c2c(-c3ccc(F)cc3)nc(N)n3nc(CN4CCCCC4)nc23)c[nH]c1=O 10.1021/acsmedchemlett.1c00620
CHEMBL4876056 186519 None 0 Human Functional pIC50 = 8.2 8.2 22 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 433 4 2 7 3.2 Cc1cc(-c2c(-c3ccc(F)cc3)nc(N)n3nc(CN4CCCCC4)nc23)c[nH]c1=O 10.1021/acsmedchemlett.1c00620
CHEMBL5075422 216860 None 4 Human Functional pIC50 = 8.2 8.2 4 4
Antagonist activity at human recombinant adenosine A2A receptor transfected in HEK293 cells co-transfected with Galpha15/16 assessed as intracellular calcium change incubated for 10 mins by microplate reader methodAntagonist activity at human recombinant adenosine A2A receptor transfected in HEK293 cells co-transfected with Galpha15/16 assessed as intracellular calcium change incubated for 10 mins by microplate reader method
ChEMBL None None None Cn1cc(-c2cnc(N)n3nc(-c4ccco4)nc23)ccc1=O 10.1021/acsmedchemlett.1c00599
46230238 203361 None 0 Human Functional pIC50 = 8.2 8.2 23 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 595 12 6 10 3.0 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4c[nH]cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL601514 203361 None 0 Human Functional pIC50 = 8.2 8.2 23 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 595 12 6 10 3.0 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4c[nH]cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
71625118 90123 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 451 11 2 11 2.7 CCOC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.bmcl.2013.03.070
CHEMBL2381770 90123 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 451 11 2 11 2.7 CCOC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.bmcl.2013.03.070
71625118 90123 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 451 11 2 11 2.7 CCOC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.bmcl.2013.03.070
CHEMBL2381770 90123 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 451 11 2 11 2.7 CCOC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.bmcl.2013.03.070
10812872 206040 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 437 6 1 9 3.9 Nc1nc2c(cnn2Cc2ccc(OCc3ccccc3)cc2)c2nc(-c3ccco3)nn12 10.1021/jm9708689
CHEMBL66811 206040 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 437 6 1 9 3.9 Nc1nc2c(cnn2Cc2ccc(OCc3ccccc3)cc2)c2nc(-c3ccco3)nn12 10.1021/jm9708689
CHEMBL5079916 217140 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)o1 10.1021/acs.jmedchem.1c02199
46883110 5837 None 0 Human Functional pIC50 = 7.3 7.3 -2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 352 5 1 7 4.0 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079118 5837 None 0 Human Functional pIC50 = 7.3 7.3 -2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 352 5 1 7 4.0 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
4882 2099 None 54 Human Functional pIC50 = 5.3 5.3 -4 5
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
5311037 2099 None 54 Human Functional pIC50 = 5.3 5.3 -4 5
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
5311037.0 2099 None 54 Human Functional pIC50 = 5.3 5.3 -4 5
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
5608 2099 None 54 Human Functional pIC50 = 5.3 5.3 -4 5
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
CHEMBL431770 2099 None 54 Human Functional pIC50 = 5.3 5.3 -4 5
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
DB11757 2099 None 54 Human Functional pIC50 = 5.3 5.3 -4 5
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
4882 2099 None 54 Human Functional pIC50 = 5.3 5.3 -4 5
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
5311037 2099 None 54 Human Functional pIC50 = 5.3 5.3 -4 5
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
5311037.0 2099 None 54 Human Functional pIC50 = 5.3 5.3 -4 5
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
5608 2099 None 54 Human Functional pIC50 = 5.3 5.3 -4 5
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
CHEMBL431770 2099 None 54 Human Functional pIC50 = 5.3 5.3 -4 5
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
DB11757 2099 None 54 Human Functional pIC50 = 5.3 5.3 -4 5
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
24803315 203300 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 665 12 5 11 4.7 CC(C)n1cnc(CCNc2nc(NCC(c3ccccc3)c3ccccc3)c3ncn([C@@H]4C[C@H](NC(=O)C(C)(C)C)[C@@H](O)[C@H]4O)c3n2)c1 10.1016/j.bmcl.2009.11.131
CHEMBL601081 203300 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 665 12 5 11 4.7 CC(C)n1cnc(CCNc2nc(NCC(c3ccccc3)c3ccccc3)c3ncn([C@@H]4C[C@H](NC(=O)C(C)(C)C)[C@@H](O)[C@H]4O)c3n2)c1 10.1016/j.bmcl.2009.11.131
30466 69980 None 15 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 421 5 4 5 4.4 CCN1CCCC(Nc2cc(C)nc(NC(=N)Nc3ccc(Cl)c(Cl)c3)n2)C1 10.1016/j.ejmech.2021.113907
5360636 69980 None 15 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 421 5 4 5 4.4 CCN1CCCC(Nc2cc(C)nc(NC(=N)Nc3ccc(Cl)c(Cl)c3)n2)C1 10.1016/j.ejmech.2021.113907
9570364 69980 None 15 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 421 5 4 5 4.4 CCN1CCCC(Nc2cc(C)nc(NC(=N)Nc3ccc(Cl)c(Cl)c3)n2)C1 10.1016/j.ejmech.2021.113907
CHEMBL1939337 69980 None 15 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 421 5 4 5 4.4 CCN1CCCC(Nc2cc(C)nc(NC(=N)Nc3ccc(Cl)c(Cl)c3)n2)C1 10.1016/j.ejmech.2021.113907
421107 190181 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 423 7 4 6 4.6 COc1ccc2nc3cc(Cl)ccc3c(Nc3ccc(O)c(CNCCO)c3)c2c1 10.1016/j.ejmech.2021.113907
CHEMBL5172541 190181 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 423 7 4 6 4.6 COc1ccc2nc3cc(Cl)ccc3c(Nc3ccc(O)c(CNCCO)c3)c2c1 10.1016/j.ejmech.2021.113907
459794 190224 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 345 7 3 5 3.0 COc1ccc2nc3cc(Cl)ccc3c(NCCNCCO)c2c1 10.1016/j.ejmech.2021.113907
CHEMBL5173144 190224 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 345 7 3 5 3.0 COc1ccc2nc3cc(Cl)ccc3c(NCCNCCO)c2c1 10.1016/j.ejmech.2021.113907
168297646 192445 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 415 4 3 3 4.3 O[C@H]1CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@H]3C[C@H]2[C@H]1CNCc1ccccc1 10.1016/j.ejmech.2021.113907
CHEMBL5206639 192445 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 415 4 3 3 4.3 O[C@H]1CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@H]3C[C@H]2[C@H]1CNCc1ccccc1 10.1016/j.ejmech.2021.113907
71624867 90118 None 0 Human Functional pIC50 = 4.3 4.3 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 351 5 3 10 0.9 Cn1c(-n2ccnn2)nc2c(N)nc(NCCc3ccc(O)cc3)nc21 10.1016/j.bmcl.2013.03.070
CHEMBL2381764 90118 None 0 Human Functional pIC50 = 4.3 4.3 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 351 5 3 10 0.9 Cn1c(-n2ccnn2)nc2c(N)nc(NCCc3ccc(O)cc3)nc21 10.1016/j.bmcl.2013.03.070
171485718 195344 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 423 5 2 7 3.3 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(CO)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5401706 195344 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 423 5 2 7 3.3 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(CO)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
52947525 17666 None 0 Human Functional pIC50 = 5.3 5.3 -1949 3
Antagonist activity at adenosine A2A receptor by cAMP assayAntagonist activity at adenosine A2A receptor by cAMP assay
ChEMBL 451 6 2 7 5.2 COc1ccc(Nc2c(-c3ccc4nccnc4c3)c(C)nn2-c2ccccc2)c(C(=O)O)c1 10.1016/j.bmcl.2010.07.095
CHEMBL1258397 17666 None 0 Human Functional pIC50 = 5.3 5.3 -1949 3
Antagonist activity at adenosine A2A receptor by cAMP assayAntagonist activity at adenosine A2A receptor by cAMP assay
ChEMBL 451 6 2 7 5.2 COc1ccc(Nc2c(-c3ccc4nccnc4c3)c(C)nn2-c2ccccc2)c(C(=O)O)c1 10.1016/j.bmcl.2010.07.095
CHEMBL5091130 217786 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1ccc(N2CC3CCC(C2)N3CCn2c(=O)cnc3c(-c4ccc(C)o4)nc(N)nc32)cc1 10.1021/acs.jmedchem.1c02199
46230151 201998 None 0 Human Functional pIC50 = 7.3 7.3 7 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 464 7 5 11 0.8 Cc1cnn([C@H]2C[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)c1 10.1016/j.bmcl.2009.11.131
CHEMBL592246 201998 None 0 Human Functional pIC50 = 7.3 7.3 7 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 464 7 5 11 0.8 Cc1cnn([C@H]2C[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)c1 10.1016/j.bmcl.2009.11.131
171485692 196048 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 453 5 1 6 5.0 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(C(C)(C)F)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5415792 196048 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 453 5 1 6 5.0 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(C(C)(C)F)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
25138078 175823 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 338 4 1 7 2.3 COc1cncc(-c2cc(NC(C)=O)nc(-n3nc(C)cc3C)n2)c1 10.1021/jm800851u
CHEMBL458242 175823 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 338 4 1 7 2.3 COc1cncc(-c2cc(NC(C)=O)nc(-n3nc(C)cc3C)n2)c1 10.1021/jm800851u
CHEMBL5088463 217650 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCN2CCN(c3cccc(F)c3)CC2)o1 10.1021/acs.jmedchem.1c02199
155554091 175795 None 0 Human Functional pIC50 = 7.2 7.2 -20 3
Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assayAntagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay
ChEMBL 375 5 2 7 3.1 N#Cc1c(N)nc(SCc2cccc(C(N)=O)c2)c(C#N)c1-c1ccco1 10.1021/acs.jmedchem.9b00106
CHEMBL4581984 175795 None 0 Human Functional pIC50 = 7.2 7.2 -20 3
Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assayAntagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay
ChEMBL 375 5 2 7 3.1 N#Cc1c(N)nc(SCc2cccc(C(N)=O)c2)c(C#N)c1-c1ccco1 10.1021/acs.jmedchem.9b00106
CHEMBL5092067 217835 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCN2CCN(c3ccc(F)cc3)CC2)o1 10.1021/acs.jmedchem.1c02199
118726021 117280 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 445 5 2 10 1.2 Nc1nc(N2CCN(CCc3cccc4c3CC(=O)N4)CC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
CHEMBL3394276 117280 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 445 5 2 10 1.2 Nc1nc(N2CCN(CCc3cccc4c3CC(=O)N4)CC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
118726021 117280 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 445 5 2 10 1.2 Nc1nc(N2CCN(CCc3cccc4c3CC(=O)N4)CC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
CHEMBL3394276 117280 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 445 5 2 10 1.2 Nc1nc(N2CCN(CCc3cccc4c3CC(=O)N4)CC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
10233870 98043 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 713 15 6 11 3.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(CNC(=O)NCCN(C(C)C)C4CCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
CHEMBL272761 98043 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 713 15 6 11 3.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(CNC(=O)NCCN(C(C)C)C4CCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
46886596 8838 None 1 Human Functional pIC50 = 8.2 8.2 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 707 14 7 11 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
CHEMBL1096893 8838 None 1 Human Functional pIC50 = 8.2 8.2 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 707 14 7 11 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
10233870 98043 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 713 15 6 11 3.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(CNC(=O)NCCN(C(C)C)C4CCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
CHEMBL272761 98043 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 713 15 6 11 3.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(CNC(=O)NCCN(C(C)C)C4CCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
9904456 99202 None 0 Human Functional pIC50 = 8.2 8.2 30 2
Antagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECA
ChEMBL 301 2 1 9 1.6 CSc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL281129 99202 None 0 Human Functional pIC50 = 8.2 8.2 30 2
Antagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECA
ChEMBL 301 2 1 9 1.6 CSc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
127046493 139884 None 0 Human Functional pIC50 = 8.2 8.2 17 3
Antagonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 321 4 1 7 2.7 COc1ccccc1Cn1cc2nc(-c3ccco3)nc(N)c2n1 10.1016/j.bmc.2016.04.048
CHEMBL3798766 139884 None 0 Human Functional pIC50 = 8.2 8.2 17 3
Antagonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 321 4 1 7 2.7 COc1ccccc1Cn1cc2nc(-c3ccco3)nc(N)c2n1 10.1016/j.bmc.2016.04.048
127046050 140178 None 0 Human Functional pIC50 = 8.2 8.2 20 3
Antagonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 335 4 1 7 3.0 COc1cccc(Cn2cc3nc(-c4ccc(C)o4)nc(N)c3n2)c1 10.1016/j.bmc.2016.04.048
CHEMBL3800587 140178 None 0 Human Functional pIC50 = 8.2 8.2 20 3
Antagonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 335 4 1 7 3.0 COc1cccc(Cn2cc3nc(-c4ccc(C)o4)nc(N)c3n2)c1 10.1016/j.bmc.2016.04.048
CHEMBL5090017 217727 None 3 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 20 nM NECA by GloSensor cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 20 nM NECA by GloSensor cAMP detection assay
ChEMBL None None None COc1ccc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)[C@@H](C)C2)c(F)c1 10.1021/acs.jmedchem.1c02199
CHEMBL5094102 217960 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1ccc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)[C@@H](C)C2)cc1 10.1021/acs.jmedchem.1c02199
44454227 97559 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 587 12 4 11 3.2 COC[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCN4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
CHEMBL270378 97559 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 587 12 4 11 3.2 COC[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCN4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
46230239 201602 None 0 Human Functional pIC50 = 7.2 7.2 5 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 649 13 5 11 4.1 CC(C)n1cnc(CCNc2nc(NCC(c3ccccc3)c3ccccc3)c3ncn([C@@H]4C[C@H](NC(=O)C5CC5)[C@@H](O)[C@H]4O)c3n2)c1 10.1016/j.bmcl.2009.11.131
CHEMBL589348 201602 None 0 Human Functional pIC50 = 7.2 7.2 5 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 649 13 5 11 4.1 CC(C)n1cnc(CCNc2nc(NCC(c3ccccc3)c3ccccc3)c3ncn([C@@H]4C[C@H](NC(=O)C5CC5)[C@@H](O)[C@H]4O)c3n2)c1 10.1016/j.bmcl.2009.11.131
17016860 190802 None 12 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 374 7 3 7 3.7 Cc1cccc(Nc2nc(NCCCO)nc3c2cnn3-c2ccccc2)c1 10.1016/j.ejmech.2021.113907
CHEMBL5182020 190802 None 12 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 374 7 3 7 3.7 Cc1cccc(Nc2nc(NCCCO)nc3c2cnn3-c2ccccc2)c1 10.1016/j.ejmech.2021.113907
10572535 205504 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 391 5 3 10 2.4 Nc1nc2c(cnn2CCCc2ccc(O)c(O)c2)c2nc(-c3ccco3)nn12 10.1021/jm9708689
CHEMBL63520 205504 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 391 5 3 10 2.4 Nc1nc2c(cnn2CCCc2ccc(O)c(O)c2)c2nc(-c3ccco3)nn12 10.1021/jm9708689
CHEMBL5081971 217268 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCN2CCN(c3ccc(Oc4ccccc4)cc3)CC2)o1 10.1021/acs.jmedchem.1c02199
10961304 76039 None 0 Human Functional pIC50 = 7.2 7.2 -1 2
Antagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECA
ChEMBL 447 6 3 10 3.4 CCNc1c2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL20555 76039 None 0 Human Functional pIC50 = 7.2 7.2 -1 2
Antagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECA
ChEMBL 447 6 3 10 3.4 CCNc1c2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL554955 76039 None 0 Human Functional pIC50 = 7.2 7.2 -1 2
Antagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of human Adenosine A2A receptor with 100 nM NECA
ChEMBL 447 6 3 10 3.4 CCNc1c2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL5084124 217386 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCN2CCN(c3ccccc3C(F)(F)F)CC2)o1 10.1021/acs.jmedchem.1c02199
25231168 5700 None 0 Human Functional pIC50 = 5.2 5.2 -32 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 339 4 1 6 2.9 O=C(c1nc(NCc2cccnc2)nc2ccsc12)N1CCCC1 10.1016/j.bmcl.2009.08.040
CHEMBL1078030 5700 None 0 Human Functional pIC50 = 5.2 5.2 -32 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 339 4 1 6 2.9 O=C(c1nc(NCc2cccnc2)nc2ccsc12)N1CCCC1 10.1016/j.bmcl.2009.08.040
11662965 203077 None 0 Human Functional pIC50 = 7.2 7.2 12 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 478 8 5 11 1.1 CCc1cnn([C@H]2C[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)c1 10.1016/j.bmcl.2009.11.131
CHEMBL599387 203077 None 0 Human Functional pIC50 = 7.2 7.2 12 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 478 8 5 11 1.1 CCc1cnn([C@H]2C[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)c1 10.1016/j.bmcl.2009.11.131
46883208 5982 None 0 Human Functional pIC50 = 7.2 7.2 -3 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 386 5 1 7 4.6 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2cc(Cl)sc12 10.1016/j.bmcl.2009.08.040
CHEMBL1080068 5982 None 0 Human Functional pIC50 = 7.2 7.2 -3 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 386 5 1 7 4.6 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2cc(Cl)sc12 10.1016/j.bmcl.2009.08.040
155519776 170486 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced increase in cAMP accumulation preincubated for 10 mins followed by NECA addition by GloSensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced increase in cAMP accumulation preincubated for 10 mins followed by NECA addition by GloSensor cAMP assay
ChEMBL 320 2 2 6 3.7 Nc1nc(-c2cccc(O)c2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmcl.2018.12.062
CHEMBL4447861 170486 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced increase in cAMP accumulation preincubated for 10 mins followed by NECA addition by GloSensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced increase in cAMP accumulation preincubated for 10 mins followed by NECA addition by GloSensor cAMP assay
ChEMBL 320 2 2 6 3.7 Nc1nc(-c2cccc(O)c2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmcl.2018.12.062
118725997 117267 None 0 Human Functional pIC50 = 7.2 7.2 2 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 652 17 4 12 3.4 CCCN(CCCNC(=O)COc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394255 117267 None 0 Human Functional pIC50 = 7.2 7.2 2 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 652 17 4 12 3.4 CCCN(CCCNC(=O)COc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
118725997 117267 None 0 Human Functional pIC50 = 7.2 7.2 2 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 652 17 4 12 3.4 CCCN(CCCNC(=O)COc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394255 117267 None 0 Human Functional pIC50 = 7.2 7.2 2 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 652 17 4 12 3.4 CCCN(CCCNC(=O)COc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL5083945 217380 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCN2CCN(c3ccc(OC(F)F)cc3)CC2)o1 10.1021/acs.jmedchem.1c02199
46883205 5852 None 0 Human Functional pIC50 = 6.2 6.2 2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 376 6 1 7 3.9 COc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)cc1 10.1016/j.bmcl.2009.08.040
CHEMBL1079232 5852 None 0 Human Functional pIC50 = 6.2 6.2 2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 376 6 1 7 3.9 COc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)cc1 10.1016/j.bmcl.2009.08.040
25138079 185524 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 324 3 2 7 2.0 CC(=O)Nc1cc(-c2cncc(O)c2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
CHEMBL486130 185524 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 324 3 2 7 2.0 CC(=O)Nc1cc(-c2cncc(O)c2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
168270759 190101 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assayAntagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assay
ChEMBL 332 4 2 6 1.8 Nc1nc(C(=O)NCCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5171148 190101 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assayAntagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assay
ChEMBL 332 4 2 6 1.8 Nc1nc(C(=O)NCCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
9808834 95358 None 5 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 601 11 5 11 1.9 O=C(NCCN1CCCCC1)c1nc(NCC(c2ccccc2)c2ccccc2)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1016/j.bmcl.2008.01.033
CHEMBL256467 95358 None 5 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 601 11 5 11 1.9 O=C(NCCN1CCCCC1)c1nc(NCC(c2ccccc2)c2ccccc2)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1016/j.bmcl.2008.01.033
9808834 95358 None 5 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 601 11 5 11 1.9 O=C(NCCN1CCCCC1)c1nc(NCC(c2ccccc2)c2ccccc2)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1016/j.bmcl.2009.05.027
CHEMBL256467 95358 None 5 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 601 11 5 11 1.9 O=C(NCCN1CCCCC1)c1nc(NCC(c2ccccc2)c2ccccc2)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1016/j.bmcl.2009.05.027
145962202 161632 None 0 Human Functional pIC50 = 7.2 7.2 -1 3
Antagonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 2 7 4.0 COc1cccc(CNc2nc(N)c3nc(-c4ccccc4)sc3n2)c1 10.1016/j.bmc.2018.05.048
CHEMBL4128596 161632 None 0 Human Functional pIC50 = 7.2 7.2 -1 3
Antagonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 2 7 4.0 COc1cccc(CNc2nc(N)c3nc(-c4ccccc4)sc3n2)c1 10.1016/j.bmc.2018.05.048
46882994 5827 None 0 Human Functional pIC50 = 5.2 5.2 -1 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 260 2 0 5 3.3 Cc1ccc(C(=O)c2ncnc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1079059 5827 None 0 Human Functional pIC50 = 5.2 5.2 -1 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 260 2 0 5 3.3 Cc1ccc(C(=O)c2ncnc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
46230103 201769 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 651 13 5 11 4.3 CC(C)C(=O)N[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4cn(C(C)C)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL590484 201769 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 651 13 5 11 4.3 CC(C)C(=O)N[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4cn(C(C)C)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
25230180 5960 None 0 Human Functional pIC50 = 5.2 5.2 -2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 C[C@@H](Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
CHEMBL1079893 5960 None 0 Human Functional pIC50 = 5.2 5.2 -2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 C[C@@H](Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
171485697 195123 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 393 4 1 6 3.8 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3ccccc3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5397080 195123 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 393 4 1 6 3.8 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3ccccc3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
163215620 190452 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assayAntagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assay
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5176737 190452 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assayAntagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assay
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5203105 190452 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assayAntagonist activity at A2AAR in human HEK293 cells assessed as inhibition of CGS21680-induced cAMP production preincubated for 15 mins followed by CGS21680 addition and measured after 15 mins by HTRF assay
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
10212625 8833 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 770 17 7 12 2.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCCN(C(C)C)C4CCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
CHEMBL1096888 8833 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Agonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysisAgonist activity at adenosine A2A receptor in fMLP-stimulated human neutrophils assessed as inhibition of superoxide production by colorimetric analysis
ChEMBL 770 17 7 12 2.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCNC(=O)NCCN(C(C)C)C4CCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.05.027
25138090 185551 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 406 4 1 8 2.1 CC(=O)Nc1cc(-c2cccc(N3CCN(C)CC3)n2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
CHEMBL486162 185551 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 406 4 1 8 2.1 CC(=O)Nc1cc(-c2cccc(N3CCN(C)CC3)n2)nc(-n2nc(C)cc2C)n1 10.1021/jm800851u
168290291 192092 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inverse agonist activity at human adenosine A2A receptor transfected in CHO cell membranes and measured by AlphaScreencAMP assayInverse agonist activity at human adenosine A2A receptor transfected in CHO cell membranes and measured by AlphaScreencAMP assay
ChEMBL 399 5 1 9 2.1 Nc1nc(N2CCN(CCN3CCCC3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2021.113907
CHEMBL5201270 192092 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inverse agonist activity at human adenosine A2A receptor transfected in CHO cell membranes and measured by AlphaScreencAMP assayInverse agonist activity at human adenosine A2A receptor transfected in CHO cell membranes and measured by AlphaScreencAMP assay
ChEMBL 399 5 1 9 2.1 Nc1nc(N2CCN(CCN3CCCC3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2021.113907
145962355 161530 None 0 Human Functional pIC50 = 8.1 8.1 2 3
Antagonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 2 7 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3ccccc3)sc2n1 10.1016/j.bmc.2018.05.048
CHEMBL4127213 161530 None 0 Human Functional pIC50 = 8.1 8.1 2 3
Antagonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 2 7 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3ccccc3)sc2n1 10.1016/j.bmc.2018.05.048
156821338 185925 None 0 Human Functional pIC50 = 8.1 8.1 8 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 439 5 1 9 2.7 COc1ccc(Cc2nc3c(-c4ccc(=O)n(C)c4)c(-c4ccccc4)nc(N)n3n2)nc1 10.1021/acsmedchemlett.1c00620
CHEMBL4867286 185925 None 0 Human Functional pIC50 = 8.1 8.1 8 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 439 5 1 9 2.7 COc1ccc(Cc2nc3c(-c4ccc(=O)n(C)c4)c(-c4ccccc4)nc(N)n3n2)nc1 10.1021/acsmedchemlett.1c00620
CHEMBL5085791 217477 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COCCOc1ccc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)CC2)c(F)c1 10.1021/acs.jmedchem.1c02199
10190 935 None 41 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at adenosine 2A receptor in human T cells assessed as inhibition of cAMP incubated for 10 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at adenosine 2A receptor in human T cells assessed as inhibition of cAMP incubated for 10 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.0c00237
44537963 935 None 41 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at adenosine 2A receptor in human T cells assessed as inhibition of cAMP incubated for 10 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at adenosine 2A receptor in human T cells assessed as inhibition of cAMP incubated for 10 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.0c00237
44537963.0 935 None 41 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at adenosine 2A receptor in human T cells assessed as inhibition of cAMP incubated for 10 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at adenosine 2A receptor in human T cells assessed as inhibition of cAMP incubated for 10 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.0c00237
CHEMBL4297184 935 None 41 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at adenosine 2A receptor in human T cells assessed as inhibition of cAMP incubated for 10 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at adenosine 2A receptor in human T cells assessed as inhibition of cAMP incubated for 10 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.0c00237
DB16125 935 None 41 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at adenosine 2A receptor in human T cells assessed as inhibition of cAMP incubated for 10 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at adenosine 2A receptor in human T cells assessed as inhibition of cAMP incubated for 10 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.0c00237
25074004 185438 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 395 7 1 8 2.4 COCCN(C)c1cccc(-c2cc(NC(C)=O)nc(-n3nc(C)cc3C)n2)n1 10.1021/jm800851u
CHEMBL485972 185438 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS-21680-induced cAMP production
ChEMBL 395 7 1 8 2.4 COCCN(C)c1cccc(-c2cc(NC(C)=O)nc(-n3nc(C)cc3C)n2)n1 10.1021/jm800851u
145990800 166906 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting methodAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting method
ChEMBL 266 2 1 5 3.9 Nc1cc(-c2ccco2)c2oc(-c3ccco3)nc2c1 10.1016/j.ejmech.2017.12.007
CHEMBL4284595 166906 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting methodAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting method
ChEMBL 266 2 1 5 3.9 Nc1cc(-c2ccco2)c2oc(-c3ccco3)nc2c1 10.1016/j.ejmech.2017.12.007
145990800 166906 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells and measured by [35S]-GTPS binding assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells and measured by [35S]-GTPS binding assay
ChEMBL 266 2 1 5 3.9 Nc1cc(-c2ccco2)c2oc(-c3ccco3)nc2c1 10.1016/j.ejmech.2021.113907
CHEMBL4284595 166906 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells and measured by [35S]-GTPS binding assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells and measured by [35S]-GTPS binding assay
ChEMBL 266 2 1 5 3.9 Nc1cc(-c2ccco2)c2oc(-c3ccco3)nc2c1 10.1016/j.ejmech.2021.113907
25231169 5516 None 0 Human Functional pIC50 = 6.2 6.2 -2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 325 5 2 6 2.6 O=C(NC1CC1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1076503 5516 None 0 Human Functional pIC50 = 6.2 6.2 -2 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 325 5 2 6 2.6 O=C(NC1CC1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
25230098 6218 None 0 Human Functional pIC50 = 5.2 5.2 -14 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 299 4 2 6 2.1 CNC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1081334 6218 None 0 Human Functional pIC50 = 5.2 5.2 -14 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 299 4 2 6 2.1 CNC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL5078181 217028 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCCc2ccccc2)o1 10.1021/acs.jmedchem.1c02199
46883040 5689 None 0 Human Functional pIC50 = 5.2 5.2 -1 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 365 5 1 6 4.9 Cc1ccc(C(=O)c2nc(NCc3ccccc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1077985 5689 None 0 Human Functional pIC50 = 5.2 5.2 -1 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 365 5 1 6 4.9 Cc1ccc(C(=O)c2nc(NCc3ccccc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL5094358 217978 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1ccc(N2CCCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)CC2)cc1 10.1021/acs.jmedchem.1c02199
171485689 195858 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 407 4 1 6 4.1 Cc1cccc(Cn2ccc(-c3cc(-c4cccc(C#N)c4C)nc(N)n3)cc2=O)c1 10.1021/acs.jmedchem.2c01860
CHEMBL5412117 195858 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 407 4 1 6 4.1 Cc1cccc(Cn2ccc(-c3cc(-c4cccc(C#N)c4C)nc(N)n3)cc2=O)c1 10.1021/acs.jmedchem.2c01860
25230948 6037 None 0 Human Functional pIC50 = 6.1 6.1 -117 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 395 7 2 8 4.4 CCNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL1080421 6037 None 0 Human Functional pIC50 = 6.1 6.1 -117 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 395 7 2 8 4.4 CCNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
46883156 5823 None 0 Human Functional pIC50 = 6.1 6.1 -4 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 5 1 8 3.4 O=C(c1nccs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079043 5823 None 0 Human Functional pIC50 = 6.1 6.1 -4 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 5 1 8 3.4 O=C(c1nccs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
155545386 173553 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced increase in cAMP accumulation preincubated for 10 mins followed by NECA addition by GloSensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced increase in cAMP accumulation preincubated for 10 mins followed by NECA addition by GloSensor cAMP assay
ChEMBL 310 2 2 7 3.3 Nc1nc(-c2cccc(O)c2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2018.12.062
CHEMBL4529321 173553 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced increase in cAMP accumulation preincubated for 10 mins followed by NECA addition by GloSensor cAMP assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced increase in cAMP accumulation preincubated for 10 mins followed by NECA addition by GloSensor cAMP assay
ChEMBL 310 2 2 7 3.3 Nc1nc(-c2cccc(O)c2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2018.12.062
147996856 185619 None 0 Human Functional pIC50 = 7.1 7.1 4 2
Antagonist activity at human A2A expressed in human HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by NECA stimulation and measured after 30 mins by micro plate reader methodAntagonist activity at human A2A expressed in human HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by NECA stimulation and measured after 30 mins by micro plate reader method
ChEMBL 326 2 1 5 3.4 COc1cccc(-c2cn3c(nc4cc(F)c(F)cc43)c(N)n2)c1 10.1016/j.ejmech.2020.113040
CHEMBL4862573 185619 None 0 Human Functional pIC50 = 7.1 7.1 4 2
Antagonist activity at human A2A expressed in human HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by NECA stimulation and measured after 30 mins by micro plate reader methodAntagonist activity at human A2A expressed in human HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by NECA stimulation and measured after 30 mins by micro plate reader method
ChEMBL 326 2 1 5 3.4 COc1cccc(-c2cn3c(nc4cc(F)c(F)cc43)c(N)n2)c1 10.1016/j.ejmech.2020.113040
171485673 195671 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 409 4 2 7 3.5 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(O)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5408699 195671 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 409 4 2 7 3.5 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(O)c3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
46882995 5640 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 274 2 0 5 3.6 Cc1nc(C(=O)c2ccc(C)s2)c2sccc2n1 10.1016/j.bmcl.2009.08.040
CHEMBL1077749 5640 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 274 2 0 5 3.6 Cc1nc(C(=O)c2ccc(C)s2)c2sccc2n1 10.1016/j.bmcl.2009.08.040
10668865 103168 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 403 5 1 10 2.7 Nc1nc2c(cnn2CCCc2ccc3c(c2)OCO3)c2nc(-c3ccco3)nn12 10.1021/jm9708689
CHEMBL307748 103168 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 403 5 1 10 2.7 Nc1nc2c(cnn2CCCc2ccc3c(c2)OCO3)c2nc(-c3ccco3)nn12 10.1021/jm9708689
145436761 162932 None 0 Human Functional pIC50 = 8.1 8.1 1 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 325 4 2 9 2.3 Nc1nc(NCc2cnccn2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4172818 162932 None 0 Human Functional pIC50 = 8.1 8.1 1 2
Inverse agonist activity at human adenosine A2A 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 A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 325 4 2 9 2.3 Nc1nc(NCc2cnccn2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
11699353 202038 None 0 Human Functional pIC50 = 8.1 8.1 301 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 527 12 5 11 2.4 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NC(CC)CC)nc(NCCc4cn(C(C)C)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL592540 202038 None 0 Human Functional pIC50 = 8.1 8.1 301 2
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assayAgonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay
ChEMBL 527 12 5 11 2.4 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NC(CC)CC)nc(NCCc4cn(C(C)C)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL5090017 217727 None 3 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 40 nM NECA by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 40 nM NECA by ultra LANCE cAMP detection assay
ChEMBL None None None COc1ccc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)[C@@H](C)C2)c(F)c1 10.1021/acs.jmedchem.1c02199
CHEMBL5090017 217727 None 3 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COc1ccc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)[C@@H](C)C2)c(F)c1 10.1021/acs.jmedchem.1c02199
CHEMBL5078028 217019 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCN2CCN(c3ccc(F)cc3F)CC2)o1 10.1021/acs.jmedchem.1c02199
156821341 186522 None 0 Human Functional pIC50 = 8.1 8.1 2 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 461 4 2 9 2.5 Cn1cc(-c2c(-c3ccc(F)cc3)nc(N)n3nc([C@H](O)c4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
CHEMBL4876080 186522 None 0 Human Functional pIC50 = 8.1 8.1 2 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 461 4 2 9 2.5 Cn1cc(-c2c(-c3ccc(F)cc3)nc(N)n3nc([C@H](O)c4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
10190 935 None 41 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.2c01860
44537963 935 None 41 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.2c01860
44537963.0 935 None 41 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.2c01860
CHEMBL4297184 935 None 41 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.2c01860
DB16125 935 None 41 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.2c01860
176407 4148 None 56 Human Functional pIC50 = 7.1 7.1 13 2
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting methodAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2017.12.007
405 4148 None 56 Human Functional pIC50 = 7.1 7.1 13 2
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting methodAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2017.12.007
CHEMBL113142 4148 None 56 Human Functional pIC50 = 7.1 7.1 13 2
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting methodAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2017.12.007
DB08770 4148 None 56 Human Functional pIC50 = 7.1 7.1 13 2
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting methodAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2017.12.007
25230952 146640 None 0 Human Functional pIC50 = 6.1 6.1 -12 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 458 8 2 9 5.0 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2cc(NCc3cccnc3)sc12 nan
CHEMBL3922797 146640 None 0 Human Functional pIC50 = 6.1 6.1 -12 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 458 8 2 9 5.0 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2cc(NCc3cccnc3)sc12 nan
148938245 185160 None 0 Human Functional pIC50 = 7.1 7.1 1 2
Antagonist activity at human A2A expressed in human HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by NECA stimulation and measured after 30 mins by micro plate reader methodAntagonist activity at human A2A expressed in human HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by NECA stimulation and measured after 30 mins by micro plate reader method
ChEMBL 338 1 1 4 3.9 Nc1nc(-c2cccc(Br)c2)cn2c1nc1ccccc12 10.1016/j.ejmech.2020.113040
CHEMBL4855390 185160 None 0 Human Functional pIC50 = 7.1 7.1 1 2
Antagonist activity at human A2A expressed in human HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by NECA stimulation and measured after 30 mins by micro plate reader methodAntagonist activity at human A2A expressed in human HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins followed by NECA stimulation and measured after 30 mins by micro plate reader method
ChEMBL 338 1 1 4 3.9 Nc1nc(-c2cccc(Br)c2)cn2c1nc1ccccc12 10.1016/j.ejmech.2020.113040
155514696 169999 None 0 Human Functional pIC50 = 7.1 7.1 -30 2
Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assayAntagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay
ChEMBL 333 4 1 7 3.4 N#Cc1c(N)nc(SCc2cccnc2)c(C#N)c1-c1ccco1 10.1021/acs.jmedchem.9b00106
CHEMBL4440752 169999 None 0 Human Functional pIC50 = 7.1 7.1 -30 2
Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assayAntagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay
ChEMBL 333 4 1 7 3.4 N#Cc1c(N)nc(SCc2cccnc2)c(C#N)c1-c1ccco1 10.1021/acs.jmedchem.9b00106
145962529 161485 None 0 Human Functional pIC50 = 7.1 7.1 1 3
Inverse agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of basal cAMP level after 30 mins by Alphascreen assayInverse agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of basal cAMP level after 30 mins by Alphascreen assay
ChEMBL 291 4 2 7 2.7 Cc1nc2c(N)nc(NCCc3cccs3)nc2s1 10.1016/j.bmc.2018.05.048
CHEMBL4126427 161485 None 0 Human Functional pIC50 = 7.1 7.1 1 3
Inverse agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of basal cAMP level after 30 mins by Alphascreen assayInverse agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as inhibition of basal cAMP level after 30 mins by Alphascreen assay
ChEMBL 291 4 2 7 2.7 Cc1nc2c(N)nc(NCCc3cccs3)nc2s1 10.1016/j.bmc.2018.05.048
156821411 185805 None 0 Human Functional pIC50 = 7.1 7.1 1 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 373 4 1 8 2.6 Nc1nc(-c2ccccc2)c(-c2ccnnc2)c2nc(CC3CCCO3)nn12 10.1021/acsmedchemlett.1c00620
CHEMBL4865474 185805 None 0 Human Functional pIC50 = 7.1 7.1 1 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 373 4 1 8 2.6 Nc1nc(-c2ccccc2)c(-c2ccnnc2)c2nc(CC3CCCO3)nn12 10.1021/acsmedchemlett.1c00620
24812771 175811 None 2 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2A receptor assessed as inhibition of CGS-21680-stimulated cAMP productionAntagonist activity at human adenosine A2A receptor assessed as inhibition of CGS-21680-stimulated cAMP production
ChEMBL 344 5 1 7 1.9 COC[C@H]1CCCN1c1cc(NC(C)=O)nc(-n2nc(C)cc2C)n1 10.1021/jm800908d
CHEMBL458224 175811 None 2 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2A receptor assessed as inhibition of CGS-21680-stimulated cAMP productionAntagonist activity at human adenosine A2A receptor assessed as inhibition of CGS-21680-stimulated cAMP production
ChEMBL 344 5 1 7 1.9 COC[C@H]1CCCN1c1cc(NC(C)=O)nc(-n2nc(C)cc2C)n1 10.1021/jm800908d
25138078 175823 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2A receptor assessed as inhibition of CGS-21680-stimulated cAMP productionAntagonist activity at human adenosine A2A receptor assessed as inhibition of CGS-21680-stimulated cAMP production
ChEMBL 338 4 1 7 2.3 COc1cncc(-c2cc(NC(C)=O)nc(-n3nc(C)cc3C)n2)c1 10.1021/jm800908d
CHEMBL458242 175823 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2A receptor assessed as inhibition of CGS-21680-stimulated cAMP productionAntagonist activity at human adenosine A2A receptor assessed as inhibition of CGS-21680-stimulated cAMP production
ChEMBL 338 4 1 7 2.3 COc1cncc(-c2cc(NC(C)=O)nc(-n3nc(C)cc3C)n2)c1 10.1021/jm800908d
118726013 117277 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 300 3 3 9 0.5 Nc1nc(NC2CCNCC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
CHEMBL3394268 117277 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 300 3 3 9 0.5 Nc1nc(NC2CCNCC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
118726013 117277 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 300 3 3 9 0.5 Nc1nc(NC2CCNCC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
CHEMBL3394268 117277 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 300 3 3 9 0.5 Nc1nc(NC2CCNCC2)nc2nc(-c3ccco3)nn12 10.1021/jm501254d
10190 935 None 41 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 40 nM NECA by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 40 nM NECA by ultra LANCE cAMP detection assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.1c02199
44537963 935 None 41 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 40 nM NECA by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 40 nM NECA by ultra LANCE cAMP detection assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.1c02199
44537963.0 935 None 41 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 40 nM NECA by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 40 nM NECA by ultra LANCE cAMP detection assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.1c02199
CHEMBL4297184 935 None 41 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 40 nM NECA by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 40 nM NECA by ultra LANCE cAMP detection assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.1c02199
DB16125 935 None 41 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 40 nM NECA by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in NECA-induced cAMP production incubated for 20 mins in presence of 40 nM NECA by ultra LANCE cAMP detection assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.1c02199
10190 935 None 41 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.1c02199
44537963 935 None 41 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.1c02199
44537963.0 935 None 41 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.1c02199
CHEMBL4297184 935 None 41 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.1c02199
DB16125 935 None 41 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.1c02199
CHEMBL5078193 217030 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCN2CCN(c3ccc(F)cc3Cl)CC2)o1 10.1021/acs.jmedchem.1c02199
9895687 155472 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 642 12 5 11 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCN4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
CHEMBL403478 155472 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Agonist activity at adenosine A2A receptorAgonist activity at adenosine A2A receptor
ChEMBL 642 12 5 11 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(C(=O)NCCN4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2008.01.033
168451710 197167 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 452 5 2 8 3.4 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(C(C)(C)O)n3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
CHEMBL5440290 197167 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assayAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation pretreated for 30 mins followed by NECA induction by GloSensor assay
ChEMBL 452 5 2 8 3.4 Cc1c(C#N)cccc1-c1cc(-c2ccn(Cc3cccc(C(C)(C)O)n3)c(=O)c2)nc(N)n1 10.1021/acs.jmedchem.2c01860
156821415 185579 None 0 Human Functional pIC50 = 8.0 8.0 -5 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 398 4 1 8 3.0 Nc1nc(-c2ccccc2)c(-c2ccnnc2)c2nc(Cc3ncccc3F)nn12 10.1021/acsmedchemlett.1c00620
CHEMBL4862010 185579 None 0 Human Functional pIC50 = 8.0 8.0 -5 2
Antagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2aR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 398 4 1 8 3.0 Nc1nc(-c2ccccc2)c(-c2ccnnc2)c2nc(Cc3ncccc3F)nn12 10.1021/acsmedchemlett.1c00620
CHEMBL5079399 217104 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None COCCOc1ccc(N2CCN(CCn3c(=O)cnc4c(-c5ccc(C)o5)nc(N)nc43)CC2)c(F)c1F 10.1021/acs.jmedchem.1c02199
168278285 191232 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Inverse agonist activity at human adenosine A2A receptor transfected in CHO cell membranes and measured by AlphaScreencAMP assayInverse agonist activity at human adenosine A2A receptor transfected in CHO cell membranes and measured by AlphaScreencAMP assay
ChEMBL 378 3 1 8 3.3 Nc1nc(N2CCN(c3ccccc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2021.113907
CHEMBL5188037 191232 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Inverse agonist activity at human adenosine A2A receptor transfected in CHO cell membranes and measured by AlphaScreencAMP assayInverse agonist activity at human adenosine A2A receptor transfected in CHO cell membranes and measured by AlphaScreencAMP assay
ChEMBL 378 3 1 8 3.3 Nc1nc(N2CCN(c3ccccc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2021.113907
67364057 74315 None 0 Rat Functional pIC50 = 8.0 8.0 -2 2
Antagonist activity at rat adenosine 2A receptor assessed as reduction in cAMP level in presence of 0.1 uM adenosineAntagonist activity at rat adenosine 2A receptor assessed as reduction in cAMP level in presence of 0.1 uM adenosine
ChEMBL 295 2 1 5 2.9 Cc1cc(-c2nnc(N)nc2-c2ccc(F)cc2)cc(C)n1 10.1021/acs.jmedchem.0c00237
CHEMBL2024116 74315 None 0 Rat Functional pIC50 = 8.0 8.0 -2 2
Antagonist activity at rat adenosine 2A receptor assessed as reduction in cAMP level in presence of 0.1 uM adenosineAntagonist activity at rat adenosine 2A receptor assessed as reduction in cAMP level in presence of 0.1 uM adenosine
ChEMBL 295 2 1 5 2.9 Cc1cc(-c2nnc(N)nc2-c2ccc(F)cc2)cc(C)n1 10.1021/acs.jmedchem.0c00237
10766011 206084 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 451 7 1 9 4.1 Nc1nc2c(cnn2CCc2ccc(OCc3ccccc3)cc2)c2nc(-c3ccco3)nn12 10.1021/jm9708689
CHEMBL67134 206084 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human plateletsInhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
ChEMBL 451 7 1 9 4.1 Nc1nc2c(cnn2CCc2ccc(OCc3ccccc3)cc2)c2nc(-c3ccco3)nn12 10.1021/jm9708689
118726010 117274 None 0 Human Functional pIC50 = 6.0 6.0 -10 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 475 11 3 10 2.6 CCCN(CCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394265 117274 None 0 Human Functional pIC50 = 6.0 6.0 -10 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 475 11 3 10 2.6 CCCN(CCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
118726010 117274 None 0 Human Functional pIC50 = 6.0 6.0 -10 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 475 11 3 10 2.6 CCCN(CCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394265 117274 None 0 Human Functional pIC50 = 6.0 6.0 -10 2
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assayInhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
ChEMBL 475 11 3 10 2.6 CCCN(CCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
71625254 90112 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 465 11 2 12 1.9 CCOC(=O)CCCOc1ccc(CCNc2nc(N)c3nc(-n4nccn4)n(C)c3n2)cc1 10.1016/j.bmcl.2013.03.070
CHEMBL2381758 90112 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 465 11 2 12 1.9 CCOC(=O)CCCOc1ccc(CCNc2nc(N)c3nc(-n4nccn4)n(C)c3n2)cc1 10.1016/j.bmcl.2013.03.070
71625254 90112 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 465 11 2 12 1.9 CCOC(=O)CCCOc1ccc(CCNc2nc(N)c3nc(-n4nccn4)n(C)c3n2)cc1 10.1016/j.bmcl.2013.03.070
CHEMBL2381758 90112 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 465 11 2 12 1.9 CCOC(=O)CCCOc1ccc(CCNc2nc(N)c3nc(-n4nccn4)n(C)c3n2)cc1 10.1016/j.bmcl.2013.03.070
67364057 74315 None 0 Rat Functional pIC50 = 7.0 7.0 -2 2
Antagonist activity at rat adenosine 2A receptor assessed as reduction in cAMP level in presence of 10 uM adenosineAntagonist activity at rat adenosine 2A receptor assessed as reduction in cAMP level in presence of 10 uM adenosine
ChEMBL 295 2 1 5 2.9 Cc1cc(-c2nnc(N)nc2-c2ccc(F)cc2)cc(C)n1 10.1021/acs.jmedchem.0c00237
CHEMBL2024116 74315 None 0 Rat Functional pIC50 = 7.0 7.0 -2 2
Antagonist activity at rat adenosine 2A receptor assessed as reduction in cAMP level in presence of 10 uM adenosineAntagonist activity at rat adenosine 2A receptor assessed as reduction in cAMP level in presence of 10 uM adenosine
ChEMBL 295 2 1 5 2.9 Cc1cc(-c2nnc(N)nc2-c2ccc(F)cc2)cc(C)n1 10.1021/acs.jmedchem.0c00237
25207803 5687 None 0 Human Functional pIC50 = 6.0 6.0 -234 4
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
CHEMBL1077943 5687 None 0 Human Functional pIC50 = 6.0 6.0 -234 4
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
71625255 90113 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 421 8 2 11 1.9 CCCC(=O)Oc1ccc(CCNc2nc(N)c3nc(-n4nccn4)n(C)c3n2)cc1 10.1016/j.bmcl.2013.03.070
CHEMBL2381759 90113 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 421 8 2 11 1.9 CCCC(=O)Oc1ccc(CCNc2nc(N)c3nc(-n4nccn4)n(C)c3n2)cc1 10.1016/j.bmcl.2013.03.070
71624866 90117 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 351 5 3 10 0.9 Cn1c(-n2nccn2)nc2c(N)nc(NCCc3ccc(O)cc3)nc21 10.1016/j.bmcl.2013.03.070
CHEMBL2381763 90117 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 351 5 3 10 0.9 Cn1c(-n2nccn2)nc2c(N)nc(NCCc3ccc(O)cc3)nc21 10.1016/j.bmcl.2013.03.070
71625255 90113 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 421 8 2 11 1.9 CCCC(=O)Oc1ccc(CCNc2nc(N)c3nc(-n4nccn4)n(C)c3n2)cc1 10.1016/j.bmcl.2013.03.070
CHEMBL2381759 90113 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 421 8 2 11 1.9 CCCC(=O)Oc1ccc(CCNc2nc(N)c3nc(-n4nccn4)n(C)c3n2)cc1 10.1016/j.bmcl.2013.03.070
71624866 90117 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 351 5 3 10 0.9 Cn1c(-n2nccn2)nc2c(N)nc(NCCc3ccc(O)cc3)nc21 10.1016/j.bmcl.2013.03.070
CHEMBL2381763 90117 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 minsAntagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
ChEMBL 351 5 3 10 0.9 Cn1c(-n2nccn2)nc2c(N)nc(NCCc3ccc(O)cc3)nc21 10.1016/j.bmcl.2013.03.070
CHEMBL5083868 217378 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assayAntagonist activity at human A2aR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 60 mins by ultra LANCE cAMP detection assay
ChEMBL None None None Cc1ccc(-c2nc(N)nc3c2ncc(=O)n3CCCCc2ccccc2)o1 10.1021/acs.jmedchem.1c02199
137637667 156334 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine receptor A2A expressed in CHO cell membranes assessed as inhibition of NECA-induced increase of cAMP accumulation preincubated for 10 mins followed by NECA addition measured after 10 mins by GloSensor cAMP assayAntagonist activity at human adenosine receptor A2A expressed in CHO cell membranes assessed as inhibition of NECA-induced increase of cAMP accumulation preincubated for 10 mins followed by NECA addition measured after 10 mins by GloSensor cAMP assay
ChEMBL 347 4 1 7 2.5 CCOc1ccc(-c2cn3c(=O)n(-c4ccccc4)nc3c(N)n2)cc1 10.1021/acs.jmedchem.7b00457
CHEMBL4064795 156334 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine receptor A2A expressed in CHO cell membranes assessed as inhibition of NECA-induced increase of cAMP accumulation preincubated for 10 mins followed by NECA addition measured after 10 mins by GloSensor cAMP assayAntagonist activity at human adenosine receptor A2A expressed in CHO cell membranes assessed as inhibition of NECA-induced increase of cAMP accumulation preincubated for 10 mins followed by NECA addition measured after 10 mins by GloSensor cAMP assay
ChEMBL 347 4 1 7 2.5 CCOc1ccc(-c2cn3c(=O)n(-c4ccccc4)nc3c(N)n2)cc1 10.1021/acs.jmedchem.7b00457
46883107 5834 None 0 Human Functional pIC50 = 7 7.0 -5 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 1 7 4.9 Cc1ccc(C(=O)c2nc(NC(C)c3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1079115 5834 None 0 Human Functional pIC50 = 7 7.0 -5 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 1 7 4.9 Cc1ccc(C(=O)c2nc(NC(C)c3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
46883043 5737 None 0 Human Functional pIC50 = 6 6.0 -18 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 366 5 1 7 4.3 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078349 5737 None 0 Human Functional pIC50 = 6 6.0 -18 2
Antagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 366 5 1 7 4.3 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
46912314 91177 None 16 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA additionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
ChEMBL 286 4 1 9 0.0 CC(=O)CCc1nc(N)c2nc(-n3nccn3)n(C)c2n1 10.1021/jm400491x
CHEMBL2398486 91177 None 16 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA additionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
ChEMBL 286 4 1 9 0.0 CC(=O)CCc1nc(N)c2nc(-n3nccn3)n(C)c2n1 10.1021/jm400491x
2817165 188929 None 2 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as effect on CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as effect on CGS-21680-induced cAMP production
ChEMBL 251 2 1 5 3.1 N#Cc1c(-c2ccco2)cc(-c2ccco2)nc1N 10.1021/jm701594y
CHEMBL506250 188929 None 2 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as effect on CGS-21680-induced cAMP productionAntagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as effect on CGS-21680-induced cAMP production
ChEMBL 251 2 1 5 3.1 N#Cc1c(-c2ccco2)cc(-c2ccco2)nc1N 10.1021/jm701594y
21874557 3996 None 45 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells treated for 15 mins by calcium mobilization-based FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells treated for 15 mins by calcium mobilization-based FLIPR assay
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm800961g
5612 3996 None 45 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells treated for 15 mins by calcium mobilization-based FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells treated for 15 mins by calcium mobilization-based FLIPR assay
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm800961g
CHEMBL447664 3996 None 45 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells treated for 15 mins by calcium mobilization-based FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells treated for 15 mins by calcium mobilization-based FLIPR assay
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm800961g
DB06625 3996 None 45 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells treated for 15 mins by calcium mobilization-based FLIPR assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells treated for 15 mins by calcium mobilization-based FLIPR assay
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm800961g
11684443 133227 None 0 Human Functional pKd = 6.0 6.0 - 0
Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assay
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL370378 133227 None 0 Human Functional pKd = 6.0 6.0 - 0
Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assay
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11684443 133227 None 0 Rat Functional pKd = 6.9 6.9 - 0
Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleAntagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscle
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL370378 133227 None 0 Rat Functional pKd = 6.9 6.9 - 0
Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleAntagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscle
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11642035 73570 None 0 Human Functional pKd = 5.9 5.9 - 0
Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assay
ChEMBL 512 6 2 7 3.0 COc1cc(OCC(=O)Nc2ccc(Br)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
CHEMBL201750 73570 None 0 Human Functional pKd = 5.9 5.9 - 0
Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assay
ChEMBL 512 6 2 7 3.0 COc1cc(OCC(=O)Nc2ccc(Br)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
44451283 96516 None 0 Rat Functional pKd = 6.8 6.8 - 0
Antagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscleAntagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscle
ChEMBL 473 5 1 7 2.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL262332 96516 None 0 Rat Functional pKd = 6.8 6.8 - 0
Antagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscleAntagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscle
ChEMBL 473 5 1 7 2.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
44587956 174876 None 0 Rat Functional pKd = 6.7 6.7 - 0
Antagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta assessed as inhibition of phenylephrine-induced contractionAntagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta assessed as inhibition of phenylephrine-induced contraction
ChEMBL 554 9 3 7 4.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL456125 174876 None 0 Rat Functional pKd = 6.7 6.7 - 0
Antagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta assessed as inhibition of phenylephrine-induced contractionAntagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta assessed as inhibition of phenylephrine-induced contraction
ChEMBL 554 9 3 7 4.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
44451048 96039 None 0 Rat Functional pKd = 6.6 6.6 - 0
Antagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscleAntagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscle
ChEMBL 519 7 1 7 3.0 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(F)cc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL259580 96039 None 0 Rat Functional pKd = 6.6 6.6 - 0
Antagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscleAntagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscle
ChEMBL 519 7 1 7 3.0 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(F)cc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
44574165 189576 None 0 Rat Functional pKd = 7.6 7.6 - 0
Antagonist activity at adenosine A2A receptor in Wistar-Kyoto rat aorta assessed as inhibition of phenylephrine-induced contraction treated 30 mins before phenylephrine challenge measured after 60 minsAntagonist activity at adenosine A2A receptor in Wistar-Kyoto rat aorta assessed as inhibition of phenylephrine-induced contraction treated 30 mins before phenylephrine challenge measured after 60 mins
ChEMBL 410 4 2 7 3.0 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccsc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL513681 189576 None 0 Rat Functional pKd = 7.6 7.6 - 0
Antagonist activity at adenosine A2A receptor in Wistar-Kyoto rat aorta assessed as inhibition of phenylephrine-induced contraction treated 30 mins before phenylephrine challenge measured after 60 minsAntagonist activity at adenosine A2A receptor in Wistar-Kyoto rat aorta assessed as inhibition of phenylephrine-induced contraction treated 30 mins before phenylephrine challenge measured after 60 mins
ChEMBL 410 4 2 7 3.0 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccsc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
11649145 135273 None 0 Human Functional pKd = 5.5 5.5 - 0
Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assay
ChEMBL 508 8 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(-c5ccccc5)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL372148 135273 None 0 Human Functional pKd = 5.5 5.5 - 0
Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assay
ChEMBL 508 8 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(-c5ccccc5)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
44451199 156960 None 0 Rat Functional pKd = 6.4 6.4 - 0
Antagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscleAntagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscle
ChEMBL 557 9 1 7 4.5 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL407179 156960 None 0 Rat Functional pKd = 6.4 6.4 - 0
Antagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscleAntagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscle
ChEMBL 557 9 1 7 4.5 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
11640539 140986 None 0 Rat Functional pKd = 7.4 7.4 - 0
Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleAntagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscle
ChEMBL 429 5 2 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL382135 140986 None 0 Rat Functional pKd = 7.4 7.4 - 0
Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleAntagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscle
ChEMBL 429 5 2 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11649145 135273 None 0 Rat Functional pKd = 6.3 6.3 - 0
Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleAntagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscle
ChEMBL 508 8 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(-c5ccccc5)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL372148 135273 None 0 Rat Functional pKd = 6.3 6.3 - 0
Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleAntagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscle
ChEMBL 508 8 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(-c5ccccc5)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11640539 140986 None 0 Human Functional pKd = 7.3 7.3 - 0
Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assay
ChEMBL 429 5 2 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL382135 140986 None 0 Human Functional pKd = 7.3 7.3 - 0
Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assay
ChEMBL 429 5 2 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
44450829 95930 None 0 Rat Functional pKd = 6.3 6.3 - 0
Antagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscleAntagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscle
ChEMBL 444 4 1 6 2.2 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCc5ccccc5C4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL259105 95930 None 0 Rat Functional pKd = 6.3 6.3 - 0
Antagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscleAntagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscle
ChEMBL 444 4 1 6 2.2 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCc5ccccc5C4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
11568001 72655 None 0 Rat Functional pKd = 7.3 7.3 - 0
Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleAntagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscle
ChEMBL 422 5 2 6 2.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL199446 72655 None 0 Rat Functional pKd = 7.3 7.3 - 0
Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleAntagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscle
ChEMBL 422 5 2 6 2.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11568001 72655 None 0 Human Functional pKd = 7.2 7.2 - 0
Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assay
ChEMBL 422 5 2 6 2.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL199446 72655 None 0 Human Functional pKd = 7.2 7.2 - 0
Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assay
ChEMBL 422 5 2 6 2.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11632785 73561 None 0 Rat Functional pKd = 6.2 6.2 - 0
Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleAntagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscle
ChEMBL 404 5 2 6 2.3 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL201721 73561 None 0 Rat Functional pKd = 6.2 6.2 - 0
Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleAntagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscle
ChEMBL 404 5 2 6 2.3 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11632785 73561 None 0 Human Functional pKd = 6.2 6.2 - 0
Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assay
ChEMBL 404 5 2 6 2.3 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL201721 73561 None 0 Human Functional pKd = 6.2 6.2 - 0
Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assay
ChEMBL 404 5 2 6 2.3 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
44450982 101029 None 0 Rat Functional pKd = 5.1 5.1 - 0
Antagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscleAntagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscle
ChEMBL 576 8 1 6 5.1 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)(c5ccccc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL294223 101029 None 0 Rat Functional pKd = 5.1 5.1 - 0
Antagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscleAntagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscle
ChEMBL 576 8 1 6 5.1 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)(c5ccccc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
11642035 73570 None 0 Rat Functional pKd = 6.0 6.0 - 0
Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleAntagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscle
ChEMBL 512 6 2 7 3.0 COc1cc(OCC(=O)Nc2ccc(Br)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
CHEMBL201750 73570 None 0 Rat Functional pKd = 6.0 6.0 - 0
Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleAntagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscle
ChEMBL 512 6 2 7 3.0 COc1cc(OCC(=O)Nc2ccc(Br)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
56944736 163691 None 0 Rat Functional pKi = 10.3 10.3 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 532 5 1 13 2.0 Cc1nc2cc(N3CCN(CCn4c(=O)n(C)c5c4nc(N)n4nc(-c6ccco6)nc54)CC3)c(F)cc2o1 10.1021/acsmedchemlett.7b00175
CHEMBL4203542 163691 None 0 Rat Functional pKi = 10.3 10.3 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 532 5 1 13 2.0 Cc1nc2cc(N3CCN(CCn4c(=O)n(C)c5c4nc(N)n4nc(-c6ccco6)nc54)CC3)c(F)cc2o1 10.1021/acsmedchemlett.7b00175
56943964 164831 None 0 Human Functional pKi = 10.2 10.2 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 507 6 1 12 1.6 COc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)c1 10.1021/acsmedchemlett.7b00175
CHEMBL4217582 164831 None 0 Human Functional pKi = 10.2 10.2 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 507 6 1 12 1.6 COc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)c1 10.1021/acsmedchemlett.7b00175
56943964 164831 None 0 Rat Functional pKi = 10.2 10.2 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 507 6 1 12 1.6 COc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)c1 10.1021/acsmedchemlett.7b00175
CHEMBL4217582 164831 None 0 Rat Functional pKi = 10.2 10.2 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 507 6 1 12 1.6 COc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)c1 10.1021/acsmedchemlett.7b00175
56943866 164800 None 0 Human Functional pKi = 10.2 10.2 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 495 5 1 11 1.7 Cn1c(=O)n(CCN2CCN(c3ccc(F)cc3F)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
CHEMBL4217248 164800 None 0 Human Functional pKi = 10.2 10.2 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 495 5 1 11 1.7 Cn1c(=O)n(CCN2CCN(c3ccc(F)cc3F)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
10445452 8734 None 0 Human Functional pKi = 10 10.0 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 263 1 1 5 2.5 Nc1nc(-c2ccco2)c2c(n1)-c1ccccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1095999 8734 None 0 Human Functional pKi = 10 10.0 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 263 1 1 5 2.5 Nc1nc(-c2ccco2)c2c(n1)-c1ccccc1C2=O 10.1016/j.bmcl.2010.03.042
10038941 132172 None 3 Human Functional pKi = 10 10.0 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 273 1 1 4 2.9 Nc1nc(-c2ccccc2)c2c(n1)-c1ccccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL369573 132172 None 3 Human Functional pKi = 10 10.0 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 273 1 1 4 2.9 Nc1nc(-c2ccccc2)c2c(n1)-c1ccccc1C2=O 10.1016/j.bmcl.2010.03.042
56954252 82132 None 0 Human Functional pKi = 10 10.0 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 398 3 1 5 4.6 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(Cc3cnccc3Cl)ccc1C2=O 10.1021/jm201640m
CHEMBL2165801 82132 None 0 Human Functional pKi = 10 10.0 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 398 3 1 5 4.6 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(Cc3cnccc3Cl)ccc1C2=O 10.1021/jm201640m
44438081 93469 None 0 Human Functional pKi = 10 10.0 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 459 6 1 11 2.1 COc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1016/j.bmcl.2006.12.104
CHEMBL245848 93469 None 0 Human Functional pKi = 10 10.0 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 459 6 1 11 2.1 COc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1016/j.bmcl.2006.12.104
10445452 8734 None 0 Human Functional pKi = 10 10.0 - 0
Antagonist activity at human recombinant adenosine receptor A2a by cAMP assayAntagonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 263 1 1 5 2.5 Nc1nc(-c2ccco2)c2c(n1)-c1ccccc1C2=O 10.1021/jm4011669
CHEMBL1095999 8734 None 0 Human Functional pKi = 10 10.0 - 0
Antagonist activity at human recombinant adenosine receptor A2a by cAMP assayAntagonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 263 1 1 5 2.5 Nc1nc(-c2ccco2)c2c(n1)-c1ccccc1C2=O 10.1021/jm4011669
56944736 163691 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 532 5 1 13 2.0 Cc1nc2cc(N3CCN(CCn4c(=O)n(C)c5c4nc(N)n4nc(-c6ccco6)nc54)CC3)c(F)cc2o1 10.1021/acsmedchemlett.7b00175
CHEMBL4203542 163691 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 532 5 1 13 2.0 Cc1nc2cc(N3CCN(CCn4c(=O)n(C)c5c4nc(N)n4nc(-c6ccco6)nc54)CC3)c(F)cc2o1 10.1021/acsmedchemlett.7b00175
46888889 8889 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 297 1 1 5 3.2 Nc1nc(-c2ccc(Cl)o2)c2c(n1)-c1ccccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1097494 8889 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 297 1 1 5 3.2 Nc1nc(-c2ccc(Cl)o2)c2c(n1)-c1ccccc1C2=O 10.1016/j.bmcl.2010.03.042
132941757 158991 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 460 7 1 7 4.4 CCN(CC)C1CCC(C)(C(=O)Nc2nc3c(OC)ccc(N4CCOCC4)c3s2)CC1 10.1021/acs.jmedchem.6b01584
CHEMBL4095355 158991 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 460 7 1 7 4.4 CCN(CC)C1CCC(C)(C(=O)Nc2nc3c(OC)ccc(N4CCOCC4)c3s2)CC1 10.1021/acs.jmedchem.6b01584
132941757 158991 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assayAntagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assay
ChEMBL 460 7 1 7 4.4 CCN(CC)C1CCC(C)(C(=O)Nc2nc3c(OC)ccc(N4CCOCC4)c3s2)CC1 10.1016/j.ejmech.2021.113907
CHEMBL4095355 158991 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assayAntagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assay
ChEMBL 460 7 1 7 4.4 CCN(CC)C1CCC(C)(C(=O)Nc2nc3c(OC)ccc(N4CCOCC4)c3s2)CC1 10.1016/j.ejmech.2021.113907
56943867 164485 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 489 6 1 12 1.5 COc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
CHEMBL4213177 164485 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 489 6 1 12 1.5 COc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
56944358 164460 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 545 7 1 13 1.6 Cn1c(=O)n(CCN2CCN(c3ccc(OC4CCOC4)cc3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
CHEMBL4212821 164460 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 545 7 1 13 1.6 Cn1c(=O)n(CCN2CCN(c3ccc(OC4CCOC4)cc3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
168270116 190057 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 351 6 1 8 2.4 COC[C@H]1CCCN1c1cc(Nc2ccccn2)nc(-n2cccn2)n1 10.1016/j.ejmech.2022.114378
CHEMBL5170337 190057 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 351 6 1 8 2.4 COC[C@H]1CCCN1c1cc(Nc2ccccn2)nc(-n2cccn2)n1 10.1016/j.ejmech.2022.114378
56944062 163880 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 515 7 1 12 2.0 Cn1c(=O)n(CCN2CCN(c3ccc(OC4CC4)cc3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
CHEMBL4205884 163880 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 515 7 1 12 2.0 Cn1c(=O)n(CCN2CCN(c3ccc(OC4CC4)cc3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
137636304 156292 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 419 4 2 7 3.4 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(C)(O)CC3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4064207 156292 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 419 4 2 7 3.4 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(C)(O)CC3)nc12 10.1021/acs.jmedchem.6b01584
137636304 156292 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assayAntagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assay
ChEMBL 419 4 2 7 3.4 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(C)(O)CC3)nc12 10.1016/j.ejmech.2021.113907
CHEMBL4064207 156292 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assayAntagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assay
ChEMBL 419 4 2 7 3.4 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(C)(O)CC3)nc12 10.1016/j.ejmech.2021.113907
56944443 164068 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 559 7 1 13 2.0 Cn1c(=O)n(CCN2CCN(c3ccc(OC4CCOCC4)cc3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
CHEMBL4207914 164068 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 559 7 1 13 2.0 Cn1c(=O)n(CCN2CCN(c3ccc(OC4CCOCC4)cc3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
56944733 164838 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 525 7 1 12 2.0 Cn1c(=O)n(CCN2CCN(c3ccc(OC(F)F)cc3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
CHEMBL4217668 164838 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 525 7 1 12 2.0 Cn1c(=O)n(CCN2CCN(c3ccc(OC(F)F)cc3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
56943766 163838 None 0 Rat Functional pKi = 9.6 9.6 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 533 9 1 13 1.5 COCCOc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
CHEMBL4205341 163838 None 0 Rat Functional pKi = 9.6 9.6 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 533 9 1 13 1.5 COCCOc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
44217846 60997 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 307 3 1 8 1.0 C=Cn1ncc2c1nc(N)n1c(=O)n(Cc3ccccc3)nc21 10.1016/j.bmcl.2011.02.045
CHEMBL1762510 60997 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 307 3 1 8 1.0 C=Cn1ncc2c1nc(N)n1c(=O)n(Cc3ccccc3)nc21 10.1016/j.bmcl.2011.02.045
56944263 164408 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 484 5 1 12 1.3 Cn1c(=O)n(CCN2CCN(c3ccc(C#N)cc3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
CHEMBL4212278 164408 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 484 5 1 12 1.3 Cn1c(=O)n(CCN2CCN(c3ccc(C#N)cc3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
25242240 82138 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 364 3 1 5 3.9 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(Cc3cccnc3)ccc1C2=O 10.1021/jm201640m
CHEMBL2165807 82138 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 364 3 1 5 3.9 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(Cc3cccnc3)ccc1C2=O 10.1021/jm201640m
44438084 93516 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 481 5 1 10 2.9 Nc1nc2c(ncn2CCN2CCN(c3ccc(Cl)cc3F)CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
CHEMBL246055 93516 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 481 5 1 10 2.9 Nc1nc2c(ncn2CCN2CCN(c3ccc(Cl)cc3F)CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
10668061 3553 None 51 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL 389 6 1 9 3.0 COc1ccc(cc1)CCCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1021/acs.jmedchem.0c02169
3283 3553 None 51 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL 389 6 1 9 3.0 COc1ccc(cc1)CCCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1021/acs.jmedchem.0c02169
CHEMBL136689 3553 None 51 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL 389 6 1 9 3.0 COc1ccc(cc1)CCCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1021/acs.jmedchem.0c02169
11618368 3847 None 50 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/acs.jmedchem.6b01584
5611 3847 None 50 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/acs.jmedchem.6b01584
CHEMBL2105747 3847 None 50 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/acs.jmedchem.6b01584
DB12203 3847 None 50 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/acs.jmedchem.6b01584
44217847 60998 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 341 3 1 8 1.6 C=Cn1ncc2c1nc(N)n1c(=O)n(Cc3cccc(Cl)c3)nc21 10.1016/j.bmcl.2011.02.045
CHEMBL1762511 60998 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 341 3 1 8 1.6 C=Cn1ncc2c1nc(N)n1c(=O)n(Cc3cccc(Cl)c3)nc21 10.1016/j.bmcl.2011.02.045
56944264 163990 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 502 5 1 12 1.5 Cn1c(=O)n(CCN2CCN(c3ccc(C#N)c(F)c3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
CHEMBL4207104 163990 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 502 5 1 12 1.5 Cn1c(=O)n(CCN2CCN(c3ccc(C#N)c(F)c3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
145973260 164693 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 568 9 1 14 1.5 COCCOc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5nccs5)nc43)CC2)cc1F 10.1021/acsmedchemlett.7b00175
CHEMBL4215754 164693 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 568 9 1 14 1.5 COCCOc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5nccs5)nc43)CC2)cc1F 10.1021/acsmedchemlett.7b00175
56943869 164799 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 474 5 1 12 1.1 Cc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)nc1 10.1021/acsmedchemlett.7b00175
CHEMBL4217235 164799 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 474 5 1 12 1.1 Cc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)nc1 10.1021/acsmedchemlett.7b00175
44438085 93557 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 463 5 1 10 2.8 Nc1nc2c(ncn2CCN2CCN(c3cccc(Cl)c3)CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
CHEMBL246261 93557 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 463 5 1 10 2.8 Nc1nc2c(ncn2CCN2CCN(c3cccc(Cl)c3)CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
44438082 146208 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 571 9 1 12 3.2 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(C(F)(F)F)c1 10.1016/j.bmcl.2006.12.104
CHEMBL391953 146208 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 571 9 1 12 3.2 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(C(F)(F)F)c1 10.1016/j.bmcl.2006.12.104
16654984 155186 None 0 Human Functional pKi = 9.4 9.4 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 460 8 1 8 3.9 Cc1cc(C)n(-c2cc(NC(=O)COc3cccc(CN(C)C)c3)nc(-c3ccc(C)o3)n2)n1 10.1021/jm4011669
CHEMBL401895 155186 None 0 Human Functional pKi = 9.4 9.4 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 460 8 1 8 3.9 Cc1cc(C)n(-c2cc(NC(=O)COc3cccc(CN(C)C)c3)nc(-c3ccc(C)o3)n2)n1 10.1021/jm4011669
25074316 186476 None 25 Human Functional pKi = 9.4 9.4 - 2
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 421 5 1 8 2.9 COC1CCN(c2cccc(-c3cc(NC(C)=O)nc(-n4nc(C)cc4C)n3)n2)CC1 10.1021/jm4011669
CHEMBL487553 186476 None 25 Human Functional pKi = 9.4 9.4 - 2
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 421 5 1 8 2.9 COC1CCN(c2cccc(-c3cc(NC(C)=O)nc(-n4nc(C)cc4C)n3)n2)CC1 10.1021/jm4011669
56943766 163838 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 533 9 1 13 1.5 COCCOc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
CHEMBL4205341 163838 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 533 9 1 13 1.5 COCCOc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
145964038 164173 None 0 Rat Functional pKi = 9.4 9.4 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 547 9 1 13 1.9 COCC(C)Oc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
CHEMBL4209408 164173 None 0 Rat Functional pKi = 9.4 9.4 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 547 9 1 13 1.9 COCC(C)Oc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
145973260 164693 None 0 Rat Functional pKi = 9.4 9.4 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 568 9 1 14 1.5 COCCOc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5nccs5)nc43)CC2)cc1F 10.1021/acsmedchemlett.7b00175
CHEMBL4215754 164693 None 0 Rat Functional pKi = 9.4 9.4 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 568 9 1 14 1.5 COCCOc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5nccs5)nc43)CC2)cc1F 10.1021/acsmedchemlett.7b00175
44199445 60996 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 343 2 1 6 2.3 Nc1nc2c(c3nn(Cc4ccccc4)c(=O)n13)CCc1ccccc1-2 10.1016/j.bmcl.2011.02.045
CHEMBL1762509 60996 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 343 2 1 6 2.3 Nc1nc2c(c3nn(Cc4ccccc4)c(=O)n13)CCc1ccccc1-2 10.1016/j.bmcl.2011.02.045
46888929 7463 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 280 1 1 6 2.4 Nc1nc(-c2nccs2)c2c(n1)-c1ccccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1086847 7463 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 280 1 1 6 2.4 Nc1nc(-c2nccs2)c2c(n1)-c1ccccc1C2=O 10.1016/j.bmcl.2010.03.042
10117987 3164 None 60 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1016/j.ejmech.2017.12.007
10117987 3164 None 60 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1016/j.ejmech.2021.113907
5614 3164 None 60 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1016/j.ejmech.2017.12.007
5614 3164 None 60 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1016/j.ejmech.2021.113907
CHEMBL240624 3164 None 60 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1016/j.ejmech.2017.12.007
CHEMBL240624 3164 None 60 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1016/j.ejmech.2021.113907
DB11864 3164 None 60 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1016/j.ejmech.2017.12.007
DB11864 3164 None 60 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1016/j.ejmech.2021.113907
56944261 164248 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 533 9 1 13 1.5 COCCOc1cccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c1 10.1021/acsmedchemlett.7b00175
CHEMBL4210241 164248 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 533 9 1 13 1.5 COCCOc1cccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c1 10.1021/acsmedchemlett.7b00175
56954253 82133 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 378 3 1 6 3.6 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(C(=O)c3cccnc3)ccc1C2=O 10.1021/jm201640m
CHEMBL2165802 82133 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 378 3 1 6 3.6 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(C(=O)c3cccnc3)ccc1C2=O 10.1021/jm201640m
44568291 192696 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 451 6 1 9 4.2 COc1ccc(-c2ccc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)cc2)cc1 10.1016/j.bmcl.2008.05.074
CHEMBL521438 192696 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 451 6 1 9 4.2 COc1ccc(-c2ccc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)cc2)cc1 10.1016/j.bmcl.2008.05.074
3284 3216 None 29 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1016/j.ejmech.2021.113907
44185871 3216 None 29 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1016/j.ejmech.2021.113907
5728 3216 None 29 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1016/j.ejmech.2021.113907
CHEMBL483688 3216 None 29 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1016/j.ejmech.2021.113907
56943867 164485 None 0 Rat Functional pKi = 9.2 9.2 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 489 6 1 12 1.5 COc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
CHEMBL4213177 164485 None 0 Rat Functional pKi = 9.2 9.2 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 489 6 1 12 1.5 COc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
9970832 7462 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 279 1 1 5 3.0 Nc1nc(-c2cccs2)c2c(n1)-c1ccccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1086846 7462 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 279 1 1 5 3.0 Nc1nc(-c2cccs2)c2c(n1)-c1ccccc1C2=O 10.1016/j.bmcl.2010.03.042
44568316 191409 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 436 5 1 9 3.9 Cc1ccc(-c2ccc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)cc2)cn1 10.1016/j.bmcl.2008.05.074
CHEMBL519111 191409 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 436 5 1 9 3.9 Cc1ccc(-c2ccc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)cc2)cn1 10.1016/j.bmcl.2008.05.074
10117987 3164 None 60 Human Functional pKi = 9.2 9.2 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1021/jm4011669
5614 3164 None 60 Human Functional pKi = 9.2 9.2 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1021/jm4011669
CHEMBL240624 3164 None 60 Human Functional pKi = 9.2 9.2 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1021/jm4011669
DB11864 3164 None 60 Human Functional pKi = 9.2 9.2 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1021/jm4011669
11380183 155081 None 0 Human Functional pKi = 9.2 9.2 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 269 3 1 6 1.9 CC(=O)Nc1cc(-n2cccn2)nc(-c2ccco2)n1 10.1021/jm4011669
CHEMBL401321 155081 None 0 Human Functional pKi = 9.2 9.2 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 269 3 1 6 1.9 CC(=O)Nc1cc(-n2cccn2)nc(-c2ccco2)n1 10.1021/jm4011669
56943869 164799 None 0 Rat Functional pKi = 9.2 9.2 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 474 5 1 12 1.1 Cc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)nc1 10.1021/acsmedchemlett.7b00175
CHEMBL4217235 164799 None 0 Rat Functional pKi = 9.2 9.2 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 474 5 1 12 1.1 Cc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)nc1 10.1021/acsmedchemlett.7b00175
56954336 82131 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 382 3 1 5 4.1 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(Cc3ccncc3F)ccc1C2=O 10.1021/jm201640m
CHEMBL2165800 82131 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 382 3 1 5 4.1 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(Cc3ccncc3F)ccc1C2=O 10.1021/jm201640m
10161974 93514 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 465 5 1 10 2.4 Nc1nc2c(ncn2CCN2CCN(c3ccc(F)cc3F)CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
CHEMBL246053 93514 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 465 5 1 10 2.4 Nc1nc2c(ncn2CCN2CCN(c3ccc(F)cc3F)CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
44216395 93515 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 502 9 1 11 3.2 COCCOc1ccc(C2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1016/j.bmcl.2006.12.104
CHEMBL246054 93515 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 502 9 1 11 3.2 COCCOc1ccc(C2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1016/j.bmcl.2006.12.104
10310635 179255 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 459 5 1 11 2.3 Nc1nc2c(cnn2CCN2CCc3ccc([N+](=O)[O-])cc3CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
CHEMBL472111 179255 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 459 5 1 11 2.3 Nc1nc2c(cnn2CCN2CCc3ccc([N+](=O)[O-])cc3CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
56943965 163758 None 0 Rat Functional pKi = 9.1 9.1 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 561 9 1 13 2.2 COCC(C)(C)Oc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
CHEMBL4204531 163758 None 0 Rat Functional pKi = 9.1 9.1 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 561 9 1 13 2.2 COCC(C)(C)Oc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
56943870 164873 None 0 Rat Functional pKi = 9.1 9.1 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 473 5 1 11 1.8 Cc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
CHEMBL4218105 164873 None 0 Rat Functional pKi = 9.1 9.1 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 473 5 1 11 1.8 Cc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
44216394 93470 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 521 9 1 12 2.3 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)c1 10.1016/j.bmcl.2006.12.104
CHEMBL245849 93470 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 521 9 1 12 2.3 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c(F)c1 10.1016/j.bmcl.2006.12.104
176407 4148 None 56 Human Functional pKi = 9.1 9.1 13 2
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm4011669
405 4148 None 56 Human Functional pKi = 9.1 9.1 13 2
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm4011669
CHEMBL113142 4148 None 56 Human Functional pKi = 9.1 9.1 13 2
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm4011669
DB08770 4148 None 56 Human Functional pKi = 9.1 9.1 13 2
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm4011669
56944354 164459 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 534 5 1 13 1.9 Cn1c(=O)n(CCN2CCN(c3nc(C(F)(F)F)cs3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
CHEMBL4212810 164459 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 534 5 1 13 1.9 Cn1c(=O)n(CCN2CCN(c3nc(C(F)(F)F)cs3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
44438087 93617 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 464 5 1 11 2.2 Nc1nc2c(ncn2CCN2CCN(c3ccc(Cl)cn3)CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
CHEMBL246467 93617 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 464 5 1 11 2.2 Nc1nc2c(ncn2CCN2CCN(c3ccc(Cl)cn3)CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
44438083 146485 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 446 5 1 9 3.3 Nc1nc2c(ncn2CCN2CCC(c3ccc(F)cc3)CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
CHEMBL392168 146485 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 446 5 1 9 3.3 Nc1nc2c(ncn2CCN2CCC(c3ccc(F)cc3)CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
10278807 150630 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1016/j.bmcl.2006.12.104
CHEMBL395472 150630 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1016/j.bmcl.2006.12.104
21363905 184000 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 423 5 1 10 3.0 Nc1nc2c(cnn2CCc2ccc(-c3cnccn3)cc2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.074
CHEMBL481132 184000 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 423 5 1 10 3.0 Nc1nc2c(cnn2CCc2ccc(-c3cnccn3)cc2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.074
46888823 9016 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 393 5 2 6 4.0 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(NCCc3ccncc3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1098458 9016 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 393 5 2 6 4.0 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(NCCc3ccncc3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
46888824 9053 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 393 5 2 6 4.0 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(NCCc3ccccn3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1098765 9053 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 393 5 2 6 4.0 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(NCCc3ccccn3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
10278807 150630 None 0 Human Functional pKi = 9.1 9.1 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/jm4011669
CHEMBL395472 150630 None 0 Human Functional pKi = 9.1 9.1 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/jm4011669
137654317 158996 None 0 Human Functional pKi = 9.0 9.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 445 6 1 7 4.1 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3cccc(F)c3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4095424 158996 None 0 Human Functional pKi = 9.0 9.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 445 6 1 7 4.1 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3cccc(F)c3)nc12 10.1021/acs.jmedchem.6b01584
54582022 60993 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 317 3 1 6 2.2 Nc1nc(-c2ccccc2)cc2nn(Cc3ccccc3)c(=O)n12 10.1016/j.bmcl.2011.02.045
CHEMBL1762506 60993 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 317 3 1 6 2.2 Nc1nc(-c2ccccc2)cc2nn(Cc3ccccc3)c(=O)n12 10.1016/j.bmcl.2011.02.045
46889098 7642 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 387 4 2 7 2.3 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CNN3CCOCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1088247 7642 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 387 4 2 7 2.3 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CNN3CCOCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.042
10203891 146488 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 444 5 1 11 1.8 Cc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)nc1 10.1016/j.bmcl.2006.12.104
CHEMBL392169 146488 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 444 5 1 11 1.8 Cc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccco5)nc43)CC2)nc1 10.1016/j.bmcl.2006.12.104
137644817 158201 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 463 6 1 7 4.2 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3c(F)cccc3F)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4086751 158201 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 463 6 1 7 4.2 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3c(F)cccc3F)nc12 10.1021/acs.jmedchem.6b01584
56944733 164838 None 0 Rat Functional pKi = 9.0 9.0 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 525 7 1 12 2.0 Cn1c(=O)n(CCN2CCN(c3ccc(OC(F)F)cc3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
CHEMBL4217668 164838 None 0 Rat Functional pKi = 9.0 9.0 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 525 7 1 12 2.0 Cn1c(=O)n(CCN2CCN(c3ccc(OC(F)F)cc3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
56943870 164873 None 0 Human Functional pKi = 9.0 9.0 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 473 5 1 11 1.8 Cc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
CHEMBL4218105 164873 None 0 Human Functional pKi = 9.0 9.0 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 473 5 1 11 1.8 Cc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
10152242 179256 None 0 Human Functional pKi = 9.0 9.0 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 492 4 1 9 3.2 Nc1nc2c(cnn2CCN2CCc3ccc(Br)cc3CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
CHEMBL472112 179256 None 0 Human Functional pKi = 9.0 9.0 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 492 4 1 9 3.2 Nc1nc2c(cnn2CCN2CCc3ccc(Br)cc3CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
44568290 184127 None 0 Human Functional pKi = 9.0 9.0 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 421 5 1 8 4.2 Nc1nc2c(cnn2CCc2ccc(-c3ccccc3)cc2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.074
CHEMBL482078 184127 None 0 Human Functional pKi = 9.0 9.0 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 421 5 1 8 4.2 Nc1nc2c(cnn2CCc2ccc(-c3ccccc3)cc2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.074
137661874 159396 None 0 Human Functional pKi = 9.0 9.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 405 4 2 7 3.0 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(O)CC3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4099688 159396 None 0 Human Functional pKi = 9.0 9.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 405 4 2 7 3.0 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(O)CC3)nc12 10.1021/acs.jmedchem.6b01584
137661874 159396 None 0 Human Functional pKi = 9.0 9.0 - 0
Antagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assayAntagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assay
ChEMBL 405 4 2 7 3.0 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(O)CC3)nc12 10.1016/j.ejmech.2021.113907
CHEMBL4099688 159396 None 0 Human Functional pKi = 9.0 9.0 - 0
Antagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assayAntagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assay
ChEMBL 405 4 2 7 3.0 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(O)CC3)nc12 10.1016/j.ejmech.2021.113907
10117987 3164 None 60 Human Functional pKi = 9.0 9.0 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1021/jm4011669
5614 3164 None 60 Human Functional pKi = 9.0 9.0 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1021/jm4011669
CHEMBL240624 3164 None 60 Human Functional pKi = 9.0 9.0 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1021/jm4011669
DB11864 3164 None 60 Human Functional pKi = 9.0 9.0 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 10.1021/jm4011669
176408 3557 None 55 Human Functional pKi = 9.0 9.0 - 1
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/jm4011669
403 3557 None 55 Human Functional pKi = 9.0 9.0 - 1
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/jm4011669
431 3557 None 55 Human Functional pKi = 9.0 9.0 - 1
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/jm4011669
CHEMBL17127 3557 None 55 Human Functional pKi = 9.0 9.0 - 1
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/jm4011669
9949541 96345 None 0 Human Functional pKi = 9.0 9.0 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 334 3 2 7 2.4 Nc1nc(-c2ccco2)c2ncn(C(=O)NCc3ccccc3)c2n1 10.1021/jm4011669
CHEMBL261203 96345 None 0 Human Functional pKi = 9.0 9.0 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 334 3 2 7 2.4 Nc1nc(-c2ccco2)c2ncn(C(=O)NCc3ccccc3)c2n1 10.1021/jm4011669
56944263 164408 None 0 Rat Functional pKi = 8.9 8.9 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 484 5 1 12 1.3 Cn1c(=O)n(CCN2CCN(c3ccc(C#N)cc3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
CHEMBL4212278 164408 None 0 Rat Functional pKi = 8.9 8.9 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 484 5 1 12 1.3 Cn1c(=O)n(CCN2CCN(c3ccc(C#N)cc3)CC2)c2nc(N)n3nc(-c4ccco4)nc3c21 10.1021/acsmedchemlett.7b00175
56944063 163808 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 569 9 1 13 1.7 COCCOc1cc(F)c(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1F 10.1021/acsmedchemlett.7b00175
CHEMBL4205030 163808 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 569 9 1 13 1.7 COCCOc1cc(F)c(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1F 10.1021/acsmedchemlett.7b00175
56943872 164104 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 550 9 1 14 1.3 COCCOc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5nccs5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
CHEMBL4208426 164104 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 550 9 1 14 1.3 COCCOc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5nccs5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
21874557 3996 None 45 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1016/j.ejmech.2021.113907
5612 3996 None 45 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1016/j.ejmech.2021.113907
CHEMBL447664 3996 None 45 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1016/j.ejmech.2021.113907
DB06625 3996 None 45 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1016/j.ejmech.2021.113907
56954335 82129 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 382 3 1 5 4.1 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(Cc3cncc(F)c3)ccc1C2=O 10.1021/jm201640m
CHEMBL2165799 82129 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 382 3 1 5 4.1 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(Cc3cncc(F)c3)ccc1C2=O 10.1021/jm201640m
44568402 189963 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 509 6 1 11 3.5 CC(c1ccc2cc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)ccc2n1)N1CCOCC1 10.1016/j.bmcl.2008.05.074
CHEMBL516753 189963 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 509 6 1 11 3.5 CC(c1ccc2cc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)ccc2n1)N1CCOCC1 10.1016/j.bmcl.2008.05.074
21874557 3996 None 45 Human Functional pKi = 8.9 8.9 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm4011669
5612 3996 None 45 Human Functional pKi = 8.9 8.9 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm4011669
CHEMBL447664 3996 None 45 Human Functional pKi = 8.9 8.9 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm4011669
DB06625 3996 None 45 Human Functional pKi = 8.9 8.9 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm4011669
56954334 82139 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 389 3 1 6 3.8 N#Cc1cncc(Cc2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)c1 10.1021/jm201640m
CHEMBL2165808 82139 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 389 3 1 6 3.8 N#Cc1cncc(Cc2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)c1 10.1021/jm201640m
10114735 93558 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 449 5 1 12 1.1 Nc1nc2c(ncn2CCN2CCN(c3ncc(F)cn3)CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
CHEMBL246262 93558 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 449 5 1 12 1.1 Nc1nc2c(ncn2CCN2CCN(c3ncc(F)cn3)CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
45275287 89786 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 376 3 1 5 5.1 N#Cc1cccc(-c2nc(N)c3cc(Cc4ccccc4Cl)sc3n2)c1 10.1016/j.bmcl.2013.02.078
CHEMBL2377092 89786 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 376 3 1 5 5.1 N#Cc1cccc(-c2nc(N)c3cc(Cc4ccccc4Cl)sc3n2)c1 10.1016/j.bmcl.2013.02.078
9860013 157075 None 0 Human Functional pKi = 8.9 8.9 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 261 2 0 5 3.9 CC(C)c1nc(-c2nccs2)c2sccc2n1 10.1021/jm4011669
CHEMBL407307 157075 None 0 Human Functional pKi = 8.9 8.9 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 261 2 0 5 3.9 CC(C)c1nc(-c2nccs2)c2sccc2n1 10.1021/jm4011669
11154 217 None 41 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 426 5 2 9 2.8 N#Cc1cccc(c1C)c1nc(N)nc(c1)c1nnn(c1)Cc1cccc(n1)C(O)(C)C 10.1016/j.ejmech.2021.113907
135242184 217 None 41 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 426 5 2 9 2.8 N#Cc1cccc(c1C)c1nc(N)nc(c1)c1nnn(c1)Cc1cccc(n1)C(O)(C)C 10.1016/j.ejmech.2021.113907
135242184.0 217 None 41 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 426 5 2 9 2.8 N#Cc1cccc(c1C)c1nc(N)nc(c1)c1nnn(c1)Cc1cccc(n1)C(O)(C)C 10.1016/j.ejmech.2021.113907
CHEMBL4740383 217 None 41 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 426 5 2 9 2.8 N#Cc1cccc(c1C)c1nc(N)nc(c1)c1nnn(c1)Cc1cccc(n1)C(O)(C)C 10.1016/j.ejmech.2021.113907
145964038 164173 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 547 9 1 13 1.9 COCC(C)Oc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
CHEMBL4209408 164173 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 547 9 1 13 1.9 COCC(C)Oc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
44438077 93429 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 331 3 1 8 2.4 Nc1nc2c(ncn2Cc2ccccc2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
CHEMBL245645 93429 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 331 3 1 8 2.4 Nc1nc2c(ncn2Cc2ccccc2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
44568375 184003 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 498 9 1 11 3.8 COCCOC(C)c1ccc2cc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)ccc2n1 10.1016/j.bmcl.2008.05.074
CHEMBL481146 184003 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 498 9 1 11 3.8 COCCOC(C)c1ccc2cc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)ccc2n1 10.1016/j.bmcl.2008.05.074
44560507 189404 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 474 8 1 11 2.4 COCCOc1cccc2c1CN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1016/j.bmcl.2008.05.069
CHEMBL512133 189404 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 474 8 1 11 2.4 COCCOc1cccc2c1CN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1016/j.bmcl.2008.05.069
21363898 191878 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 422 5 1 9 3.6 Nc1nc2c(cnn2CCc2ccc(-c3cccnc3)cc2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.074
CHEMBL519784 191878 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 422 5 1 9 3.6 Nc1nc2c(cnn2CCc2ccc(-c3cccnc3)cc2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.074
17035750 7476 None 7 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 303 2 1 5 2.9 COc1cccc(-c2nc(N)nc3c2C(=O)c2ccccc2-3)c1 10.1016/j.bmcl.2010.03.042
CHEMBL1086978 7476 None 7 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 303 2 1 5 2.9 COc1cccc(-c2nc(N)nc3c2C(=O)c2ccccc2-3)c1 10.1016/j.bmcl.2010.03.042
176407 4148 None 56 Human Functional pKi = 8.8 8.8 13 2
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2017.12.007
176407 4148 None 56 Human Functional pKi = 8.8 8.8 13 2
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2021.113907
405 4148 None 56 Human Functional pKi = 8.8 8.8 13 2
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2017.12.007
405 4148 None 56 Human Functional pKi = 8.8 8.8 13 2
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2021.113907
CHEMBL113142 4148 None 56 Human Functional pKi = 8.8 8.8 13 2
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2017.12.007
CHEMBL113142 4148 None 56 Human Functional pKi = 8.8 8.8 13 2
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2021.113907
DB08770 4148 None 56 Human Functional pKi = 8.8 8.8 13 2
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2017.12.007
DB08770 4148 None 56 Human Functional pKi = 8.8 8.8 13 2
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2021.113907
56954254 82134 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 400 3 1 5 4.5 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(C(F)(F)c3cccnc3)ccc1C2=O 10.1021/jm201640m
CHEMBL2165803 82134 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 400 3 1 5 4.5 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(C(F)(F)c3cccnc3)ccc1C2=O 10.1021/jm201640m
10195616 179022 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 479 4 1 10 2.5 Nc1nc2c(cnn2CCN2CCc3ncc(Br)cc3C2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
CHEMBL470088 179022 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 479 4 1 10 2.5 Nc1nc2c(cnn2CCN2CCc3ncc(Br)cc3C2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
44568401 184133 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 509 5 1 11 2.6 Nc1nc2c(cnn2CCc2ccc3nc(C(=O)N4CCOCC4)ccc3c2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.074
CHEMBL482138 184133 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 509 5 1 11 2.6 Nc1nc2c(cnn2CCc2ccc3nc(C(=O)N4CCOCC4)ccc3c2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.074
176407 4148 None 56 Human Functional pKi = 8.8 8.8 13 2
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.bmcl.2013.03.070
405 4148 None 56 Human Functional pKi = 8.8 8.8 13 2
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.bmcl.2013.03.070
CHEMBL113142 4148 None 56 Human Functional pKi = 8.8 8.8 13 2
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.bmcl.2013.03.070
DB08770 4148 None 56 Human Functional pKi = 8.8 8.8 13 2
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.bmcl.2013.03.070
11153 2008 None 42 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 10.1016/j.ejmech.2021.113907
86676119 2008 None 42 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 10.1016/j.ejmech.2021.113907
CHEMBL4594442 2008 None 42 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 10.1016/j.ejmech.2021.113907
DB16192 2008 None 42 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 10.1016/j.ejmech.2021.113907
44438079 93468 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 365 3 1 8 3.0 Nc1nc2c(ncn2Cc2ccccc2Cl)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
CHEMBL245847 93468 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 365 3 1 8 3.0 Nc1nc2c(ncn2Cc2ccccc2Cl)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
44438086 93559 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 436 5 1 12 1.6 Nc1nc2c(ncn2CCN2CCN(c3nccs3)CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
CHEMBL246263 93559 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 436 5 1 12 1.6 Nc1nc2c(ncn2CCN2CCN(c3nccs3)CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
44438076 93994 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 429 5 1 10 2.1 Nc1nc2c(ncn2CCN2CCN(c3ccccc3)CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
CHEMBL248300 93994 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 429 5 1 10 2.1 Nc1nc2c(ncn2CCN2CCN(c3ccccc3)CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
9923269 96083 None 0 Human Functional pKi = 8.8 8.8 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 324 3 2 8 2.0 Nc1nc(-c2ccco2)c2ncn(C(=O)NCc3ccco3)c2n1 10.1021/jm4011669
CHEMBL259832 96083 None 0 Human Functional pKi = 8.8 8.8 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 324 3 2 8 2.0 Nc1nc(-c2ccco2)c2ncn(C(=O)NCc3ccco3)c2n1 10.1021/jm4011669
11739282 199114 None 0 Human Functional pKi = 8.8 8.8 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 339 6 2 7 1.8 COCc1cccc(CNC(=O)c2cc(-c3ccco3)nc(N)n2)n1 10.1021/jm4011669
CHEMBL564473 199114 None 0 Human Functional pKi = 8.8 8.8 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 339 6 2 7 1.8 COCc1cccc(CNC(=O)c2cc(-c3ccco3)nc(N)n2)n1 10.1021/jm4011669
24810000 82135 None 13 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 324 3 1 5 3.3 CC(C)n1cc(-c2ncc(N)nc2-c2ccc(F)cc2)ccc1=O 10.1021/jm201640m
CHEMBL2165804 82135 None 13 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 324 3 1 5 3.3 CC(C)n1cc(-c2ncc(N)nc2-c2ccc(F)cc2)ccc1=O 10.1021/jm201640m
44568403 183478 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 481 5 1 11 2.9 Nc1nc2c(cnn2CCc2ccc3nc(N4CCOCC4)ccc3c2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.074
CHEMBL479784 183478 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 481 5 1 11 2.9 Nc1nc2c(cnn2CCc2ccc3nc(N4CCOCC4)ccc3c2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.074
137654513 158908 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 487 8 1 9 4.0 COc1ccc(OC(C)(C)C(=O)Nc2nc3c(OC)ccc(N4CCOCC4)c3s2)cc1OC 10.1021/acs.jmedchem.6b01584
CHEMBL4094491 158908 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 487 8 1 9 4.0 COc1ccc(OC(C)(C)C(=O)Nc2nc3c(OC)ccc(N4CCOCC4)c3s2)cc1OC 10.1021/acs.jmedchem.6b01584
24810000 82135 None 13 Human Functional pKi = 8.7 8.7 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 324 3 1 5 3.3 CC(C)n1cc(-c2ncc(N)nc2-c2ccc(F)cc2)ccc1=O 10.1021/jm4011669
CHEMBL2165804 82135 None 13 Human Functional pKi = 8.7 8.7 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 324 3 1 5 3.3 CC(C)n1cc(-c2ncc(N)nc2-c2ccc(F)cc2)ccc1=O 10.1021/jm4011669
20770622 184174 None 0 Human Functional pKi = 8.7 8.7 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 489 6 1 9 2.8 CN(CCN1CCN(c2ccc(F)cc2F)CC1)c1cc2nc(-c3cccc(C#N)c3)nn2c(N)n1 10.1021/jm4011669
CHEMBL482329 184174 None 0 Human Functional pKi = 8.7 8.7 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 489 6 1 9 2.8 CN(CCN1CCN(c2ccc(F)cc2F)CC1)c1cc2nc(-c3cccc(C#N)c3)nn2c(N)n1 10.1021/jm4011669
10288204 179001 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 441 5 1 10 2.6 Nc1nc2c(cnn2CCN2CCc3ncc(C4CC4)cc3C2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
CHEMBL469893 179001 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 441 5 1 10 2.6 Nc1nc2c(cnn2CCN2CCc3ncc(C4CC4)cc3C2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
10288740 179021 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 474 6 1 11 2.8 COc1cc2c(cc1OC)CN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)C(C)C2 10.1016/j.bmcl.2008.05.069
CHEMBL470087 179021 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 474 6 1 11 2.8 COc1cc2c(cc1OC)CN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)C(C)C2 10.1016/j.bmcl.2008.05.069
9955121 179257 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 444 5 1 10 2.4 COc1ccc2c(c1)CCN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1016/j.bmcl.2008.05.069
CHEMBL472114 179257 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 444 5 1 10 2.4 COc1ccc2c(c1)CCN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1016/j.bmcl.2008.05.069
44568315 184083 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 452 6 1 10 3.6 COc1ccc(-c2ccc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)cc2)cn1 10.1016/j.bmcl.2008.05.074
CHEMBL481771 184083 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 452 6 1 10 3.6 COc1ccc(-c2ccc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)cc2)cn1 10.1016/j.bmcl.2008.05.074
449 2643 None 38 Human Functional pKi = 8.7 8.7 -36 4
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2021.113907
453 2643 None 38 Human Functional pKi = 8.7 8.7 -36 4
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2021.113907
6603931 2643 None 38 Human Functional pKi = 8.7 8.7 -36 4
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2021.113907
CHEMBL273807 2643 None 38 Human Functional pKi = 8.7 8.7 -36 4
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2021.113907
44438091 93912 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 581 9 1 11 3.6 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccccc5C(F)(F)F)nc43)CC2)cc1 10.1016/j.bmcl.2006.12.104
CHEMBL247900 93912 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 581 9 1 11 3.6 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccccc5C(F)(F)F)nc43)CC2)cc1 10.1016/j.bmcl.2006.12.104
45278944 109651 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 332 3 1 6 3.6 Nc1nc(-c2ccc(Cl)o2)nc2sc(CN3CC=CC3)cc12 10.1039/C1MD00082A
CHEMBL3222085 109651 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 332 3 1 6 3.6 Nc1nc(-c2ccc(Cl)o2)nc2sc(CN3CC=CC3)cc12 10.1039/C1MD00082A
10455114 60385 None 0 Rat Functional pKi = 8 8.0 - 0
Antagonist activity at rat adenosine A2A receptorAntagonist activity at rat adenosine A2A receptor
ChEMBL 425 6 2 10 2.5 Nc1nc(NC[C@H]2CCCN2Cc2ccnc(Cl)c2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2022.114378
CHEMBL174628 60385 None 0 Rat Functional pKi = 8 8.0 - 0
Antagonist activity at rat adenosine A2A receptorAntagonist activity at rat adenosine A2A receptor
ChEMBL 425 6 2 10 2.5 Nc1nc(NC[C@H]2CCCN2Cc2ccnc(Cl)c2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2022.114378
46888881 8569 None 0 Human Functional pKi = 8 8.0 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 385 2 1 6 3.1 CN1CCCN(c2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
CHEMBL1094548 8569 None 0 Human Functional pKi = 8 8.0 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 385 2 1 6 3.1 CN1CCCN(c2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
45279824 109634 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 318 3 1 6 3.1 Nc1nc(-c2ccco2)nc2sc(CN3CCC(F)C3)cc12 10.1039/C1MD00082A
CHEMBL3222067 109634 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 318 3 1 6 3.1 Nc1nc(-c2ccco2)nc2sc(CN3CCC(F)C3)cc12 10.1039/C1MD00082A
44217687 61020 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 505 6 1 11 0.1 CS(=O)(=O)N1CCN(CCn2ncc3c2nc(N)n2c(=O)n(Cc4cccc(Cl)c4)nc32)CC1 10.1016/j.bmcl.2011.02.045
CHEMBL1762629 61020 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 505 6 1 11 0.1 CS(=O)(=O)N1CCN(CCn2ncc3c2nc(N)n2c(=O)n(Cc4cccc(Cl)c4)nc32)CC1 10.1016/j.bmcl.2011.02.045
46888890 8890 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 363 5 1 7 2.5 CN(C)CCN(C)c1ccc(-c2nc(N)nc3c2C(=O)c2ccccc2-3)o1 10.1016/j.bmcl.2010.03.042
CHEMBL1097495 8890 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 363 5 1 7 2.5 CN(C)CCN(C)c1ccc(-c2nc(N)nc3c2C(=O)c2ccccc2-3)o1 10.1016/j.bmcl.2010.03.042
11386134 67490 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 482 4 1 11 2.1 Cn1nc(C(F)(F)F)c(CN2CCN(c3nc(N)n4nc(-c5ccco5)nc4n3)CC2)c1Cl 10.1016/j.ejmech.2022.114378
CHEMBL189192 67490 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 482 4 1 11 2.1 Cn1nc(C(F)(F)F)c(CN2CCN(c3nc(N)n4nc(-c5ccco5)nc4n3)CC2)c1Cl 10.1016/j.ejmech.2022.114378
45275818 89825 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 352 3 1 6 4.9 Cc1csc(-c2nc(N)c3cc(C(C)c4ccccc4)sc3n2)n1 10.1016/j.bmcl.2013.02.078
CHEMBL2377234 89825 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 352 3 1 6 4.9 Cc1csc(-c2nc(N)c3cc(C(C)c4ccccc4)sc3n2)n1 10.1016/j.bmcl.2013.02.078
848601 9220 None 9 Guinea pig Functional pKi = 6 6.0 - 1
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 272 1 2 6 0.3 Cn1c(=O)c2nc(-c3cccc(O)c3)[nH]c2n(C)c1=O 10.1021/jm00382a018
CHEMBL11054 9220 None 9 Guinea pig Functional pKi = 6 6.0 - 1
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 272 1 2 6 0.3 Cn1c(=O)c2nc(-c3cccc(O)c3)[nH]c2n(C)c1=O 10.1021/jm00382a018
92411 98196 None 2 Guinea pig Functional pKi = 6 6.0 - 1
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 361 5 2 6 2.6 CCCn1c(=O)c2nc(-c3ccc(Cl)cc3N)[nH]c2n(CCC)c1=O 10.1021/jm00382a018
CHEMBL273671 98196 None 2 Guinea pig Functional pKi = 6 6.0 - 1
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 361 5 2 6 2.6 CCCn1c(=O)c2nc(-c3ccc(Cl)cc3N)[nH]c2n(CCC)c1=O 10.1021/jm00382a018
101446 92365 None 18 Guinea pig Functional pKi = 5 5.0 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 220 2 0 6 -0.4 C=CCn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00157a035
CHEMBL24289 92365 None 18 Guinea pig Functional pKi = 5 5.0 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 220 2 0 6 -0.4 C=CCn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00157a035
45279360 109662 None 0 Human Functional pKi = 6 6.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 317 3 1 8 1.8 Nc1nc(-c2ccon2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
CHEMBL3222096 109662 None 0 Human Functional pKi = 6 6.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 317 3 1 8 1.8 Nc1nc(-c2ccon2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
45275171 89792 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 385 3 1 4 5.6 Nc1nc(-c2cccc(C(F)(F)F)c2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
CHEMBL2377098 89792 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 385 3 1 4 5.6 Nc1nc(-c2cccc(C(F)(F)F)c2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
45278699 109297 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 367 3 1 6 3.7 N#Cc1ccccc1-c1nc(N)c2cc(CN3CCC(F)CC3)sc2n1 10.1039/C1MD00082A
CHEMBL3217869 109297 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 367 3 1 6 3.7 N#Cc1ccccc1-c1nc(N)c2cc(CN3CCC(F)CC3)sc2n1 10.1039/C1MD00082A
14539598 118436 None 0 Rat Functional pKi = 5.0 5.0 - 0
Agonistic activity against Adenosine A2A receptor on rat striatal membranesAgonistic activity against Adenosine A2A receptor on rat striatal membranes
ChEMBL 504 7 5 10 2.9 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc5ccccc45)nc(NC4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/s0960-894x(00)00017-2
CHEMBL341031 118436 None 0 Rat Functional pKi = 5.0 5.0 - 0
Agonistic activity against Adenosine A2A receptor on rat striatal membranesAgonistic activity against Adenosine A2A receptor on rat striatal membranes
ChEMBL 504 7 5 10 2.9 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc5ccccc45)nc(NC4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/s0960-894x(00)00017-2
45275713 89827 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 364 3 1 6 4.8 Cc1csc(-c2nc(N)c3cc(C4(c5ccccc5)CC4)sc3n2)n1 10.1016/j.bmcl.2013.02.078
CHEMBL2377236 89827 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 364 3 1 6 4.8 Cc1csc(-c2nc(N)c3cc(C4(c5ccccc5)CC4)sc3n2)n1 10.1016/j.bmcl.2013.02.078
90665312 109302 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 376 3 1 5 4.3 Nc1nc(-c2cccc(C(F)(F)F)c2)nc2sc(CN3CC=CC3)cc12 10.1039/C1MD00082A
CHEMBL3217873 109302 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 376 3 1 5 4.3 Nc1nc(-c2cccc(C(F)(F)F)c2)nc2sc(CN3CC=CC3)cc12 10.1039/C1MD00082A
59277997 89828 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 231 1 1 5 2.8 Cc1ccc(-c2nc(N)c3ccsc3n2)o1 10.1016/j.bmcl.2013.02.078
CHEMBL2377237 89828 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 231 1 1 5 2.8 Cc1ccc(-c2nc(N)c3ccsc3n2)o1 10.1016/j.bmcl.2013.02.078
44217688 61016 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 484 5 1 11 1.4 Nc1nc2c(cnn2CCN2CCC3(CC2)OCCO3)c2nn(Cc3cccc(Cl)c3)c(=O)n12 10.1016/j.bmcl.2011.02.045
CHEMBL1762625 61016 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 484 5 1 11 1.4 Nc1nc2c(cnn2CCN2CCC3(CC2)OCCO3)c2nn(Cc3cccc(Cl)c3)c(=O)n12 10.1016/j.bmcl.2011.02.045
11618368 3847 None 50 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1016/j.ejmech.2022.114378
5611 3847 None 50 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1016/j.ejmech.2022.114378
CHEMBL2105747 3847 None 50 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1016/j.ejmech.2022.114378
DB12203 3847 None 50 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1016/j.ejmech.2022.114378
45278868 109650 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 346 3 1 6 3.9 Nc1nc(-c2ccc(Cl)o2)nc2sc(CN3CC=CCC3)cc12 10.1039/C1MD00082A
CHEMBL3222084 109650 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 346 3 1 6 3.9 Nc1nc(-c2ccc(Cl)o2)nc2sc(CN3CC=CCC3)cc12 10.1039/C1MD00082A
45275715 89803 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 351 4 1 6 4.4 COc1ccccc1Cc1cc2c(N)nc(-c3ccc(C)o3)nc2s1 10.1016/j.bmcl.2013.02.078
CHEMBL2377109 89803 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 351 4 1 6 4.4 COc1ccccc1Cc1cc2c(N)nc(-c3ccc(C)o3)nc2s1 10.1016/j.bmcl.2013.02.078
45275517 89830 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 321 3 1 5 4.4 Cc1ccc(-c2nc(N)c3cc(Cc4ccccc4)sc3n2)o1 10.1016/j.bmcl.2013.02.078
CHEMBL2377239 89830 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 321 3 1 5 4.4 Cc1ccc(-c2nc(N)c3cc(Cc4ccccc4)sc3n2)o1 10.1016/j.bmcl.2013.02.078
56943872 164104 None 0 Rat Functional pKi = 8.0 8.0 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 550 9 1 14 1.3 COCCOc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5nccs5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
CHEMBL4208426 164104 None 0 Rat Functional pKi = 8.0 8.0 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 550 9 1 14 1.3 COCCOc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5nccs5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
46889228 7446 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 417 2 1 6 2.5 CN1CCN(C(=O)c2ccc3c(c2)-c2nc(N)nc(-c4ccc(F)cc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
CHEMBL1086697 7446 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 417 2 1 6 2.5 CN1CCN(C(=O)c2ccc3c(c2)-c2nc(N)nc(-c4ccc(F)cc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
46888991 7567 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 385 3 1 6 2.7 CN1CCN(Cc2cccc3c2-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.042
CHEMBL1087702 7567 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 385 3 1 6 2.7 CN1CCN(Cc2cccc3c2-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.042
46889043 7571 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 384 3 1 5 4.3 CC1CCC(C)N1Cc1cccc2c1-c1nc(N)nc(-c3ccccc3)c1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1087711 7571 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 384 3 1 5 4.3 CC1CCC(C)N1Cc1cccc2c1-c1nc(N)nc(-c3ccccc3)c1C2=O 10.1016/j.bmcl.2010.03.042
44568345 184163 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 423 5 1 10 3.0 Nc1nc2c(cnn2CCc2ccc(-c3cccnc3)cn2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.074
CHEMBL482283 184163 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 423 5 1 10 3.0 Nc1nc2c(cnn2CCc2ccc(-c3cccnc3)cn2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.074
45275056 89784 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 342 3 1 5 4.4 N#Cc1cccc(-c2nc(N)c3cc(Cc4ccccc4)sc3n2)c1 10.1016/j.bmcl.2013.02.078
CHEMBL2377090 89784 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 342 3 1 5 4.4 N#Cc1cccc(-c2nc(N)c3cc(Cc4ccccc4)sc3n2)c1 10.1016/j.bmcl.2013.02.078
46861782 8527 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 385 3 1 6 3.1 CCN1CCN(c2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
CHEMBL1094244 8527 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 385 3 1 6 3.1 CCN1CCN(c2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
122071 165381 None 4 Guinea pig Functional pKi = 7.0 7.0 - 0
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 356 6 2 6 2.1 CCCn1c(=O)c2nc(-c3ccc(C(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm00382a018
CHEMBL423239 165381 None 4 Guinea pig Functional pKi = 7.0 7.0 - 0
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 356 6 2 6 2.1 CCCn1c(=O)c2nc(-c3ccc(C(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm00382a018
59276711 109640 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 382 4 1 6 5.2 C[C@H]1CCC[C@@H](C)N1Cc1cc2c(N)nc(-c3ccc(C4CC4)o3)nc2s1 10.1039/C1MD00082A
CHEMBL3222074 109640 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 382 4 1 6 5.2 C[C@H]1CCC[C@@H](C)N1Cc1cc2c(N)nc(-c3ccc(C4CC4)o3)nc2s1 10.1039/C1MD00082A
45279543 109664 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 316 3 1 6 3.6 Nc1nc(-c2cccs2)nc2sc(CN3CCCC3)cc12 10.1039/C1MD00082A
CHEMBL3222098 109664 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 316 3 1 6 3.6 Nc1nc(-c2cccs2)nc2sc(CN3CCCC3)cc12 10.1039/C1MD00082A
45278537 109670 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 344 3 1 6 2.9 Nc1nc(-c2cccc(F)c2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
CHEMBL3222104 109670 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 344 3 1 6 2.9 Nc1nc(-c2cccc(F)c2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
44459940 96433 None 0 Guinea pig Functional pKi = 5.0 5.0 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 264 4 0 6 1.0 CCCn1cnc2c1c(=O)n(C)c(=O)n2CC(C)C 10.1021/jm00157a035
CHEMBL26176 96433 None 0 Guinea pig Functional pKi = 5.0 5.0 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 264 4 0 6 1.0 CCCn1cnc2c1c(=O)n(C)c(=O)n2CC(C)C 10.1021/jm00157a035
847168 96813 None 22 Guinea pig Functional pKi = 5.0 5.0 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 222 2 0 6 -0.2 CCCn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00157a035
CHEMBL26455 96813 None 22 Guinea pig Functional pKi = 5.0 5.0 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 222 2 0 6 -0.2 CCCn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00157a035
3041753 96986 None 4 Guinea pig Functional pKi = 5.0 5.0 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 312 4 0 6 1.6 CC(C)Cn1c(=O)n(C)c(=O)c2c1ncn2Cc1ccccc1 10.1021/jm00157a035
CHEMBL26606 96986 None 4 Guinea pig Functional pKi = 5.0 5.0 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 312 4 0 6 1.6 CC(C)Cn1c(=O)n(C)c(=O)c2c1ncn2Cc1ccccc1 10.1021/jm00157a035
3287 2642 None 33 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1016/j.ejmech.2010.04.039
5139184 2642 None 33 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1016/j.ejmech.2010.04.039
CHEMBL17002 2642 None 33 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1016/j.ejmech.2010.04.039
3287 2642 None 33 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1021/jm990421v
5139184 2642 None 33 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1021/jm990421v
CHEMBL17002 2642 None 33 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1021/jm990421v
78268 27793 None 42 Human Functional pKi = 6.9 6.9 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 248 2 1 4 2.8 Nc1nnc(-c2ccccc2)c(-c2ccccc2)n1 10.1021/jm4011669
CHEMBL1370747 27793 None 42 Human Functional pKi = 6.9 6.9 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 248 2 1 4 2.8 Nc1nnc(-c2ccccc2)c(-c2ccccc2)n1 10.1021/jm4011669
46888924 7489 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 404 5 1 6 3.6 Nc1nc(-c2ccc(F)cc2)c2c(n1)-c1cc(OCCN3CCCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1087081 7489 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 404 5 1 6 3.6 Nc1nc(-c2ccc(F)cc2)c2c(n1)-c1cc(OCCN3CCCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
45275172 89793 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 347 4 1 5 4.5 COc1cccc(-c2nc(N)c3cc(Cc4ccccc4)sc3n2)c1 10.1016/j.bmcl.2013.02.078
CHEMBL2377099 89793 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 347 4 1 5 4.5 COc1cccc(-c2nc(N)c3cc(Cc4ccccc4)sc3n2)c1 10.1016/j.bmcl.2013.02.078
10839296 58160 None 1 Rat Functional pKi = 5.9 5.9 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 506 10 2 9 3.3 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc([N+](=O)[O-])cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16787 58160 None 1 Rat Functional pKi = 5.9 5.9 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 506 10 2 9 3.3 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc([N+](=O)[O-])cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
4882 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.ejmech.2017.12.007
4882 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.ejmech.2021.113907
5311037 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.ejmech.2017.12.007
5311037 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.ejmech.2021.113907
5311037.0 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.ejmech.2017.12.007
5311037.0 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.ejmech.2021.113907
5608 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.ejmech.2017.12.007
5608 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.ejmech.2021.113907
CHEMBL431770 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.ejmech.2017.12.007
CHEMBL431770 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.ejmech.2021.113907
DB11757 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.ejmech.2017.12.007
DB11757 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.ejmech.2021.113907
4882 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
5311037 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
5311037.0 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
5608 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
CHEMBL431770 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
DB11757 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1016/j.bmcl.2013.03.070
52943351 18321 None 0 Rat Functional pKi = 7.9 7.9 - 0
Antagonist activity at rat A2A receptor by cAMP functional assayAntagonist activity at rat A2A receptor by cAMP functional assay
ChEMBL 434 8 1 7 3.1 COCCCn1c(NC(=O)c2cccc(C#N)c2)nc2cc(C(=O)N(C)C(C)C)cnc21 10.1016/j.bmcl.2010.08.064
CHEMBL1270709 18321 None 0 Rat Functional pKi = 7.9 7.9 - 0
Antagonist activity at rat A2A receptor by cAMP functional assayAntagonist activity at rat A2A receptor by cAMP functional assay
ChEMBL 434 8 1 7 3.1 COCCCn1c(NC(=O)c2cccc(C#N)c2)nc2cc(C(=O)N(C)C(C)C)cnc21 10.1016/j.bmcl.2010.08.064
4882 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/jm4011669
5311037 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/jm4011669
5311037.0 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/jm4011669
5608 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/jm4011669
CHEMBL431770 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/jm4011669
DB11757 2099 None 54 Human Functional pKi = 7.9 7.9 -4 5
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/jm4011669
46912314 91177 None 16 Human Functional pKi = 7.9 7.9 - 1
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 286 4 1 9 0.0 CC(=O)CCc1nc(N)c2nc(-n3nccn3)n(C)c2n1 10.1021/jm4011669
CHEMBL2398486 91177 None 16 Human Functional pKi = 7.9 7.9 - 1
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 286 4 1 9 0.0 CC(=O)CCc1nc(N)c2nc(-n3nccn3)n(C)c2n1 10.1021/jm4011669
46846868 110843 None 0 Human Functional pKi = 7.9 7.9 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 365 3 0 4 3.7 O=C(c1ccc(C(=O)N2CCCCCC2)cc1)c1cnc2ccc(F)cn12 10.1021/jm4011669
CHEMBL3260729 110843 None 0 Human Functional pKi = 7.9 7.9 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 365 3 0 4 3.7 O=C(c1ccc(C(=O)N2CCCCCC2)cc1)c1cnc2ccc(F)cn12 10.1021/jm4011669
53386422 131975 None 8 Human Functional pKi = 7.9 7.9 - 0
cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).
ChEMBL 339 2 1 7 3.1 Nc1nc(-c2nccs2)nc(-c2nccs2)c1Br nan
CHEMBL3694785 131975 None 8 Human Functional pKi = 7.9 7.9 - 0
cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).
ChEMBL 339 2 1 7 3.1 Nc1nc(-c2nccs2)nc(-c2nccs2)c1Br nan
45279445 109655 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 420 3 1 6 5.1 C[C@H]1CCC[C@@H](C)N1Cc1cc2c(N)nc(-c3ccc(Br)o3)nc2s1 10.1039/C1MD00082A
CHEMBL3222089 109655 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 420 3 1 6 5.1 C[C@H]1CCC[C@@H](C)N1Cc1cc2c(N)nc(-c3ccc(Br)o3)nc2s1 10.1039/C1MD00082A
46889171 7644 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 401 5 1 6 2.6 CN(C)CCN(C)C(=O)c1ccc2c(c1)-c1nc(N)nc(-c3ccccc3)c1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1088259 7644 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 401 5 1 6 2.6 CN(C)CCN(C)C(=O)c1ccc2c(c1)-c1nc(N)nc(-c3ccccc3)c1C2=O 10.1016/j.bmcl.2010.03.024
46888851 8710 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 399 4 2 6 3.8 CCN1CCC(Nc2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
CHEMBL1095812 8710 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 399 4 2 6 3.8 CCN1CCC(Nc2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
10118562 93668 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 514 9 1 12 2.0 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccccn5)nc43)CC2)cc1 10.1016/j.bmcl.2006.12.104
CHEMBL246675 93668 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 514 9 1 12 2.0 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccccn5)nc43)CC2)cc1 10.1016/j.bmcl.2006.12.104
10118562 93668 None 0 Human Functional pKi = 7.9 7.9 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 514 9 1 12 2.0 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccccn5)nc43)CC2)cc1 10.1021/jm4011669
CHEMBL246675 93668 None 0 Human Functional pKi = 7.9 7.9 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 514 9 1 12 2.0 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccccn5)nc43)CC2)cc1 10.1021/jm4011669
44217689 61024 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 471 6 1 12 0.5 Nc1nc2c(cnn2CCN2CCN(c3cnccn3)CC2)c2nn(Cc3ccccc3)c(=O)n12 10.1016/j.bmcl.2011.02.045
CHEMBL1762636 61024 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 471 6 1 12 0.5 Nc1nc2c(cnn2CCN2CCN(c3cnccn3)CC2)c2nn(Cc3ccccc3)c(=O)n12 10.1016/j.bmcl.2011.02.045
46889126 7670 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 389 4 2 6 3.2 Nc1nc(-c2ccc(F)cc2)c2c(n1)-c1cc(CNN3CCCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1088533 7670 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 389 4 2 6 3.2 Nc1nc(-c2ccc(F)cc2)c2c(n1)-c1cc(CNN3CCCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.042
44217690 61025 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 505 6 1 12 1.1 Nc1nc2c(cnn2CCN2CCN(c3cnccn3)CC2)c2nn(Cc3cccc(Cl)c3)c(=O)n12 10.1016/j.bmcl.2011.02.045
CHEMBL1762637 61025 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 505 6 1 12 1.1 Nc1nc2c(cnn2CCN2CCN(c3cnccn3)CC2)c2nn(Cc3cccc(Cl)c3)c(=O)n12 10.1016/j.bmcl.2011.02.045
46889096 7575 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 399 4 2 6 3.8 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CNN3CCCCCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1087727 7575 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 399 4 2 6 3.8 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CNN3CCCCCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.042
45279822 109671 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 360 3 1 6 3.4 Nc1nc(-c2cccc(Cl)c2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
CHEMBL3222105 109671 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 360 3 1 6 3.4 Nc1nc(-c2cccc(Cl)c2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
161713 98844 None 45 Guinea pig Functional pKi = 5.9 5.9 - 2
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 250 4 0 6 0.7 CCCn1c(=O)c2c(ncn2C)n(CCC)c1=O 10.1021/jm00157a035
CHEMBL278332 98844 None 45 Guinea pig Functional pKi = 5.9 5.9 - 2
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 250 4 0 6 0.7 CCCn1c(=O)c2c(ncn2C)n(CCC)c1=O 10.1021/jm00157a035
45279539 109665 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 332 3 1 7 2.8 Nc1nc(-c2cccs2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
CHEMBL3222099 109665 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 332 3 1 7 2.8 Nc1nc(-c2cccs2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
9936058 59577 None 2 Rat Functional pKi = 6.9 6.9 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 508 9 2 9 1.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NN4C(=O)C(C)=C(C)C4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17173 59577 None 2 Rat Functional pKi = 6.9 6.9 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 508 9 2 9 1.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NN4C(=O)C(C)=C(C)C4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
44276476 168197 None 0 Rat Functional pKi = 6.9 6.9 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 475 9 2 7 3.7 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL432664 168197 None 0 Rat Functional pKi = 6.9 6.9 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 475 9 2 7 3.7 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
14484978 97645 None 0 Rat Functional pKi = 6.9 6.9 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 483 9 1 10 1.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)ON4C(=O)CCC4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL27081 97645 None 0 Rat Functional pKi = 6.9 6.9 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 483 9 1 10 1.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)ON4C(=O)CCC4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
137632333 156622 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assayAntagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assay
ChEMBL 445 6 1 7 4.1 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3)nc12 10.1016/j.ejmech.2021.113907
CHEMBL4068032 156622 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assayAntagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assay
ChEMBL 445 6 1 7 4.1 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3)nc12 10.1016/j.ejmech.2021.113907
71458816 82136 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 384 3 1 5 4.3 CC1CC[C@@H](C)N1Cc1ccc2c(c1)-c1nc(N)nc(-c3ccccc3)c1C2=O 10.1021/jm201640m
CHEMBL2165805 82136 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 384 3 1 5 4.3 CC1CC[C@@H](C)N1Cc1ccc2c(c1)-c1nc(N)nc(-c3ccccc3)c1C2=O 10.1021/jm201640m
45274426 89817 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 387 5 1 6 5.1 COc1ccccc1Cc1cc2c(N)nc(-c3ccc(C(F)F)o3)nc2s1 10.1016/j.bmcl.2013.02.078
CHEMBL2377226 89817 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 387 5 1 6 5.1 COc1ccccc1Cc1cc2c(N)nc(-c3ccc(C(F)F)o3)nc2s1 10.1016/j.bmcl.2013.02.078
45278621 109294 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 347 3 1 6 3.6 N#Cc1cccc(-c2nc(N)c3cc(CN4CC=CCC4)sc3n2)c1 10.1039/C1MD00082A
CHEMBL3217866 109294 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 347 3 1 6 3.6 N#Cc1cccc(-c2nc(N)c3cc(CN4CC=CCC4)sc3n2)c1 10.1039/C1MD00082A
45275718 89822 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 368 4 1 7 4.3 COc1ccccc1Cc1cc2c(N)nc(-c3nc(C)cs3)nc2s1 10.1016/j.bmcl.2013.02.078
CHEMBL2377231 89822 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 368 4 1 7 4.3 COc1ccccc1Cc1cc2c(N)nc(-c3nc(C)cs3)nc2s1 10.1016/j.bmcl.2013.02.078
137648326 157758 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 464 6 1 8 3.6 COc1cnc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3F)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4081533 157758 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 464 6 1 8 3.6 COc1cnc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3F)nc12 10.1021/acs.jmedchem.6b01584
46889173 7646 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 415 7 2 6 3.0 CCN(CC)CCNC(=O)c1ccc2c(c1)-c1nc(N)nc(-c3ccccc3)c1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1088261 7646 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 415 7 2 6 3.0 CCN(CC)CCNC(=O)c1ccc2c(c1)-c1nc(N)nc(-c3ccccc3)c1C2=O 10.1016/j.bmcl.2010.03.024
46889256 8581 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 416 7 1 6 4.4 CC(C)N(CCOc1ccc2c(c1)-c1nc(N)nc(-c3ccccc3)c1C2=O)C(C)C 10.1016/j.bmcl.2010.03.024
CHEMBL1094721 8581 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 416 7 1 6 4.4 CC(C)N(CCOc1ccc2c(c1)-c1nc(N)nc(-c3ccccc3)c1C2=O)C(C)C 10.1016/j.bmcl.2010.03.024
935972 97587 None 7 Guinea pig Functional pKi = 6.9 6.9 - 1
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 272 1 2 6 0.3 Cn1c(=O)c2nc(-c3ccc(O)cc3)[nH]c2n(C)c1=O 10.1021/jm00382a018
CHEMBL27047 97587 None 7 Guinea pig Functional pKi = 6.9 6.9 - 1
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 272 1 2 6 0.3 Cn1c(=O)c2nc(-c3ccc(O)cc3)[nH]c2n(C)c1=O 10.1021/jm00382a018
13525058 98644 None 0 Guinea pig Functional pKi = 6.9 6.9 - 2
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 271 1 2 6 0.2 Cn1c(=O)c2nc(-c3ccc(N)cc3)[nH]c2n(C)c1=O 10.1021/jm00382a018
CHEMBL276830 98644 None 0 Guinea pig Functional pKi = 6.9 6.9 - 2
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 271 1 2 6 0.2 Cn1c(=O)c2nc(-c3ccc(N)cc3)[nH]c2n(C)c1=O 10.1021/jm00382a018
45279362 109663 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 343 3 1 7 3.7 C[C@H]1CCC[C@@H](C)N1Cc1cc2c(N)nc(-c3ccon3)nc2s1 10.1039/C1MD00082A
CHEMBL3222097 109663 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 343 3 1 7 3.7 C[C@H]1CCC[C@@H](C)N1Cc1cc2c(N)nc(-c3ccon3)nc2s1 10.1039/C1MD00082A
9871761 59501 None 0 Rat Functional pKi = 5.9 5.9 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 533 11 4 9 1.2 CCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(CC(=O)NCCN)cc4)cc3)[nH]c2n(CC)c1=O 10.1021/jm990421v
CHEMBL17141 59501 None 0 Rat Functional pKi = 5.9 5.9 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 533 11 4 9 1.2 CCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(CC(=O)NCCN)cc4)cc3)[nH]c2n(CC)c1=O 10.1021/jm990421v
52945717 18339 None 0 Rat Functional pKi = 7.9 7.9 - 0
Antagonist activity at rat A2A receptor by cAMP functional assayAntagonist activity at rat A2A receptor by cAMP functional assay
ChEMBL 460 7 1 7 3.6 COCCCn1c(NC(=O)c2cccc(C#N)c2)nc2cc(C(=O)N3CCCC[C@@H]3C)cnc21 10.1016/j.bmcl.2010.08.064
CHEMBL1270814 18339 None 0 Rat Functional pKi = 7.9 7.9 - 0
Antagonist activity at rat A2A receptor by cAMP functional assayAntagonist activity at rat A2A receptor by cAMP functional assay
ChEMBL 460 7 1 7 3.6 COCCCn1c(NC(=O)c2cccc(C#N)c2)nc2cc(C(=O)N3CCCC[C@@H]3C)cnc21 10.1016/j.bmcl.2010.08.064
44217536 61001 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 428 5 1 10 0.9 Nc1nc2c(cnn2CCN2CCOCC2)c2nn(Cc3cccc(Cl)c3)c(=O)n12 10.1016/j.bmcl.2011.02.045
CHEMBL1762515 61001 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 428 5 1 10 0.9 Nc1nc2c(cnn2CCN2CCOCC2)c2nn(Cc3cccc(Cl)c3)c(=O)n12 10.1016/j.bmcl.2011.02.045
44217536 61001 None 0 Human Functional pKi = 7.9 7.9 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 428 5 1 10 0.9 Nc1nc2c(cnn2CCN2CCOCC2)c2nn(Cc3cccc(Cl)c3)c(=O)n12 10.1021/jm4011669
CHEMBL1762515 61001 None 0 Human Functional pKi = 7.9 7.9 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 428 5 1 10 0.9 Nc1nc2c(cnn2CCN2CCOCC2)c2nn(Cc3cccc(Cl)c3)c(=O)n12 10.1021/jm4011669
46888990 7566 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 370 3 1 5 3.9 Nc1nc(-c2ccccc2)c2c(n1)-c1c(CN3CCCCC3)cccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1087701 7566 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 370 3 1 5 3.9 Nc1nc(-c2ccccc2)c2c(n1)-c1c(CN3CCCCC3)cccc1C2=O 10.1016/j.bmcl.2010.03.042
10126504 179227 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 386 4 1 9 2.3 Nc1nc2c(cnn2CCN2Cc3ccccc3C2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
CHEMBL471923 179227 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 386 4 1 9 2.3 Nc1nc2c(cnn2CCN2Cc3ccccc3C2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
46889229 7490 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 413 3 1 6 2.7 CCN1CCN(C(=O)c2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
CHEMBL1087084 7490 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 413 3 1 6 2.7 CCN1CCN(C(=O)c2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
45279729 109614 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 274 3 1 6 2.6 CN(C)Cc1cc2c(N)nc(-c3ccco3)nc2s1 10.1039/C1MD00082A
CHEMBL3222047 109614 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 274 3 1 6 2.6 CN(C)Cc1cc2c(N)nc(-c3ccco3)nc2s1 10.1039/C1MD00082A
9870396 139124 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 494 7 1 7 4.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(C(F)(F)F)ccc4Cl)c3)[nH]c2n(CCC)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL378598 139124 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 494 7 1 7 4.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(C(F)(F)F)ccc4Cl)c3)[nH]c2n(CCC)c1=O 10.1016/j.ejmech.2010.04.039
11492842 163235 None 0 Guinea pig Functional pKi = 5.9 5.9 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 278 6 0 6 1.6 CCCn1c(=O)c2c(ncn2CCC)n(CCC)c1=O 10.1021/jm00157a035
CHEMBL417834 163235 None 0 Guinea pig Functional pKi = 5.9 5.9 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 278 6 0 6 1.6 CCCn1c(=O)c2c(ncn2CCC)n(CCC)c1=O 10.1021/jm00157a035
2153 3800 None 72 Guinea pig Functional pKi = 4.9 4.9 - 5
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00382a018
2153.0 3800 None 72 Guinea pig Functional pKi = 4.9 4.9 - 5
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00382a018
2620 3800 None 72 Guinea pig Functional pKi = 4.9 4.9 - 5
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00382a018
413 3800 None 72 Guinea pig Functional pKi = 4.9 4.9 - 5
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00382a018
CHEMBL190 3800 None 72 Guinea pig Functional pKi = 4.9 4.9 - 5
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00382a018
DB00277 3800 None 72 Guinea pig Functional pKi = 4.9 4.9 - 5
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00382a018
95030 209073 None 15 Guinea pig Functional pKi = 4.9 4.9 - 0
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 194 0 1 5 -0.7 Cc1nc2c(=O)n(C)c(=O)n(C)c2[nH]1 10.1021/jm00382a018
CHEMBL89062 209073 None 15 Guinea pig Functional pKi = 4.9 4.9 - 0
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 194 0 1 5 -0.7 Cc1nc2c(=O)n(C)c(=O)n(C)c2[nH]1 10.1021/jm00382a018
2153 3800 None 72 Guinea pig Functional pKi = 4.9 4.9 - 5
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00157a035
2153.0 3800 None 72 Guinea pig Functional pKi = 4.9 4.9 - 5
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00157a035
2620 3800 None 72 Guinea pig Functional pKi = 4.9 4.9 - 5
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00157a035
413 3800 None 72 Guinea pig Functional pKi = 4.9 4.9 - 5
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00157a035
CHEMBL190 3800 None 72 Guinea pig Functional pKi = 4.9 4.9 - 5
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00157a035
DB00277 3800 None 72 Guinea pig Functional pKi = 4.9 4.9 - 5
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm00157a035
95028 93861 None 21 Guinea pig Functional pKi = 4.9 4.9 - 1
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 270 2 0 6 0.5 Cn1c(=O)c2c(ncn2Cc2ccccc2)n(C)c1=O 10.1021/jm00157a035
CHEMBL24759 93861 None 21 Guinea pig Functional pKi = 4.9 4.9 - 1
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 270 2 0 6 0.5 Cn1c(=O)c2c(ncn2Cc2ccccc2)n(C)c1=O 10.1021/jm00157a035
250782 93889 None 8 Guinea pig Functional pKi = 4.9 4.9 - 1
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 332 4 1 5 2.0 O=c1c2[nH]cnc2n(Cc2ccccc2)c(=O)n1Cc1ccccc1 10.1021/jm00157a035
CHEMBL24774 93889 None 8 Guinea pig Functional pKi = 4.9 4.9 - 1
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 332 4 1 5 2.0 O=c1c2[nH]cnc2n(Cc2ccccc2)c(=O)n1Cc1ccccc1 10.1021/jm00157a035
9892149 59644 None 0 Rat Functional pKi = 6.8 6.8 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 499 9 2 7 4.2 CCCn1c(=O)c2nc(-c3ccc(/C=C/C(=O)Nc4ccccc4C(C)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17202 59644 None 0 Rat Functional pKi = 6.8 6.8 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 499 9 2 7 4.2 CCCn1c(=O)c2nc(-c3ccc(/C=C/C(=O)Nc4ccccc4C(C)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
54586844 61023 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 595 10 1 12 2.5 COCCOc1ccc(N2CCN(CCn3ncc4c3nc(N)n3c(=O)n(Cc5cccc(Cl)c5)nc43)CC2)c(F)c1 10.1016/j.bmcl.2011.02.045
CHEMBL1762635 61023 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 595 10 1 12 2.5 COCCOc1ccc(N2CCN(CCn3ncc4c3nc(N)n3c(=O)n(Cc5cccc(Cl)c5)nc43)CC2)c(F)c1 10.1016/j.bmcl.2011.02.045
45279273 109652 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 370 3 1 6 4.0 Nc1nc(-c2ccc(Cl)o2)nc2sc(CN3CCC(F)(F)C3)cc12 10.1039/C1MD00082A
CHEMBL3222086 109652 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 370 3 1 6 4.0 Nc1nc(-c2ccc(Cl)o2)nc2sc(CN3CCC(F)(F)C3)cc12 10.1039/C1MD00082A
45279361 109296 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 379 3 1 7 3.4 C[C@H]1CN(Cc2cc3c(N)nc(-c4cccc(C#N)c4)nc3s2)C[C@@H](C)O1 10.1039/C1MD00082A
CHEMBL3217868 109296 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 379 3 1 7 3.4 C[C@H]1CN(Cc2cc3c(N)nc(-c4cccc(C#N)c4)nc3s2)C[C@@H](C)O1 10.1039/C1MD00082A
11537163 163289 None 3 Guinea pig Functional pKi = 5.8 5.8 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 326 6 0 6 2.2 CCCn1c(=O)c2c(ncn2Cc2ccccc2)n(CCC)c1=O 10.1021/jm00157a035
CHEMBL418193 163289 None 3 Guinea pig Functional pKi = 5.8 5.8 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 326 6 0 6 2.2 CCCn1c(=O)c2c(ncn2Cc2ccccc2)n(CCC)c1=O 10.1021/jm00157a035
13525048 98232 None 0 Guinea pig Functional pKi = 4.8 4.8 - 1
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 300 2 2 6 0.3 Cn1c(=O)c2nc(-c3cccc(C(=O)O)c3)[nH]c2n(C)c1=O 10.1021/jm00382a018
CHEMBL273953 98232 None 0 Guinea pig Functional pKi = 4.8 4.8 - 1
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 300 2 2 6 0.3 Cn1c(=O)c2nc(-c3cccc(C(=O)O)c3)[nH]c2n(C)c1=O 10.1021/jm00382a018
9957239 59434 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 490 7 2 6 4.8 O=C(O)/C=C/c1ccc(-c2nc3c(=O)n(CC4CCCCC4)c(=O)n(CC4CCCCC4)c3[nH]2)cc1 10.1021/jm990421v
CHEMBL17103 59434 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 490 7 2 6 4.8 O=C(O)/C=C/c1ccc(-c2nc3c(=O)n(CC4CCCCC4)c(=O)n(CC4CCCCC4)c3[nH]2)cc1 10.1021/jm990421v
11801496 98800 None 0 Rat Functional pKi = 6.8 6.8 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 587 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL278039 98800 None 0 Rat Functional pKi = 6.8 6.8 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 587 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
17757368 18198 None 0 Rat Functional pKi = 7.8 7.8 - 0
Antagonist activity at rat A2A receptor by cAMP functional assayAntagonist activity at rat A2A receptor by cAMP functional assay
ChEMBL 433 9 1 6 3.7 CCN(CC)C(=O)c1ccc2nc(NC(=O)c3cccc(C#N)c3)n(CCCOC)c2c1 10.1016/j.bmcl.2010.08.064
CHEMBL1269901 18198 None 0 Rat Functional pKi = 7.8 7.8 - 0
Antagonist activity at rat A2A receptor by cAMP functional assayAntagonist activity at rat A2A receptor by cAMP functional assay
ChEMBL 433 9 1 6 3.7 CCN(CC)C(=O)c1ccc2nc(NC(=O)c3cccc(C#N)c3)n(CCCOC)c2c1 10.1016/j.bmcl.2010.08.064
53354627 110842 None 0 Human Functional pKi = 7.8 7.8 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 285 2 1 6 1.7 CC1CN(c2nnc(N)nc2-c2ccccc2)CC(C)O1 10.1021/jm4011669
CHEMBL3260728 110842 None 0 Human Functional pKi = 7.8 7.8 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 285 2 1 6 1.7 CC1CN(c2nnc(N)nc2-c2ccccc2)CC(C)O1 10.1021/jm4011669
45275717 89821 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 338 3 1 6 4.3 Cc1csc(-c2nc(N)c3cc(Cc4ccccc4)sc3n2)n1 10.1016/j.bmcl.2013.02.078
CHEMBL2377230 89821 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 338 3 1 6 4.3 Cc1csc(-c2nc(N)c3cc(Cc4ccccc4)sc3n2)n1 10.1016/j.bmcl.2013.02.078
10767043 59040 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 479 9 2 7 3.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16929 59040 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 479 9 2 7 3.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
46889206 7510 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 441 4 2 6 3.5 CC(C)N1CCC(NC(=O)c2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
CHEMBL1087183 7510 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 441 4 2 6 3.5 CC(C)N1CCC(NC(=O)c2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
11690712 77821 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 439 7 3 6 2.0 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)NCc4ccccc4)cc3)nc2c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL209230 77821 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 439 7 3 6 2.0 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)NCc4ccccc4)cc3)nc2c1=O 10.1016/j.ejmech.2010.04.039
10840167 59196 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 539 9 2 7 4.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17003 59196 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 539 9 2 7 4.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL5089483 217699 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCCn1c(=O)c2nc(C34CCC(C(=O)NCCCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
45274227 89808 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 349 4 1 5 5.2 CC(C)c1ccc(-c2nc(N)c3cc(Cc4ccccc4)sc3n2)o1 10.1016/j.bmcl.2013.02.078
CHEMBL2377114 89808 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 349 4 1 5 5.2 CC(C)c1ccc(-c2nc(N)c3cc(Cc4ccccc4)sc3n2)o1 10.1016/j.bmcl.2013.02.078
45279277 109638 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 384 4 1 6 5.4 CC(C)c1ccc(-c2nc(N)c3cc(CN4[C@@H](C)CCC[C@H]4C)sc3n2)o1 10.1039/C1MD00082A
CHEMBL3222072 109638 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 384 4 1 6 5.4 CC(C)c1ccc(-c2nc(N)c3cc(CN4[C@@H](C)CCC[C@H]4C)sc3n2)o1 10.1039/C1MD00082A
45274225 89798 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 319 3 1 6 3.3 Nc1nc(-c2ncccn2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
CHEMBL2377104 89798 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 319 3 1 6 3.3 Nc1nc(-c2ncccn2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
46889252 7688 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 360 5 1 6 2.9 CN(C)CCOc1ccc2c(c1)-c1nc(N)nc(-c3ccccc3)c1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1088710 7688 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 360 5 1 6 2.9 CN(C)CCOc1ccc2c(c1)-c1nc(N)nc(-c3ccccc3)c1C2=O 10.1016/j.bmcl.2010.03.024
10174142 178999 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 477 5 1 10 3.4 Nc1nc2c(cnn2CCN2CCc3ncc(-c4ccccc4)cc3C2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
CHEMBL469879 178999 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 477 5 1 10 3.4 Nc1nc2c(cnn2CCN2CCc3ncc(-c4ccccc4)cc3C2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
45279545 109617 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 328 4 2 6 4.0 Nc1nc(-c2ccco2)nc2sc(CNC3CCCCC3)cc12 10.1039/C1MD00082A
CHEMBL3222050 109617 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 328 4 2 6 4.0 Nc1nc(-c2ccco2)nc2sc(CNC3CCCCC3)cc12 10.1039/C1MD00082A
13525064 9341 None 0 Guinea pig Functional pKi = 5.8 5.8 - 2
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 271 1 2 6 0.2 Cn1c(=O)c2nc(-c3ccccc3N)[nH]c2n(C)c1=O 10.1021/jm00382a018
CHEMBL11120 9341 None 0 Guinea pig Functional pKi = 5.8 5.8 - 2
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 271 1 2 6 0.2 Cn1c(=O)c2nc(-c3ccccc3N)[nH]c2n(C)c1=O 10.1021/jm00382a018
936355 162004 None 7 Guinea pig Functional pKi = 5.8 5.8 - 1
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 272 1 2 6 0.3 Cn1c(=O)c2nc(-c3ccccc3O)[nH]c2n(C)c1=O 10.1021/jm00382a018
CHEMBL415248 162004 None 7 Guinea pig Functional pKi = 5.8 5.8 - 1
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 272 1 2 6 0.3 Cn1c(=O)c2nc(-c3ccccc3O)[nH]c2n(C)c1=O 10.1021/jm00382a018
54587363 60598 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 347 4 2 7 1.7 Nc1nc(-c2cccc(CO)c2)cc2nn(Cc3ccccc3)c(=O)n12 10.1016/j.bmcl.2011.02.045
CHEMBL1760026 60598 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 347 4 2 7 1.7 Nc1nc(-c2cccc(CO)c2)cc2nn(Cc3ccccc3)c(=O)n12 10.1016/j.bmcl.2011.02.045
3048504 96685 None 1 Guinea pig Functional pKi = 5.8 5.8 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 264 4 1 5 1.2 CC(C)Cn1c(=O)c2nc[nH]c2n(CC(C)C)c1=O 10.1021/jm00157a035
CHEMBL26350 96685 None 1 Guinea pig Functional pKi = 5.8 5.8 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 264 4 1 5 1.2 CC(C)Cn1c(=O)c2nc[nH]c2n(CC(C)C)c1=O 10.1021/jm00157a035
155511832 169705 None 0 Human Functional pKi = 5.8 5.8 - 0
Inverse agonist activity at recombinant human A2A receptor expressed in HEK293T cells co-expressing Gs assessed as decrease in cAMP accumulation measured after 15 mins by Glosensor chemiluminescence assayInverse agonist activity at recombinant human A2A receptor expressed in HEK293T cells co-expressing Gs assessed as decrease in cAMP accumulation measured after 15 mins by Glosensor chemiluminescence assay
ChEMBL 341 5 3 6 2.9 Nc1nc(NCc2ccc(Cl)cc2)nc(-c2ccccc2CO)n1 10.1021/acs.jmedchem.9b00869
CHEMBL4436453 169705 None 0 Human Functional pKi = 5.8 5.8 - 0
Inverse agonist activity at recombinant human A2A receptor expressed in HEK293T cells co-expressing Gs assessed as decrease in cAMP accumulation measured after 15 mins by Glosensor chemiluminescence assayInverse agonist activity at recombinant human A2A receptor expressed in HEK293T cells co-expressing Gs assessed as decrease in cAMP accumulation measured after 15 mins by Glosensor chemiluminescence assay
ChEMBL 341 5 3 6 2.9 Nc1nc(NCc2ccc(Cl)cc2)nc(-c2ccccc2CO)n1 10.1021/acs.jmedchem.9b00869
2153 3800 None 72 Human Functional pKi = 5.8 5.8 -2 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
2153.0 3800 None 72 Human Functional pKi = 5.8 5.8 -2 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
2620 3800 None 72 Human Functional pKi = 5.8 5.8 -2 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
413 3800 None 72 Human Functional pKi = 5.8 5.8 -2 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
CHEMBL190 3800 None 72 Human Functional pKi = 5.8 5.8 -2 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
DB00277 3800 None 72 Human Functional pKi = 5.8 5.8 -2 5
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
135921140 11347 None 0 Rat Functional pKi = 4.8 4.8 - 0
Inhibition against A2A-Adenosine Receptor of rat PC12 cell membranes (functional antagonist activity)Inhibition against A2A-Adenosine Receptor of rat PC12 cell membranes (functional antagonist activity)
ChEMBL 267 1 1 4 1.7 Cn1c(-c2ccccc2)nc2c1C1=NCCN1C(=O)N2 10.1021/jm011093d
CHEMBL117962 11347 None 0 Rat Functional pKi = 4.8 4.8 - 0
Inhibition against A2A-Adenosine Receptor of rat PC12 cell membranes (functional antagonist activity)Inhibition against A2A-Adenosine Receptor of rat PC12 cell membranes (functional antagonist activity)
ChEMBL 267 1 1 4 1.7 Cn1c(-c2ccccc2)nc2c1C1=NCCN1C(=O)N2 10.1021/jm011093d
71603090 89800 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 352 3 1 5 4.6 Nc1nc(-c2cccc(Cl)n2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
CHEMBL2377106 89800 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 352 3 1 5 4.6 Nc1nc(-c2cccc(Cl)n2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
46888783 8664 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 420 5 1 7 2.8 Nc1nc(-c2ccc(F)cc2)c2c(n1)-c1cc(OCCN3CCOCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1095489 8664 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 420 5 1 7 2.8 Nc1nc(-c2ccc(F)cc2)c2c(n1)-c1cc(OCCN3CCOCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
46888989 7565 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 358 5 1 5 3.8 CCN(CC)Cc1cccc2c1-c1nc(N)nc(-c3ccccc3)c1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1087700 7565 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 358 5 1 5 3.8 CCN(CC)Cc1cccc2c1-c1nc(N)nc(-c3ccccc3)c1C2=O 10.1016/j.bmcl.2010.03.042
404 4098 None 26 Human Functional pKi = 7.7 7.7 - 2
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1021/jm990421v
432 4098 None 26 Human Functional pKi = 7.7 7.7 - 2
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1021/jm990421v
5697 4098 None 26 Human Functional pKi = 7.7 7.7 - 2
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1021/jm990421v
CHEMBL273094 4098 None 26 Human Functional pKi = 7.7 7.7 - 2
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1021/jm990421v
46889205 7460 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 427 3 1 6 3.1 CN1CCC(N(C)C(=O)c2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
CHEMBL1086804 7460 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 427 3 1 6 3.1 CN1CCC(N(C)C(=O)c2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
45278539 109300 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 347 3 1 6 3.6 N#Cc1ccc(-c2nc(N)c3cc(CN4CC=CCC4)sc3n2)cc1 10.1039/C1MD00082A
CHEMBL3217871 109300 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 347 3 1 6 3.6 N#Cc1ccc(-c2nc(N)c3cc(CN4CC=CCC4)sc3n2)cc1 10.1039/C1MD00082A
11610869 80287 None 0 Rat Functional pKi = 6.7 6.7 - 0
Antagonist activity against rat adenosine A2A receptorAntagonist activity against rat adenosine A2A receptor
ChEMBL 393 5 3 8 -1.0 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)NCC(=O)O)cc3)[nH]c2n(C)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL213878 80287 None 0 Rat Functional pKi = 6.7 6.7 - 0
Antagonist activity against rat adenosine A2A receptorAntagonist activity against rat adenosine A2A receptor
ChEMBL 393 5 3 8 -1.0 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)NCC(=O)O)cc3)[nH]c2n(C)c1=O 10.1016/j.ejmech.2010.04.039
10720065 98450 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 495 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Cl)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL275427 98450 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 495 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Cl)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
46888784 8665 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 386 5 1 6 3.4 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(OCCN3CCCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1095490 8665 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 386 5 1 6 3.4 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(OCCN3CCCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
59276682 109626 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 332 3 1 6 3.5 Nc1nc(-c2ccco2)nc2sc(CN3CCC(F)CC3)cc12 10.1039/C1MD00082A
CHEMBL3222059 109626 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 332 3 1 6 3.5 Nc1nc(-c2ccco2)nc2sc(CN3CCC(F)CC3)cc12 10.1039/C1MD00082A
443 755 None 9 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 382 7 2 6 2.5 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)/C=C/C(=O)O 10.1021/jm990421v
6439089 755 None 9 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 382 7 2 6 2.5 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)/C=C/C(=O)O 10.1021/jm990421v
CHEMBL16997 755 None 9 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 382 7 2 6 2.5 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)/C=C/C(=O)O 10.1021/jm990421v
9936058 59577 None 2 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 508 9 2 9 1.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NN4C(=O)C(C)=C(C)C4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17173 59577 None 2 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 508 9 2 9 1.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NN4C(=O)C(C)=C(C)C4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
176408 3557 None 55 Human Functional pKi = 8.7 8.7 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1016/j.bmcl.2008.05.069
176408 3557 None 55 Human Functional pKi = 8.7 8.7 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1016/j.bmcl.2008.05.074
403 3557 None 55 Human Functional pKi = 8.7 8.7 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1016/j.bmcl.2008.05.069
403 3557 None 55 Human Functional pKi = 8.7 8.7 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1016/j.bmcl.2008.05.074
431 3557 None 55 Human Functional pKi = 8.7 8.7 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1016/j.bmcl.2008.05.069
431 3557 None 55 Human Functional pKi = 8.7 8.7 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1016/j.bmcl.2008.05.074
CHEMBL17127 3557 None 55 Human Functional pKi = 8.7 8.7 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1016/j.bmcl.2008.05.069
CHEMBL17127 3557 None 55 Human Functional pKi = 8.7 8.7 - 1
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1016/j.bmcl.2008.05.074
44438089 93619 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 531 9 1 11 2.7 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5cccc(F)c5)nc43)CC2)cc1 10.1016/j.bmcl.2006.12.104
CHEMBL246469 93619 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 531 9 1 11 2.7 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5cccc(F)c5)nc43)CC2)cc1 10.1016/j.bmcl.2006.12.104
10288990 179175 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 488 8 1 11 2.4 COCCOc1ccc2c(c1)CCN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1016/j.bmcl.2008.05.069
CHEMBL471553 179175 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 488 8 1 11 2.4 COCCOc1ccc2c(c1)CCN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1016/j.bmcl.2008.05.069
10287757 179254 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 414 4 1 9 2.4 Nc1nc2c(cnn2CCN2CCc3ccccc3CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
CHEMBL472110 179254 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 414 4 1 9 2.4 Nc1nc2c(cnn2CCN2CCc3ccccc3CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
10287779 189541 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 415 4 1 10 2.1 Cc1cnc2c(c1)CN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1016/j.bmcl.2008.05.069
CHEMBL513364 189541 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 415 4 1 10 2.1 Cc1cnc2c(c1)CN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1016/j.bmcl.2008.05.069
10287779 189541 None 0 Human Functional pKi = 8.7 8.7 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 415 4 1 10 2.1 Cc1cnc2c(c1)CN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1021/jm4011669
CHEMBL513364 189541 None 0 Human Functional pKi = 8.7 8.7 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 415 4 1 10 2.1 Cc1cnc2c(c1)CN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1021/jm4011669
56943965 163758 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 561 9 1 13 2.2 COCC(C)(C)Oc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
CHEMBL4204531 163758 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 561 9 1 13 2.2 COCC(C)(C)Oc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)cc1 10.1021/acsmedchemlett.7b00175
137632691 156616 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 447 5 2 7 4.0 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(O)(C(C)C)CC3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4067952 156616 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 447 5 2 7 4.0 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(O)(C(C)C)CC3)nc12 10.1021/acs.jmedchem.6b01584
137661957 159617 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 471 6 1 9 3.7 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc4c(c3)OCO4)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4102234 159617 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 471 6 1 9 3.7 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc4c(c3)OCO4)nc12 10.1021/acs.jmedchem.6b01584
176408 3557 None 55 Human Functional pKi = 8.6 8.6 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1016/j.ejmech.2022.114378
403 3557 None 55 Human Functional pKi = 8.6 8.6 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1016/j.ejmech.2022.114378
431 3557 None 55 Human Functional pKi = 8.6 8.6 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1016/j.ejmech.2022.114378
CHEMBL17127 3557 None 55 Human Functional pKi = 8.6 8.6 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1016/j.ejmech.2022.114378
44568376 184004 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 495 6 1 11 2.9 Nc1nc2c(cnn2CCc2ccc3nc(CN4CCOCC4)ccc3c2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.074
CHEMBL481147 184004 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 495 6 1 11 2.9 Nc1nc2c(cnn2CCc2ccc3nc(CN4CCOCC4)ccc3c2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.074
10152925 189264 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 550 8 1 11 4.2 COc1cc2c(cc1OC)C(Cc1ccccc1)N(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1016/j.bmcl.2008.05.069
CHEMBL510959 189264 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 550 8 1 11 4.2 COc1cc2c(cc1OC)C(Cc1ccccc1)N(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1016/j.bmcl.2008.05.069
24894065 192508 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 410 4 1 9 3.4 Cc1ccc2cc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)ccc2n1 10.1016/j.bmcl.2008.05.074
CHEMBL520782 192508 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 410 4 1 9 3.4 Cc1ccc2cc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)ccc2n1 10.1016/j.bmcl.2008.05.074
137634085 156380 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 463 6 1 7 4.2 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)c(F)c3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4065326 156380 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 463 6 1 7 4.2 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)c(F)c3)nc12 10.1021/acs.jmedchem.6b01584
45274324 89797 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 319 3 1 6 3.3 Nc1nc(-c2cnccn2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
CHEMBL2377103 89797 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 319 3 1 6 3.3 Nc1nc(-c2cnccn2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
24894065 192508 None 0 Human Functional pKi = 8.6 8.6 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 410 4 1 9 3.4 Cc1ccc2cc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)ccc2n1 10.1021/jm4011669
CHEMBL520782 192508 None 0 Human Functional pKi = 8.6 8.6 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 410 4 1 9 3.4 Cc1ccc2cc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)ccc2n1 10.1021/jm4011669
46861769 7569 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 356 3 1 5 3.5 Nc1nc(-c2ccccc2)c2c(n1)-c1c(CN3CCCC3)cccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1087709 7569 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 356 3 1 5 3.5 Nc1nc(-c2ccccc2)c2c(n1)-c1c(CN3CCCC3)cccc1C2=O 10.1016/j.bmcl.2010.03.042
10288019 178968 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 430 5 1 10 2.4 COc1ccc2c(c1)CCN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)C2 10.1016/j.bmcl.2008.05.069
CHEMBL469673 178968 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 430 5 1 10 2.4 COc1ccc2c(c1)CCN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)C2 10.1016/j.bmcl.2008.05.069
44520976 204648 None 1 Human Functional pKi = 8.6 8.6 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 323 4 2 6 2.3 Cc1cccc(CNC(=O)c2cc(-c3ccc(C)o3)nc(N)n2)n1 10.1021/jm4011669
CHEMBL609578 204648 None 1 Human Functional pKi = 8.6 8.6 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 323 4 2 6 2.3 Cc1cccc(CNC(=O)c2cc(-c3ccc(C)o3)nc(N)n2)n1 10.1021/jm4011669
137658498 159693 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 463 6 1 7 4.2 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3F)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4103179 159693 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 463 6 1 7 4.2 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3F)nc12 10.1021/acs.jmedchem.6b01584
44568373 184111 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 424 5 1 9 3.7 CCc1ccc2cc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)ccc2n1 10.1016/j.bmcl.2008.05.074
CHEMBL481956 184111 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 424 5 1 9 3.7 CCc1ccc2cc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)ccc2n1 10.1016/j.bmcl.2008.05.074
46861781 8741 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 371 2 1 6 2.7 CN1CCN(c2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
CHEMBL1096134 8741 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 371 2 1 6 2.7 CN1CCN(c2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
44568374 183708 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 484 9 1 11 3.3 COCCOCc1ccc2cc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)ccc2n1 10.1016/j.bmcl.2008.05.074
CHEMBL480177 183708 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 484 9 1 11 3.3 COCCOCc1ccc2cc(CCn3ncc4c3nc(N)n3nc(-c5ccco5)nc43)ccc2n1 10.1016/j.bmcl.2008.05.074
45274330 89804 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 355 3 1 5 5.1 Cc1ccc(-c2nc(N)c3cc(Cc4ccccc4Cl)sc3n2)o1 10.1016/j.bmcl.2013.02.078
CHEMBL2377110 89804 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 355 3 1 5 5.1 Cc1ccc(-c2nc(N)c3cc(Cc4ccccc4Cl)sc3n2)o1 10.1016/j.bmcl.2013.02.078
46888879 8715 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 358 2 1 6 2.8 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(N3CCOCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1095822 8715 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 358 2 1 6 2.8 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(N3CCOCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
44438092 93667 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 527 9 1 11 2.9 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccccc5C)nc43)CC2)cc1 10.1016/j.bmcl.2006.12.104
CHEMBL246674 93667 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 527 9 1 11 2.9 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccccc5C)nc43)CC2)cc1 10.1016/j.bmcl.2006.12.104
46889231 7492 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 427 3 1 6 3.1 CC(C)N1CCN(C(=O)c2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
CHEMBL1087086 7492 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 427 3 1 6 3.1 CC(C)N1CCN(C(=O)c2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
45279724 109624 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 376 3 1 6 4.4 Cc1ccc(-c2nc(N)c3cc(CN4CCc5ccccc5C4)sc3n2)o1 10.1039/C1MD00082A
CHEMBL3222057 109624 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 376 3 1 6 4.4 Cc1ccc(-c2nc(N)c3cc(CN4CCc5ccccc5C4)sc3n2)o1 10.1039/C1MD00082A
45275823 89802 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 335 4 1 5 4.6 Cc1ccc(-c2nc(N)c3cc(CCc4ccccc4)sc3n2)o1 10.1016/j.bmcl.2013.02.078
CHEMBL2377108 89802 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 335 4 1 5 4.6 Cc1ccc(-c2nc(N)c3cc(CCc4ccccc4)sc3n2)o1 10.1016/j.bmcl.2013.02.078
71603017 89781 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 303 2 1 4 4.6 Nc1nc(-c2ccccc2)nc2sc(-c3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
CHEMBL2377087 89781 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 303 2 1 4 4.6 Nc1nc(-c2ccccc2)nc2sc(-c3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
45279358 109660 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 347 3 1 8 2.5 Cc1csc(-c2nc(N)c3cc(CN4CCOCC4)sc3n2)n1 10.1039/C1MD00082A
CHEMBL3222094 109660 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 347 3 1 8 2.5 Cc1csc(-c2nc(N)c3cc(CN4CCOCC4)sc3n2)n1 10.1039/C1MD00082A
45275716 89795 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 318 3 1 5 3.9 Nc1nc(-c2cccnc2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
CHEMBL2377101 89795 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 318 3 1 5 3.9 Nc1nc(-c2cccnc2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
45278865 109646 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 334 3 1 6 3.8 Nc1nc(-c2ccc(Cl)o2)nc2sc(CN3CCCC3)cc12 10.1039/C1MD00082A
CHEMBL3222080 109646 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 334 3 1 6 3.8 Nc1nc(-c2ccc(Cl)o2)nc2sc(CN3CCCC3)cc12 10.1039/C1MD00082A
45279633 109653 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 378 3 1 6 3.9 Nc1nc(-c2ccc(Br)o2)nc2sc(CN3CCCC3)cc12 10.1039/C1MD00082A
CHEMBL3222087 109653 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 378 3 1 6 3.9 Nc1nc(-c2ccc(Br)o2)nc2sc(CN3CCCC3)cc12 10.1039/C1MD00082A
9935943 59042 None 0 Rat Functional pKi = 6.7 6.7 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 505 10 3 8 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16931 59042 None 0 Rat Functional pKi = 6.7 6.7 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 505 10 3 8 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
126079 4100 None 29 Rat Functional pKi = 5.7 5.7 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 10.1021/jm990421v
451 4100 None 29 Rat Functional pKi = 5.7 5.7 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 10.1021/jm990421v
CHEMBL27041 4100 None 29 Rat Functional pKi = 5.7 5.7 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 10.1021/jm990421v
10840167 59196 None 0 Rat Functional pKi = 6.7 6.7 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 539 9 2 7 4.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17003 59196 None 0 Rat Functional pKi = 6.7 6.7 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 539 9 2 7 4.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
45275061 89790 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 368 3 1 5 4.9 N#Cc1cccc(-c2nc(N)c3cc(C4(c5ccccc5)CC4)sc3n2)c1 10.1016/j.bmcl.2013.02.078
CHEMBL2377096 89790 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 368 3 1 5 4.9 N#Cc1cccc(-c2nc(N)c3cc(C4(c5ccccc5)CC4)sc3n2)c1 10.1016/j.bmcl.2013.02.078
10839228 59885 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 504 8 2 8 2.1 CCCn1c(=O)c2nc(-c3ccc(/C=C/C(=O)NN4C(=O)C(C)=C(C)C4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17294 59885 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 504 8 2 8 2.1 CCCn1c(=O)c2nc(-c3ccc(/C=C/C(=O)NN4C(=O)C(C)=C(C)C4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
90665318 109306 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 413 4 1 6 3.6 CN(C)C(=O)c1cccc(-c2nc(N)c3cc(CN4CCC(F)CC4)sc3n2)c1 10.1039/C1MD00082A
CHEMBL3217879 109306 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 413 4 1 6 3.6 CN(C)C(=O)c1cccc(-c2nc(N)c3cc(CN4CCC(F)CC4)sc3n2)c1 10.1039/C1MD00082A
50899648 18212 None 1 Rat Functional pKi = 7.6 7.6 - 0
Antagonist activity at rat A2A receptor by cAMP functional assayAntagonist activity at rat A2A receptor by cAMP functional assay
ChEMBL 420 8 1 7 2.7 CCN(C)C(=O)c1ccc2nc(NC(=O)c3cccc(C#N)c3)n(CCCOC)c2n1 10.1016/j.bmcl.2010.08.064
CHEMBL1270008 18212 None 1 Rat Functional pKi = 7.6 7.6 - 0
Antagonist activity at rat A2A receptor by cAMP functional assayAntagonist activity at rat A2A receptor by cAMP functional assay
ChEMBL 420 8 1 7 2.7 CCN(C)C(=O)c1ccc2nc(NC(=O)c3cccc(C#N)c3)n(CCCOC)c2n1 10.1016/j.bmcl.2010.08.064
46888880 8568 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 411 4 1 6 3.5 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(N3CCN(CC4CC4)CC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1094547 8568 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 411 4 1 6 3.5 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(N3CCN(CC4CC4)CC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
44218166 61022 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 539 6 1 10 2.6 Nc1nc2c(cnn2CCN2CCN(c3ccc(F)cc3F)CC2)c2nn(Cc3cccc(Cl)c3)c(=O)n12 10.1016/j.bmcl.2011.02.045
CHEMBL1762633 61022 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 539 6 1 10 2.6 Nc1nc2c(cnn2CCN2CCN(c3ccc(F)cc3F)CC2)c2nn(Cc3cccc(Cl)c3)c(=O)n12 10.1016/j.bmcl.2011.02.045
9912816 98487 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 475 10 2 7 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL275605 98487 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 475 10 2 7 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
45279728 109631 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 328 3 1 7 2.7 Nc1nc(-c2ccco2)nc2sc(CN3CCC(=O)CC3)cc12 10.1039/C1MD00082A
CHEMBL3222064 109631 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 328 3 1 7 2.7 Nc1nc(-c2ccco2)nc2sc(CN3CCC(=O)CC3)cc12 10.1039/C1MD00082A
2519 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
2519.0 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
407 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
463 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
CHEMBL113 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
DB00201 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
2519 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmcl.2013.03.070
2519.0 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmcl.2013.03.070
407 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmcl.2013.03.070
463 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmcl.2013.03.070
CHEMBL113 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmcl.2013.03.070
DB00201 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmcl.2013.03.070
2519 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm4011669
2519.0 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm4011669
407 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm4011669
463 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm4011669
CHEMBL113 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm4011669
DB00201 779 None 49 Human Functional pKi = 4.6 4.6 -19498 8
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm4011669
541903 57964 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 382 8 2 7 1.4 C=CCn1c(=O)c2nc(-c3ccc(OCC(=O)O)cc3)[nH]c2n(CC=C)c1=O 10.1021/jm990421v
CHEMBL16724 57964 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 382 8 2 7 1.4 C=CCn1c(=O)c2nc(-c3ccc(OCC(=O)O)cc3)[nH]c2n(CC=C)c1=O 10.1021/jm990421v
10792296 98719 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 529 9 2 7 4.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(F)(F)F)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL277386 98719 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 529 9 2 7 4.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(F)(F)F)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
45278622 109666 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 299 3 1 7 2.3 Nc1nc(-c2cocn2)nc2sc(CN3CC=CC3)cc12 10.1039/C1MD00082A
CHEMBL3222100 109666 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 299 3 1 7 2.3 Nc1nc(-c2cocn2)nc2sc(CN3CC=CC3)cc12 10.1039/C1MD00082A
137650223 157353 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 464 6 1 8 3.6 COc1cnc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)c(F)c3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4076650 157353 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 464 6 1 8 3.6 COc1cnc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)c(F)c3)nc12 10.1021/acs.jmedchem.6b01584
52940875 18307 None 0 Rat Functional pKi = 7.6 7.6 - 0
Antagonist activity at rat A2A receptor by cAMP functional assayAntagonist activity at rat A2A receptor by cAMP functional assay
ChEMBL 420 8 1 7 2.7 CCN(C)C(=O)c1cnc2c(c1)nc(NC(=O)c1cccc(C#N)c1)n2CCCOC 10.1016/j.bmcl.2010.08.064
CHEMBL1270610 18307 None 0 Rat Functional pKi = 7.6 7.6 - 0
Antagonist activity at rat A2A receptor by cAMP functional assayAntagonist activity at rat A2A receptor by cAMP functional assay
ChEMBL 420 8 1 7 2.7 CCN(C)C(=O)c1cnc2c(c1)nc(NC(=O)c1cccc(C#N)c1)n2CCCOC 10.1016/j.bmcl.2010.08.064
90668275 109657 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 299 3 1 7 2.3 Nc1nc(-c2ncco2)nc2sc(CN3CC=CC3)cc12 10.1039/C1MD00082A
CHEMBL3222091 109657 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 299 3 1 7 2.3 Nc1nc(-c2ncco2)nc2sc(CN3CC=CC3)cc12 10.1039/C1MD00082A
90668276 109658 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 313 3 1 7 2.7 Nc1nc(-c2ncco2)nc2sc(CN3CC=CCC3)cc12 10.1039/C1MD00082A
CHEMBL3222092 109658 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 313 3 1 7 2.7 Nc1nc(-c2ncco2)nc2sc(CN3CC=CCC3)cc12 10.1039/C1MD00082A
45278623 109667 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 313 3 1 7 2.7 Nc1nc(-c2cocn2)nc2sc(CN3CC=CCC3)cc12 10.1039/C1MD00082A
CHEMBL3222101 109667 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 313 3 1 7 2.7 Nc1nc(-c2cocn2)nc2sc(CN3CC=CCC3)cc12 10.1039/C1MD00082A
823558 15250 None 7 Rat Functional pKi = 5.6 5.6 - 0
Antagonist activity against rat adenosine A2A receptorAntagonist activity against rat adenosine A2A receptor
ChEMBL 271 2 2 6 0.8 COc1ccc2c(C)nc(NC3=NCC(=O)N3)nc2c1 10.1016/j.ejmech.2010.04.039
CHEMBL1210817 15250 None 7 Rat Functional pKi = 5.6 5.6 - 0
Antagonist activity against rat adenosine A2A receptorAntagonist activity against rat adenosine A2A receptor
ChEMBL 271 2 2 6 0.8 COc1ccc2c(C)nc(NC3=NCC(=O)N3)nc2c1 10.1016/j.ejmech.2010.04.039
22252243 110839 None 0 Human Functional pKi = 7.6 7.6 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 438 5 1 8 3.2 COc1ccc(C2CCOCC2)c2oc(NC(=O)c3ccnc(N4CCOCC4)c3)nc12 10.1021/jm4011669
CHEMBL3260725 110839 None 0 Human Functional pKi = 7.6 7.6 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 438 5 1 8 3.2 COc1ccc(C2CCOCC2)c2oc(NC(=O)c3ccnc(N4CCOCC4)c3)nc12 10.1021/jm4011669
10193 3010 None 42 Human Functional pKi = 7.6 7.6 56 2
cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 nan
53466958 3010 None 42 Human Functional pKi = 7.6 7.6 56 2
cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 nan
53466958.0 3010 None 42 Human Functional pKi = 7.6 7.6 56 2
cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 nan
CHEMBL3638684 3010 None 42 Human Functional pKi = 7.6 7.6 56 2
cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 nan
CHEMBL3694769 3010 None 42 Human Functional pKi = 7.6 7.6 56 2
cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 nan
45279356 109637 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 370 4 1 6 4.9 CCc1ccc(-c2nc(N)c3cc(CN4[C@@H](C)CCC[C@H]4C)sc3n2)o1 10.1039/C1MD00082A
CHEMBL3222070 109637 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 370 4 1 6 4.9 CCc1ccc(-c2nc(N)c3cc(CN4[C@@H](C)CCC[C@H]4C)sc3n2)o1 10.1039/C1MD00082A
45274431 89816 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 357 4 1 5 5.1 Nc1nc(-c2ccc(C(F)F)o2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
CHEMBL2377225 89816 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 357 4 1 5 5.1 Nc1nc(-c2ccc(C(F)F)o2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
9825550 57609 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 461 9 2 7 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16677 57609 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 461 9 2 7 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
9912816 98487 None 0 Rat Functional pKi = 7.6 7.6 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 475 10 2 7 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL275605 98487 None 0 Rat Functional pKi = 7.6 7.6 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 475 10 2 7 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
45279451 109659 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 333 3 1 8 2.2 Nc1nc(-c2nccs2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
CHEMBL3222093 109659 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 333 3 1 8 2.2 Nc1nc(-c2nccs2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
135109 9211 None 3 Guinea pig Functional pKi = 5.6 5.6 - 1
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 300 2 2 6 0.3 Cn1c(=O)c2nc(-c3ccc(C(=O)O)cc3)[nH]c2n(C)c1=O 10.1021/jm00382a018
CHEMBL11048 9211 None 3 Guinea pig Functional pKi = 5.6 5.6 - 1
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 300 2 2 6 0.3 Cn1c(=O)c2nc(-c3ccc(C(=O)O)cc3)[nH]c2n(C)c1=O 10.1021/jm00382a018
3288 1855 None 34 Human Functional pKi = 4.6 4.6 - 1
Agonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cells
ChEMBL 351 4 5 10 -1.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H]1CCC[C@@H]1O 10.1007/s00044-004-0013-y
9884817 1855 None 34 Human Functional pKi = 4.6 4.6 - 1
Agonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cells
ChEMBL 351 4 5 10 -1.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H]1CCC[C@@H]1O 10.1007/s00044-004-0013-y
CHEMBL2163568 1855 None 34 Human Functional pKi = 4.6 4.6 - 1
Agonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cells
ChEMBL 351 4 5 10 -1.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H]1CCC[C@@H]1O 10.1007/s00044-004-0013-y
10387088 59474 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 414 10 2 7 2.6 CCCCn1c(=O)c2nc(-c3ccc(OCC(=O)O)cc3)[nH]c2n(CCCC)c1=O 10.1021/jm990421v
CHEMBL17123 59474 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 414 10 2 7 2.6 CCCCn1c(=O)c2nc(-c3ccc(OCC(=O)O)cc3)[nH]c2n(CCCC)c1=O 10.1021/jm990421v
45274224 89799 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 343 3 1 6 3.8 N#Cc1cccc(-c2nc(N)c3cc(Cc4ccccc4)sc3n2)n1 10.1016/j.bmcl.2013.02.078
CHEMBL2377105 89799 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 343 3 1 6 3.8 N#Cc1cccc(-c2nc(N)c3cc(Cc4ccccc4)sc3n2)n1 10.1016/j.bmcl.2013.02.078
45279637 109619 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 314 3 1 6 3.4 Cc1ccc(-c2nc(N)c3cc(CN4CCCC4)sc3n2)o1 10.1039/C1MD00082A
CHEMBL3222052 109619 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 314 3 1 6 3.4 Cc1ccc(-c2nc(N)c3cc(CN4CCCC4)sc3n2)o1 10.1039/C1MD00082A
CHEMBL5080823 217195 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCn1c(=O)c2nc(C34CCC(C(=O)NCCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
137659296 159383 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 464 6 1 8 3.6 COc1cnc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3c(F)cccc3F)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4099543 159383 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 464 6 1 8 3.6 COc1cnc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3c(F)cccc3F)nc12 10.1021/acs.jmedchem.6b01584
45275824 89814 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 347 4 1 5 5.0 Nc1nc(-c2ccc(C3CC3)o2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
CHEMBL2377223 89814 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 347 4 1 5 5.0 Nc1nc(-c2ccc(C3CC3)o2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
44218167 61026 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 271 3 1 8 0.3 C=Cn1ncc2c1nc(N)n1c(=O)n(CC3CC3)nc21 10.1016/j.bmcl.2011.02.045
CHEMBL1762638 61026 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 271 3 1 8 0.3 C=Cn1ncc2c1nc(N)n1c(=O)n(CC3CC3)nc21 10.1016/j.bmcl.2011.02.045
90668272 109621 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 328 3 1 6 3.9 Nc1nc(-c2ccco2)nc2sc(CN3CCCCCC3)cc12 10.1039/C1MD00082A
CHEMBL3222054 109621 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 328 3 1 6 3.9 Nc1nc(-c2ccco2)nc2sc(CN3CCCCCC3)cc12 10.1039/C1MD00082A
169317 1201 None 26 Guinea pig Functional pKi = 5.6 5.6 - 2
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 10.1021/jm00382a018
427 1201 None 26 Guinea pig Functional pKi = 5.6 5.6 - 2
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 10.1021/jm00382a018
CHEMBL157655 1201 None 26 Guinea pig Functional pKi = 5.6 5.6 - 2
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 10.1021/jm00382a018
169317 1201 None 26 Guinea pig Functional pKi = 5.6 5.6 - 2
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 10.1021/jm00157a035
427 1201 None 26 Guinea pig Functional pKi = 5.6 5.6 - 2
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 10.1021/jm00157a035
CHEMBL157655 1201 None 26 Guinea pig Functional pKi = 5.6 5.6 - 2
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 10.1021/jm00157a035
12295531 78228 None 3 Guinea pig Functional pKi = 4.6 4.6 - 0
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 270 1 0 6 0.6 Cn1c(=O)c2c(nc(-c3ccccc3)n2C)n(C)c1=O 10.1021/jm00382a018
CHEMBL21053 78228 None 3 Guinea pig Functional pKi = 4.6 4.6 - 0
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 270 1 0 6 0.6 Cn1c(=O)c2c(nc(-c3ccccc3)n2C)n(C)c1=O 10.1021/jm00382a018
12295531 78228 None 3 Guinea pig Functional pKi = 4.6 4.6 - 0
Antagonist activity at adenosine receptor A2A in [3H]-adenine-labeled guinea pig cerebral cortical slices assessed as inhibition of 2-chloroadenosine-mediated [3H]cAMP accumulationAntagonist activity at adenosine receptor A2A in [3H]-adenine-labeled guinea pig cerebral cortical slices assessed as inhibition of 2-chloroadenosine-mediated [3H]cAMP accumulation
ChEMBL 270 1 0 6 0.6 Cn1c(=O)c2c(nc(-c3ccccc3)n2C)n(C)c1=O 10.1016/j.bmcl.2016.10.086
CHEMBL21053 78228 None 3 Guinea pig Functional pKi = 4.6 4.6 - 0
Antagonist activity at adenosine receptor A2A in [3H]-adenine-labeled guinea pig cerebral cortical slices assessed as inhibition of 2-chloroadenosine-mediated [3H]cAMP accumulationAntagonist activity at adenosine receptor A2A in [3H]-adenine-labeled guinea pig cerebral cortical slices assessed as inhibition of 2-chloroadenosine-mediated [3H]cAMP accumulation
ChEMBL 270 1 0 6 0.6 Cn1c(=O)c2c(nc(-c3ccccc3)n2C)n(C)c1=O 10.1016/j.bmcl.2016.10.086
21916394 160907 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 458 6 1 7 3.2 CCn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc21 10.1016/j.ejmech.2010.04.039
CHEMBL411452 160907 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 458 6 1 7 3.2 CCn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc21 10.1016/j.ejmech.2010.04.039
9850900 98404 None 0 Rat Functional pKi = 5.6 5.6 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 565 12 1 7 5.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(Cc4ccccc4)Cc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL275149 98404 None 0 Rat Functional pKi = 5.6 5.6 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 565 12 1 7 5.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(Cc4ccccc4)Cc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
137656746 159696 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 502 10 1 10 3.4 COCCOc1cccc(OC(C)(C)C(=O)Nc2nc3c(OC)cnc(N4CCOCC4)c3s2)c1 10.1021/acs.jmedchem.6b01584
CHEMBL4103199 159696 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 502 10 1 10 3.4 COCCOc1cccc(OC(C)(C)C(=O)Nc2nc3c(OC)cnc(N4CCOCC4)c3s2)c1 10.1021/acs.jmedchem.6b01584
45279541 109618 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 300 3 1 6 3.1 Nc1nc(-c2ccco2)nc2sc(CN3CCCC3)cc12 10.1039/C1MD00082A
CHEMBL3222051 109618 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 300 3 1 6 3.1 Nc1nc(-c2ccco2)nc2sc(CN3CCCC3)cc12 10.1039/C1MD00082A
44218168 61017 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 477 6 1 11 0.7 Nc1nc2c(cnn2CCN2CCC(N3CCOCC3)CC2)c2nn(Cc3ccccc3)c(=O)n12 10.1016/j.bmcl.2011.02.045
CHEMBL1762626 61017 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 477 6 1 11 0.7 Nc1nc2c(cnn2CCN2CCC(N3CCOCC3)CC2)c2nn(Cc3ccccc3)c(=O)n12 10.1016/j.bmcl.2011.02.045
46889174 7657 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 429 5 2 7 2.0 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(C(=O)NCCN3CCOCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1088393 7657 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 429 5 2 7 2.0 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(C(=O)NCCN3CCOCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
45278948 109642 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 392 4 1 6 5.2 C[C@H]1CCC[C@@H](C)N1Cc1cc2c(N)nc(-c3ccc(C(F)F)o3)nc2s1 10.1039/C1MD00082A
CHEMBL3222076 109642 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 392 4 1 6 5.2 C[C@H]1CCC[C@@H](C)N1Cc1cc2c(N)nc(-c3ccc(C(F)F)o3)nc2s1 10.1039/C1MD00082A
45279632 109620 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 328 3 1 6 3.8 Cc1ccc(-c2nc(N)c3cc(CN4CCCCC4)sc3n2)o1 10.1039/C1MD00082A
CHEMBL3222053 109620 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 328 3 1 6 3.8 Cc1ccc(-c2nc(N)c3cc(CN4CCCCC4)sc3n2)o1 10.1039/C1MD00082A
44274635 93239 None 0 Guinea pig Functional pKi = 5.6 5.6 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 260 3 0 6 0.2 C#CCn1cnc2c1c(=O)n(C)c(=O)n2CC(C)C 10.1021/jm00157a035
CHEMBL24444 93239 None 0 Guinea pig Functional pKi = 5.6 5.6 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 260 3 0 6 0.2 C#CCn1cnc2c1c(=O)n(C)c(=O)n2CC(C)C 10.1021/jm00157a035
45279725 109622 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 316 3 1 7 2.4 Nc1nc(-c2ccco2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
CHEMBL3222055 109622 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 316 3 1 7 2.4 Nc1nc(-c2ccco2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
45279725 109622 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human recombinant adenosine receptor A2a by cAMP assayAntagonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 316 3 1 7 2.4 Nc1nc(-c2ccco2)nc2sc(CN3CCOCC3)cc12 10.1021/jm4011669
CHEMBL3222055 109622 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human recombinant adenosine receptor A2a by cAMP assayAntagonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 316 3 1 7 2.4 Nc1nc(-c2ccco2)nc2sc(CN3CCOCC3)cc12 10.1021/jm4011669
46889095 7574 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 418 4 2 7 2.3 CN1CCN(NCc2ccc3c(c2)-c2nc(N)nc(-c4ccc(F)cc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.042
CHEMBL1087726 7574 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 418 4 2 7 2.3 CN1CCN(NCc2ccc3c(c2)-c2nc(N)nc(-c4ccc(F)cc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.042
45275058 89782 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 317 3 1 4 4.5 Nc1nc(-c2ccccc2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
CHEMBL2377088 89782 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 317 3 1 4 4.5 Nc1nc(-c2ccccc2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
46889069 7638 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 385 4 2 6 3.4 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CNN3CCCCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1088236 7638 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 385 4 2 6 3.4 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CNN3CCCCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.042
46846866 110844 None 0 Human Functional pKi = 8.5 8.5 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 414 4 0 7 3.0 COC[C@H]1CCCN1C(=O)c1ccc2c(-c3cnc4ccc(C#N)cn34)nn(C)c2c1 10.1021/jm4011669
CHEMBL3260730 110844 None 0 Human Functional pKi = 8.5 8.5 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 414 4 0 7 3.0 COC[C@H]1CCCN1C(=O)c1ccc2c(-c3cnc4ccc(C#N)cn34)nn(C)c2c1 10.1021/jm4011669
56954333 82137 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 382 3 1 5 4.1 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CN3C4CCC3CC4)ccc1C2=O 10.1021/jm201640m
CHEMBL2165806 82137 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 382 3 1 5 4.1 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CN3C4CCC3CC4)ccc1C2=O 10.1021/jm201640m
10310914 179023 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 475 8 1 12 1.8 COCCOc1cnc2c(c1)CN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1016/j.bmcl.2008.05.069
CHEMBL470089 179023 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 475 8 1 12 1.8 COCCOc1cnc2c(c1)CN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1016/j.bmcl.2008.05.069
46888850 8709 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 449 5 2 8 2.1 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(NCCN3CCS(=O)(=O)CC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1095811 8709 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 449 5 2 8 2.1 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(NCCN3CCS(=O)(=O)CC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
10127218 178969 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 430 5 1 10 2.4 COc1ccc2c(c1)CN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1016/j.bmcl.2008.05.069
CHEMBL469674 178969 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 430 5 1 10 2.4 COc1ccc2c(c1)CN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1016/j.bmcl.2008.05.069
46861768 7540 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 372 3 1 6 2.8 Nc1nc(-c2ccccc2)c2c(n1)-c1c(CN3CCOCC3)cccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1087462 7540 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 372 3 1 6 2.8 Nc1nc(-c2ccccc2)c2c(n1)-c1c(CN3CCOCC3)cccc1C2=O 10.1016/j.bmcl.2010.03.042
10216962 189487 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 448 4 1 9 3.1 Nc1nc2c(cnn2CCN2CCc3ccc(Cl)cc3CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
CHEMBL512892 189487 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 448 4 1 9 3.1 Nc1nc2c(cnn2CCN2CCc3ccc(Cl)cc3CC2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
10190 935 None 41 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1016/j.ejmech.2021.113907
44537963 935 None 41 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1016/j.ejmech.2021.113907
44537963.0 935 None 41 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1016/j.ejmech.2021.113907
CHEMBL4297184 935 None 41 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1016/j.ejmech.2021.113907
DB16125 935 None 41 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1016/j.ejmech.2021.113907
137645935 157668 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assayAntagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assay
ChEMBL 446 6 1 8 3.5 COc1cnc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3)nc12 10.1016/j.ejmech.2021.113907
CHEMBL4080594 157668 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assayAntagonist activity at recombinant human adenosine A2A receptor expressed in HEK293 cells measured by cAMP functional assay
ChEMBL 446 6 1 8 3.5 COc1cnc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3)nc12 10.1016/j.ejmech.2021.113907
56964225 74318 None 0 Human Functional pKi = 8.5 8.5 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 331 2 1 5 3.5 Cc1cc(-c2nnc(N)nc2-c2ccccc2)cc(C(F)(F)F)n1 10.1021/jm4011669
CHEMBL2024119 74318 None 0 Human Functional pKi = 8.5 8.5 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 331 2 1 5 3.5 Cc1cc(-c2nnc(N)nc2-c2ccccc2)cc(C(F)(F)F)n1 10.1021/jm4011669
46861770 7570 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 374 3 1 5 3.7 Nc1nc(-c2ccc(F)cc2)c2c(n1)-c1c(CN3CCCC3)cccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1087710 7570 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 374 3 1 5 3.7 Nc1nc(-c2ccc(F)cc2)c2c(n1)-c1c(CN3CCCC3)cccc1C2=O 10.1016/j.bmcl.2010.03.042
44438088 93618 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 513 9 1 11 2.6 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccccc5)nc43)CC2)cc1 10.1016/j.bmcl.2006.12.104
CHEMBL246468 93618 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 513 9 1 11 2.6 COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccccc5)nc43)CC2)cc1 10.1016/j.bmcl.2006.12.104
71602913 89805 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 339 3 1 5 4.6 Cc1ccc(-c2nc(N)c3cc(Cc4ccccc4F)sc3n2)o1 10.1016/j.bmcl.2013.02.078
CHEMBL2377111 89805 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 339 3 1 5 4.6 Cc1ccc(-c2nc(N)c3cc(Cc4ccccc4F)sc3n2)o1 10.1016/j.bmcl.2013.02.078
46889019 7541 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 390 3 1 6 2.9 Nc1nc(-c2ccc(F)cc2)c2c(n1)-c1c(CN3CCOCC3)cccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1087463 7541 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 390 3 1 6 2.9 Nc1nc(-c2ccc(F)cc2)c2c(n1)-c1c(CN3CCOCC3)cccc1C2=O 10.1016/j.bmcl.2010.03.042
56944261 164248 None 0 Rat Functional pKi = 8.4 8.4 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 533 9 1 13 1.5 COCCOc1cccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c1 10.1021/acsmedchemlett.7b00175
CHEMBL4210241 164248 None 0 Rat Functional pKi = 8.4 8.4 - 0
Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assayAntagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition measured after 30 mins by HTRF assay
ChEMBL 533 9 1 13 1.5 COCCOc1cccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5ccco5)nc43)CC2)c1 10.1021/acsmedchemlett.7b00175
45279274 109654 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 394 3 1 7 3.1 Nc1nc(-c2ccc(Br)o2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
CHEMBL3222088 109654 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 394 3 1 7 3.1 Nc1nc(-c2ccc(Br)o2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
45278949 109641 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 366 4 1 7 3.3 Nc1nc(-c2ccc(C(F)F)o2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
CHEMBL3222075 109641 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 366 4 1 7 3.3 Nc1nc(-c2ccc(C(F)F)o2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
128784 51818 None 33 Guinea pig Functional pKi = 6.5 6.5 - 1
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 312 5 1 5 2.4 CCCn1c(=O)c2nc(-c3ccccc3)[nH]c2n(CCC)c1=O 10.1021/jm00382a018
CHEMBL158507 51818 None 33 Guinea pig Functional pKi = 6.5 6.5 - 1
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 312 5 1 5 2.4 CCCn1c(=O)c2nc(-c3ccccc3)[nH]c2n(CCC)c1=O 10.1021/jm00382a018
45278697 109307 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 372 4 1 6 3.9 COc1cccc(-c2nc(N)c3cc(CN4CCC(F)CC4)sc3n2)c1 10.1039/C1MD00082A
CHEMBL3217880 109307 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 372 4 1 6 3.9 COc1cccc(-c2nc(N)c3cc(CN4CCC(F)CC4)sc3n2)c1 10.1039/C1MD00082A
45279825 109630 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 330 3 2 7 2.5 Nc1nc(-c2ccco2)nc2sc(CN3CCC(O)CC3)cc12 10.1039/C1MD00082A
CHEMBL3222063 109630 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 330 3 2 7 2.5 Nc1nc(-c2ccco2)nc2sc(CN3CCC(O)CC3)cc12 10.1039/C1MD00082A
45275819 89815 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 332 3 1 6 4.0 N#Cc1ccc(-c2nc(N)c3cc(Cc4ccccc4)sc3n2)o1 10.1016/j.bmcl.2013.02.078
CHEMBL2377224 89815 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 332 3 1 6 4.0 N#Cc1ccc(-c2nc(N)c3cc(Cc4ccccc4)sc3n2)o1 10.1016/j.bmcl.2013.02.078
45275714 89826 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 350 3 1 6 4.8 C=C(c1ccccc1)c1cc2c(N)nc(-c3nc(C)cs3)nc2s1 10.1016/j.bmcl.2013.02.078
CHEMBL2377235 89826 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 350 3 1 6 4.8 C=C(c1ccccc1)c1cc2c(N)nc(-c3nc(C)cs3)nc2s1 10.1016/j.bmcl.2013.02.078
CHEMBL5074992 216838 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCCn1c(=O)c2nc(C34CCC(C(=O)NCCOCCOCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
9936467 58109 None 1 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity against human adenosine A2A receptor expressed in HEK293 cells using [125 I]indo-ZM-241385Antagonist activity against human adenosine A2A receptor expressed in HEK293 cells using [125 I]indo-ZM-241385
ChEMBL 519 10 2 9 3.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)OC)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16741 58109 None 1 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity against human adenosine A2A receptor expressed in HEK293 cells using [125 I]indo-ZM-241385Antagonist activity against human adenosine A2A receptor expressed in HEK293 cells using [125 I]indo-ZM-241385
ChEMBL 519 10 2 9 3.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)OC)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
24827444 96397 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 365 5 1 8 1.6 CCCn1c(=O)c2[nH]c(-c3cnn(-c4cccnc4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL261526 96397 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 365 5 1 8 1.6 CCCn1c(=O)c2[nH]c(-c3cnn(-c4cccnc4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2010.04.039
46889230 7491 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 431 3 1 6 2.9 CCN1CCN(C(=O)c2ccc3c(c2)-c2nc(N)nc(-c4ccc(F)cc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
CHEMBL1087085 7491 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 431 3 1 6 2.9 CCN1CCN(C(=O)c2ccc3c(c2)-c2nc(N)nc(-c4ccc(F)cc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
46888987 7590 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 303 2 1 5 2.9 COc1ccccc1-c1nc(N)nc2c1C(=O)c1ccccc1-2 10.1016/j.bmcl.2010.03.042
CHEMBL1087869 7590 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 303 2 1 5 2.9 COc1ccccc1-c1nc(N)nc2c1C(=O)c1ccccc1-2 10.1016/j.bmcl.2010.03.042
46889207 7511 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 385 2 2 6 2.0 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(C(=O)N3CCNCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1087184 7511 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 385 2 2 6 2.0 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(C(=O)N3CCNCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
45279636 109623 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 330 3 1 7 2.7 Cc1ccc(-c2nc(N)c3cc(CN4CCOCC4)sc3n2)o1 10.1039/C1MD00082A
CHEMBL3222056 109623 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 330 3 1 7 2.7 Cc1ccc(-c2nc(N)c3cc(CN4CCOCC4)sc3n2)o1 10.1039/C1MD00082A
450 2970 None 7 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1016/j.ejmech.2010.04.039
454 2970 None 7 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1016/j.ejmech.2010.04.039
5311041 2970 None 7 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1016/j.ejmech.2010.04.039
CHEMBL485862 2970 None 7 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1016/j.ejmech.2010.04.039
45278866 109647 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 362 3 1 6 4.6 Nc1nc(-c2ccc(Cl)o2)nc2sc(CN3CCCCCC3)cc12 10.1039/C1MD00082A
CHEMBL3222081 109647 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 362 3 1 6 4.6 Nc1nc(-c2ccc(Cl)o2)nc2sc(CN3CCCCCC3)cc12 10.1039/C1MD00082A
101420 162133 None 11 Guinea pig Functional pKi = 5.5 5.5 - 1
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 208 2 1 5 -0.1 CCn1c(=O)c2nc[nH]c2n(CC)c1=O 10.1021/jm00157a035
CHEMBL416013 162133 None 11 Guinea pig Functional pKi = 5.5 5.5 - 1
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 208 2 1 5 -0.1 CCn1c(=O)c2nc[nH]c2n(CC)c1=O 10.1021/jm00157a035
45275170 89788 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 356 3 1 5 5.0 CC(c1ccccc1)c1cc2c(N)nc(-c3cccc(C#N)c3)nc2s1 10.1016/j.bmcl.2013.02.078
CHEMBL2377094 89788 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 356 3 1 5 5.0 CC(c1ccccc1)c1cc2c(N)nc(-c3cccc(C#N)c3)nc2s1 10.1016/j.bmcl.2013.02.078
46888821 8603 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 430 5 1 6 4.1 Nc1nc(-c2ccc(F)cc2)c2c(n1)-c1cc(OCCN3C4CCC3CC4)ccc1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1094846 8603 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 430 5 1 6 4.1 Nc1nc(-c2ccc(F)cc2)c2c(n1)-c1cc(OCCN3C4CCC3CC4)ccc1C2=O 10.1016/j.bmcl.2010.03.024
46888782 8662 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 400 5 1 6 3.8 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(OCCN3CCCCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1095487 8662 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 400 5 1 6 3.8 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(OCCN3CCCCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
45278535 109668 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 382 3 1 6 4.6 Nc1nc(-c2cc3ccccc3o2)nc2sc(CN3CCC(F)CC3)cc12 10.1039/C1MD00082A
CHEMBL3222102 109668 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 382 3 1 6 4.6 Nc1nc(-c2cc3ccccc3o2)nc2sc(CN3CCC(F)CC3)cc12 10.1039/C1MD00082A
45279730 109672 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 362 3 1 6 3.1 Nc1nc(-c2cc(F)cc(F)c2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
CHEMBL3222106 109672 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 362 3 1 6 3.1 Nc1nc(-c2cc(F)cc(F)c2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
5353365 1210 None 25 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against adenosine A2 receptorAntagonist activity against adenosine A2 receptor
ChEMBL 330 2 0 6 1.8 Clc1cccc(c1)/C=C/c1nc2c(n1C)c(=O)n(c(=O)n2C)C 10.1021/jm7009364
5609 1210 None 25 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against adenosine A2 receptorAntagonist activity against adenosine A2 receptor
ChEMBL 330 2 0 6 1.8 Clc1cccc(c1)/C=C/c1nc2c(n1C)c(=O)n(c(=O)n2C)C 10.1021/jm7009364
CHEMBL26138 1210 None 25 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against adenosine A2 receptorAntagonist activity against adenosine A2 receptor
ChEMBL 330 2 0 6 1.8 Clc1cccc(c1)/C=C/c1nc2c(n1C)c(=O)n(c(=O)n2C)C 10.1021/jm7009364
45279542 109616 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 286 4 2 6 2.8 Nc1nc(-c2ccco2)nc2sc(CNC3CC3)cc12 10.1039/C1MD00082A
CHEMBL3222049 109616 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 286 4 2 6 2.8 Nc1nc(-c2ccco2)nc2sc(CNC3CC3)cc12 10.1039/C1MD00082A
45278700 109675 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 351 3 1 7 2.6 N#Cc1cccc(-c2nc(N)c3cc(CN4CCOCC4)sc3n2)c1 10.1039/C1MD00082A
CHEMBL3222109 109675 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 351 3 1 7 2.6 N#Cc1cccc(-c2nc(N)c3cc(CN4CCOCC4)sc3n2)c1 10.1039/C1MD00082A
CHEMBL5088372 217645 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCCn1c(=O)c2nc(C34CCC(C(=O)NCCOCCOCCOCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
45278864 109649 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 366 3 1 6 4.1 Nc1nc(-c2ccc(Cl)o2)nc2sc(CN3CCC(F)CC3)cc12 10.1039/C1MD00082A
CHEMBL3222083 109649 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 366 3 1 6 4.1 Nc1nc(-c2ccc(Cl)o2)nc2sc(CN3CCC(F)CC3)cc12 10.1039/C1MD00082A
45278701 109656 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 317 3 1 8 1.8 Nc1nc(-c2ncco2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
CHEMBL3222090 109656 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 317 3 1 8 1.8 Nc1nc(-c2ncco2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
45279823 109673 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 362 3 1 6 3.1 Nc1nc(-c2ccc(F)c(F)c2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
CHEMBL3222107 109673 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 362 3 1 6 3.1 Nc1nc(-c2ccc(F)c(F)c2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
46889253 7607 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 378 5 1 6 3.0 CN(C)CCOc1ccc2c(c1)-c1nc(N)nc(-c3ccc(F)cc3)c1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1087998 7607 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 378 5 1 6 3.0 CN(C)CCOc1ccc2c(c1)-c1nc(N)nc(-c3ccc(F)cc3)c1C2=O 10.1016/j.bmcl.2010.03.024
45278785 109308 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 356 4 1 7 2.8 COc1cccc(-c2nc(N)c3cc(CN4CCOCC4)sc3n2)c1 10.1039/C1MD00082A
CHEMBL3217881 109308 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 356 4 1 7 2.8 COc1cccc(-c2nc(N)c3cc(CN4CCOCC4)sc3n2)c1 10.1039/C1MD00082A
90665317 109305 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 387 4 1 7 3.8 Nc1nc(-c2cccc([N+](=O)[O-])c2)nc2sc(CN3CCC(F)CC3)cc12 10.1039/C1MD00082A
CHEMBL3217878 109305 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 387 4 1 7 3.8 Nc1nc(-c2cccc([N+](=O)[O-])c2)nc2sc(CN3CCC(F)CC3)cc12 10.1039/C1MD00082A
CHEMBL5073669 216789 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCCn1c(=O)c2nc(C34CCC(C(=O)NCCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
44218330 61028 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 358 5 1 10 -0.4 Nc1nc2c(cnn2CCN2CCOCC2)c2nn(CC3CC3)c(=O)n12 10.1016/j.bmcl.2011.02.045
CHEMBL1762640 61028 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 358 5 1 10 -0.4 Nc1nc2c(cnn2CCN2CCOCC2)c2nn(CC3CC3)c(=O)n12 10.1016/j.bmcl.2011.02.045
9935943 59042 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 505 10 3 8 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16931 59042 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 505 10 3 8 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
9827467 98440 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 504 10 3 8 2.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(N)=O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL275360 98440 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 504 10 3 8 2.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(N)=O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
45278538 109292 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 385 3 1 6 4.0 N#Cc1cccc(-c2nc(N)c3cc(CN4CCCC(F)(F)C4)sc3n2)c1 10.1039/C1MD00082A
CHEMBL3217864 109292 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 385 3 1 6 4.0 N#Cc1cccc(-c2nc(N)c3cc(CN4CCCC(F)(F)C4)sc3n2)c1 10.1039/C1MD00082A
45278619 109299 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 367 3 1 6 3.7 N#Cc1ccc(-c2nc(N)c3cc(CN4CCC(F)CC4)sc3n2)cc1 10.1039/C1MD00082A
CHEMBL3217870 109299 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 367 3 1 6 3.7 N#Cc1ccc(-c2nc(N)c3cc(CN4CCC(F)CC4)sc3n2)cc1 10.1039/C1MD00082A
135566609 74314 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 298 2 2 5 3.1 Nc1nnc(-c2ccc(O)c(Cl)c2)c(-c2ccccc2)n1 10.1016/j.ejmech.2017.12.007
CHEMBL2024114 74314 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 298 2 2 5 3.1 Nc1nnc(-c2ccc(O)c(Cl)c2)c(-c2ccccc2)n1 10.1016/j.ejmech.2017.12.007
9868615 66194 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 455 6 1 10 1.9 CN(CCN1CCN(c2ccc(F)cc2F)CC1)c1nc(N)n2nc(-c3ccco3)nc2n1 10.1016/j.ejmech.2022.114378
CHEMBL184309 66194 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 455 6 1 10 1.9 CN(CCN1CCN(c2ccc(F)cc2F)CC1)c1nc(N)n2nc(-c3ccco3)nc2n1 10.1016/j.ejmech.2022.114378
58522807 110845 None 4 Human Functional pKi = 8.4 8.4 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 378 2 0 5 4.3 O=C(c1ccc2c(-c3cnc4ccc(F)cn34)noc2c1)N1CCCCCC1 10.1021/jm4011669
CHEMBL3260731 110845 None 4 Human Functional pKi = 8.4 8.4 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 378 2 0 5 4.3 O=C(c1ccc2c(-c3cnc4ccc(F)cn34)noc2c1)N1CCCCCC1 10.1021/jm4011669
46863665 7513 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 356 3 1 5 3.5 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CN3CCCC3)ccc1C2=O 10.1021/jm100971t
CHEMBL1087189 7513 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 356 3 1 5 3.5 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CN3CCCC3)ccc1C2=O 10.1021/jm100971t
CHEMBL3217142 7513 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 356 3 1 5 3.5 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CN3CCCC3)ccc1C2=O 10.1021/jm100971t
46889125 9132 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 371 4 2 6 3.0 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CNN3CCCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1099368 9132 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 371 4 2 6 3.0 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CNN3CCCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.042
46863665 7513 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 356 3 1 5 3.5 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CN3CCCC3)ccc1C2=O 10.1021/jm201640m
CHEMBL1087189 7513 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 356 3 1 5 3.5 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CN3CCCC3)ccc1C2=O 10.1021/jm201640m
CHEMBL3217142 7513 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionAntagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP production
ChEMBL 356 3 1 5 3.5 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CN3CCCC3)ccc1C2=O 10.1021/jm201640m
44438075 153671 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 345 4 1 8 2.6 Nc1nc2c(ncn2CCc2ccccc2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
CHEMBL398046 153671 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 345 4 1 8 2.6 Nc1nc2c(ncn2CCc2ccccc2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
44560456 178998 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 400 4 1 9 2.4 Nc1nc2c(cnn2CCN2CCc3ccccc3C2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
CHEMBL469877 178998 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 400 4 1 9 2.4 Nc1nc2c(cnn2CCN2CCc3ccccc3C2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
46863665 7513 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human recombinant adenosine receptor A2a by cAMP assayAntagonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 356 3 1 5 3.5 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CN3CCCC3)ccc1C2=O 10.1021/jm4011669
CHEMBL1087189 7513 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human recombinant adenosine receptor A2a by cAMP assayAntagonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 356 3 1 5 3.5 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CN3CCCC3)ccc1C2=O 10.1021/jm4011669
CHEMBL3217142 7513 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human recombinant adenosine receptor A2a by cAMP assayAntagonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 356 3 1 5 3.5 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CN3CCCC3)ccc1C2=O 10.1021/jm4011669
137632333 156622 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 445 6 1 7 4.1 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4068032 156622 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 445 6 1 7 4.1 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3)nc12 10.1021/acs.jmedchem.6b01584
52942205 18229 None 0 Rat Functional pKi = 8.4 8.4 - 0
Antagonist activity at rat A2A receptor by cAMP functional assayAntagonist activity at rat A2A receptor by cAMP functional assay
ChEMBL 434 8 1 7 3.1 COCCCn1c(NC(=O)c2cccc(C#N)c2)nc2ccc(C(=O)N(C)C(C)C)nc21 10.1016/j.bmcl.2010.08.064
CHEMBL1270115 18229 None 0 Rat Functional pKi = 8.4 8.4 - 0
Antagonist activity at rat A2A receptor by cAMP functional assayAntagonist activity at rat A2A receptor by cAMP functional assay
ChEMBL 434 8 1 7 3.1 COCCCn1c(NC(=O)c2cccc(C#N)c2)nc2ccc(C(=O)N(C)C(C)C)nc21 10.1016/j.bmcl.2010.08.064
46861780 8642 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human recombinant adenosine receptor A2a by cAMP assayAntagonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 401 5 2 7 2.7 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(NCCN3CCOCC3)ccc1C2=O 10.1021/jm4011669
CHEMBL1095172 8642 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human recombinant adenosine receptor A2a by cAMP assayAntagonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 401 5 2 7 2.7 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(NCCN3CCOCC3)ccc1C2=O 10.1021/jm4011669
46861780 8642 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 401 5 2 7 2.7 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(NCCN3CCOCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1095172 8642 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 401 5 2 7 2.7 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(NCCN3CCOCC3)ccc1C2=O 10.1016/j.bmcl.2010.03.024
46888930 7475 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 274 1 1 5 2.3 Nc1nc(-c2ccncc2)c2c(n1)-c1ccccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1086977 7475 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 274 1 1 5 2.3 Nc1nc(-c2ccncc2)c2c(n1)-c1ccccc1C2=O 10.1016/j.bmcl.2010.03.042
44438078 93430 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 409 3 1 8 3.1 Nc1nc2c(ncn2Cc2ccccc2Br)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
CHEMBL245646 93430 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 409 3 1 8 3.1 Nc1nc2c(ncn2Cc2ccccc2Br)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
44438080 153716 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 399 3 1 8 3.4 Nc1nc2c(ncn2Cc2ccccc2C(F)(F)F)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
CHEMBL398083 153716 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 399 3 1 8 3.4 Nc1nc2c(ncn2Cc2ccccc2C(F)(F)F)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2006.12.104
137659423 159153 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 446 6 1 8 3.5 COc1cnc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3cccc(F)c3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4097118 159153 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 446 6 1 8 3.5 COc1cnc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3cccc(F)c3)nc12 10.1021/acs.jmedchem.6b01584
71602915 89819 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 308 3 1 6 3.5 Nc1nc(-c2ncco2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
CHEMBL2377228 89819 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 308 3 1 6 3.5 Nc1nc(-c2ncco2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
46888822 9015 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 373 5 1 6 2.9 CN(C)CCN(C)c1ccc2c(c1)-c1nc(N)nc(-c3ccccc3)c1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1098457 9015 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 373 5 1 6 2.9 CN(C)CCN(C)c1ccc2c(c1)-c1nc(N)nc(-c3ccccc3)c1C2=O 10.1016/j.bmcl.2010.03.024
10150788 179176 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 401 4 1 10 1.8 Nc1nc2c(cnn2CCN2CCc3ncccc3C2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
CHEMBL471554 179176 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 401 4 1 10 1.8 Nc1nc2c(cnn2CCN2CCc3ncccc3C2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
46888852 8711 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 413 4 1 6 3.9 CCN1CCC(N(C)c2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
CHEMBL1095813 8711 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 413 4 1 6 3.9 CCN1CCC(N(C)c2ccc3c(c2)-c2nc(N)nc(-c4ccccc4)c2C3=O)CC1 10.1016/j.bmcl.2010.03.024
46888988 7564 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 387 6 1 6 2.9 CN(C)CCN(C)Cc1cccc2c1-c1nc(N)nc(-c3ccccc3)c1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1087699 7564 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 387 6 1 6 2.9 CN(C)CCN(C)Cc1cccc2c1-c1nc(N)nc(-c3ccccc3)c1C2=O 10.1016/j.bmcl.2010.03.042
45275719 89806 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 335 3 1 5 5.0 Cc1ccc(-c2nc(N)c3cc(C(C)c4ccccc4)sc3n2)o1 10.1016/j.bmcl.2013.02.078
CHEMBL2377112 89806 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 335 3 1 5 5.0 Cc1ccc(-c2nc(N)c3cc(C(C)c4ccccc4)sc3n2)o1 10.1016/j.bmcl.2013.02.078
49863226 15224 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 311 3 1 9 0.6 Nc1nc(-n2cncn2)c2nnn(Cc3ccccc3F)c2n1 10.1016/j.ejmech.2010.04.039
CHEMBL1210734 15224 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 311 3 1 9 0.6 Nc1nc(-n2cncn2)c2nnn(Cc3ccccc3F)c2n1 10.1016/j.ejmech.2010.04.039
11637638 94667 None 16 Guinea pig Functional pKi = 6.4 6.4 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 274 5 0 6 0.8 C#CCn1cnc2c1c(=O)n(CCC)c(=O)n2CCC 10.1021/jm00157a035
CHEMBL25223 94667 None 16 Guinea pig Functional pKi = 6.4 6.4 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 274 5 0 6 0.8 C#CCn1cnc2c1c(=O)n(CCC)c(=O)n2CCC 10.1021/jm00157a035
44459941 96751 None 2 Guinea pig Functional pKi = 5.4 5.4 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 246 4 0 6 0.3 C=CCn1c(=O)c2c(ncn2C)n(CC=C)c1=O 10.1021/jm00157a035
CHEMBL26406 96751 None 2 Guinea pig Functional pKi = 5.4 5.4 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 246 4 0 6 0.3 C=CCn1c(=O)c2c(ncn2C)n(CC=C)c1=O 10.1021/jm00157a035
10839228 59885 None 0 Rat Functional pKi = 6.4 6.4 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 504 8 2 8 2.1 CCCn1c(=O)c2nc(-c3ccc(/C=C/C(=O)NN4C(=O)C(C)=C(C)C4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17294 59885 None 0 Rat Functional pKi = 6.4 6.4 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 504 8 2 8 2.1 CCCn1c(=O)c2nc(-c3ccc(/C=C/C(=O)NN4C(=O)C(C)=C(C)C4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
25188209 178864 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 311 3 1 8 1.6 Nc1nc(-c2ncco2)c2nnn(Cc3ccccc3F)c2n1 10.1016/j.ejmech.2010.04.039
CHEMBL468701 178864 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 311 3 1 8 1.6 Nc1nc(-c2ncco2)c2nnn(Cc3ccccc3F)c2n1 10.1016/j.ejmech.2010.04.039
53354728 110841 None 0 Human Functional pKi = 7.4 7.4 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 283 2 1 5 2.7 CC1(C)CCCN(c2nnc(N)nc2-c2ccccc2)C1 10.1021/jm4011669
CHEMBL3260727 110841 None 0 Human Functional pKi = 7.4 7.4 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 283 2 1 5 2.7 CC1(C)CCCN(c2nnc(N)nc2-c2ccccc2)C1 10.1021/jm4011669
101422 91580 None 10 Guinea pig Functional pKi = 5.4 5.4 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 218 1 0 6 -0.9 C#CCn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00157a035
CHEMBL24049 91580 None 10 Guinea pig Functional pKi = 5.4 5.4 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 218 1 0 6 -0.9 C#CCn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00157a035
45275173 89791 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 335 3 1 4 4.7 Nc1nc(-c2cccc(F)c2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
CHEMBL2377097 89791 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 335 3 1 4 4.7 Nc1nc(-c2cccc(F)c2)nc2sc(Cc3ccccc3)cc12 10.1016/j.bmcl.2013.02.078
45278946 109643 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 382 4 1 6 4.4 Nc1nc(-c2ccc(C(F)F)o2)nc2sc(CN3CCC(F)CC3)cc12 10.1039/C1MD00082A
CHEMBL3222077 109643 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 382 4 1 6 4.4 Nc1nc(-c2ccc(C(F)F)o2)nc2sc(CN3CCC(F)CC3)cc12 10.1039/C1MD00082A
118708234 113427 None 0 Human Functional pKi = 6.4 6.4 -10 3
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production measured by scintillation counter assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production measured by scintillation counter assay
ChEMBL 329 5 1 5 3.6 Nc1nc(CCCc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2021.113907
CHEMBL3317574 113427 None 0 Human Functional pKi = 6.4 6.4 -10 3
Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production measured by scintillation counter assayAntagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production measured by scintillation counter assay
ChEMBL 329 5 1 5 3.6 Nc1nc(CCCc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2021.113907
541903 57964 None 0 Rat Functional pKi = 5.4 5.4 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 382 8 2 7 1.4 C=CCn1c(=O)c2nc(-c3ccc(OCC(=O)O)cc3)[nH]c2n(CC=C)c1=O 10.1021/jm990421v
CHEMBL16724 57964 None 0 Rat Functional pKi = 5.4 5.4 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 382 8 2 7 1.4 C=CCn1c(=O)c2nc(-c3ccc(OCC(=O)O)cc3)[nH]c2n(CC=C)c1=O 10.1021/jm990421v
45278947 109645 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 400 4 1 6 4.7 Nc1nc(-c2ccc(C(F)F)o2)nc2sc(CN3CCCC(F)(F)C3)cc12 10.1039/C1MD00082A
CHEMBL3222079 109645 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 400 4 1 6 4.7 Nc1nc(-c2ccc(C(F)F)o2)nc2sc(CN3CCCC(F)(F)C3)cc12 10.1039/C1MD00082A
9870718 60006 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 503 10 2 8 3.6 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4C(C)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17341 60006 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
ChEMBL 503 10 2 8 3.6 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4C(C)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
9870718 60006 None 0 Rat Functional pKi = 6.4 6.4 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 503 10 2 8 3.6 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4C(C)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17341 60006 None 0 Rat Functional pKi = 6.4 6.4 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 503 10 2 8 3.6 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4C(C)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
9912946 59019 None 0 Rat Functional pKi = 5.4 5.4 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 478 7 2 6 3.7 O=C(O)/C=C/c1ccc(-c2nc3c(=O)n(Cc4ccccc4)c(=O)n(Cc4ccccc4)c3[nH]2)cc1 10.1021/jm990421v
CHEMBL16908 59019 None 0 Rat Functional pKi = 5.4 5.4 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 478 7 2 6 3.7 O=C(O)/C=C/c1ccc(-c2nc3c(=O)n(Cc4ccccc4)c(=O)n(Cc4ccccc4)c3[nH]2)cc1 10.1021/jm990421v
45279272 109648 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 350 3 1 7 3.0 Nc1nc(-c2ccc(Cl)o2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
CHEMBL3222082 109648 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 350 3 1 7 3.0 Nc1nc(-c2ccc(Cl)o2)nc2sc(CN3CCOCC3)cc12 10.1039/C1MD00082A
9825550 57609 None 0 Rat Functional pKi = 7.3 7.3 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 461 9 2 7 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16677 57609 None 0 Rat Functional pKi = 7.3 7.3 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 461 9 2 7 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
11568203 96297 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 432 5 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(C)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL260975 96297 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 432 5 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(C)c1=O 10.1016/j.ejmech.2010.04.039
1882 90686 None 47 Guinea pig Functional pKi = 5.4 5.4 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 242 2 0 6 -0.3 Cn1c(=O)c2c(ncn2CCCl)n(C)c1=O 10.1021/jm00157a035
CHEMBL23903 90686 None 47 Guinea pig Functional pKi = 5.4 5.4 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 242 2 0 6 -0.3 Cn1c(=O)c2c(ncn2CCCl)n(C)c1=O 10.1021/jm00157a035
1676 99038 None 41 Human Functional pKi = 5.3 5.3 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1016/j.ejmech.2021.113907
CHEMBL279898 99038 None 41 Human Functional pKi = 5.3 5.3 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1016/j.ejmech.2021.113907
11605883 79983 None 3 Human Functional pKi = 6.3 6.3 - 1
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL212625 79983 None 3 Human Functional pKi = 6.3 6.3 - 1
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1016/j.ejmech.2010.04.039
45275619 89807 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 335 4 1 5 4.7 CCc1ccc(-c2nc(N)c3cc(Cc4ccccc4)sc3n2)o1 10.1016/j.bmcl.2013.02.078
CHEMBL2377113 89807 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 335 4 1 5 4.7 CCc1ccc(-c2nc(N)c3cc(Cc4ccccc4)sc3n2)o1 10.1016/j.bmcl.2013.02.078
45279828 109627 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 350 3 1 6 3.8 Nc1nc(-c2ccco2)nc2sc(CN3CCC(F)(F)CC3)cc12 10.1039/C1MD00082A
CHEMBL3222060 109627 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 350 3 1 6 3.8 Nc1nc(-c2ccco2)nc2sc(CN3CCC(F)(F)CC3)cc12 10.1039/C1MD00082A
21958762 155870 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 288 4 2 6 0.7 CCCn1c(=O)c2[nH]c(-c3cn[nH]c3)nc2n(CC)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL405901 155870 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 288 4 2 6 0.7 CCCn1c(=O)c2[nH]c(-c3cn[nH]c3)nc2n(CC)c1=O 10.1016/j.ejmech.2010.04.039
10648228 98488 None 0 Rat Functional pKi = 6.3 6.3 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 475 9 1 7 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(C)c4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL275606 98488 None 0 Rat Functional pKi = 6.3 6.3 - 0
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
ChEMBL 475 9 1 7 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(C)c4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
11618368 3847 None 50 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1016/j.ejmech.2021.113907
5611 3847 None 50 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1016/j.ejmech.2021.113907
CHEMBL2105747 3847 None 50 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1016/j.ejmech.2021.113907
DB12203 3847 None 50 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1016/j.ejmech.2021.113907
10174023 189323 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 469 4 1 10 2.8 Nc1nc2c(cnn2CCN2CCc3nc(C(F)(F)F)ccc3C2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
CHEMBL511446 189323 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 469 4 1 10 2.8 Nc1nc2c(cnn2CCN2CCc3nc(C(F)(F)F)ccc3C2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.069
11618368 3847 None 50 Human Functional pKi = 8.3 8.3 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/jm4011669
5611 3847 None 50 Human Functional pKi = 8.3 8.3 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/jm4011669
CHEMBL2105747 3847 None 50 Human Functional pKi = 8.3 8.3 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/jm4011669
DB12203 3847 None 50 Human Functional pKi = 8.3 8.3 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/jm4011669
11596214 110840 None 0 Human Functional pKi = 8.3 8.3 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 388 4 1 7 2.9 COc1cnc(N2CCOCC2)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1021/jm4011669
CHEMBL3260726 110840 None 0 Human Functional pKi = 8.3 8.3 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 388 4 1 7 2.9 COc1cnc(N2CCOCC2)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1021/jm4011669
10127905 189486 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 474 8 1 11 2.4 COCCOc1ccc2c(c1)CN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1016/j.bmcl.2008.05.069
CHEMBL512891 189486 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 474 8 1 11 2.4 COCCOc1ccc2c(c1)CN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)CC2 10.1016/j.bmcl.2008.05.069
44218327 60999 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 386 5 1 9 1.1 CN(C)CCn1ncc2c1nc(N)n1c(=O)n(Cc3cccc(Cl)c3)nc21 10.1016/j.bmcl.2011.02.045
CHEMBL1762513 60999 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 386 5 1 9 1.1 CN(C)CCn1ncc2c1nc(N)n1c(=O)n(Cc3cccc(Cl)c3)nc21 10.1016/j.bmcl.2011.02.045
44218327 60999 None 0 Human Functional pKi = 8.3 8.3 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 386 5 1 9 1.1 CN(C)CCn1ncc2c1nc(N)n1c(=O)n(Cc3cccc(Cl)c3)nc21 10.1021/jm4011669
CHEMBL1762513 60999 None 0 Human Functional pKi = 8.3 8.3 - 0
Inhibition of human recombinant adenosine receptor A2aInhibition of human recombinant adenosine receptor A2a
ChEMBL 386 5 1 9 1.1 CN(C)CCn1ncc2c1nc(N)n1c(=O)n(Cc3cccc(Cl)c3)nc21 10.1021/jm4011669
46889044 7572 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 382 5 2 6 3.8 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CNCc3ccco3)ccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1087714 7572 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 382 5 2 6 3.8 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CNCc3ccco3)ccc1C2=O 10.1016/j.bmcl.2010.03.042
45279727 109629 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 342 3 1 6 4.3 C[C@H]1CCC[C@@H](C)N1Cc1cc2c(N)nc(-c3ccco3)nc2s1 10.1039/C1MD00082A
CHEMBL3222062 109629 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 342 3 1 6 4.3 C[C@H]1CCC[C@@H](C)N1Cc1cc2c(N)nc(-c3ccco3)nc2s1 10.1039/C1MD00082A
45279727 109629 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human recombinant adenosine receptor A2a by cAMP assayAntagonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 342 3 1 6 4.3 C[C@H]1CCC[C@@H](C)N1Cc1cc2c(N)nc(-c3ccco3)nc2s1 10.1021/jm4011669
CHEMBL3222062 109629 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human recombinant adenosine receptor A2a by cAMP assayAntagonist activity at human recombinant adenosine receptor A2a by cAMP assay
ChEMBL 342 3 1 6 4.3 C[C@H]1CCC[C@@H](C)N1Cc1cc2c(N)nc(-c3ccco3)nc2s1 10.1021/jm4011669
46889042 7568 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 397 3 1 7 2.6 N#Cc1cccc(-c2nc(N)nc3c2C(=O)c2cccc(CN4CCOCC4)c2-3)c1 10.1016/j.bmcl.2010.03.042
CHEMBL1087708 7568 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 397 3 1 7 2.6 N#Cc1cccc(-c2nc(N)nc3c2C(=O)c2cccc(CN4CCOCC4)c2-3)c1 10.1016/j.bmcl.2010.03.042
46889068 7637 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 393 5 2 6 3.6 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CNCc3ccccn3)ccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1088235 7637 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 393 5 2 6 3.6 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CNCc3ccccn3)ccc1C2=O 10.1016/j.bmcl.2010.03.042
10287801 178997 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 416 5 1 10 2.3 COc1ccc2c(c1)CN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)C2 10.1016/j.bmcl.2008.05.069
CHEMBL469876 178997 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 416 5 1 10 2.3 COc1ccc2c(c1)CN(CCn1ncc3c1nc(N)n1nc(-c4ccco4)nc31)C2 10.1016/j.bmcl.2008.05.069
17035744 8846 None 3 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 307 1 1 4 3.6 Nc1nc(-c2ccc(Cl)cc2)c2c(n1)-c1ccccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1096998 8846 None 3 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 307 1 1 4 3.6 Nc1nc(-c2ccc(Cl)cc2)c2c(n1)-c1ccccc1C2=O 10.1016/j.bmcl.2010.03.042
135484064 2616 None 3 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2021.113907
390 2616 None 3 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2021.113907
CHEMBL260331 2616 None 3 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2021.113907
44568344 191534 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 422 5 1 9 3.6 Nc1nc2c(cnn2CCc2cccc(-c3cccnc3)c2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.074
CHEMBL519282 191534 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 422 5 1 9 3.6 Nc1nc2c(cnn2CCc2cccc(-c3cccnc3)c2)c2nc(-c3ccco3)nn12 10.1016/j.bmcl.2008.05.074
404 4098 None 26 Human Functional pKi = 8.2 8.2 - 2
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1016/j.bmcl.2013.03.070
432 4098 None 26 Human Functional pKi = 8.2 8.2 - 2
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1016/j.bmcl.2013.03.070
5697 4098 None 26 Human Functional pKi = 8.2 8.2 - 2
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1016/j.bmcl.2013.03.070
CHEMBL273094 4098 None 26 Human Functional pKi = 8.2 8.2 - 2
Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assayAntagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1016/j.bmcl.2013.03.070
46889097 9075 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 399 4 2 7 2.6 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CNN3CCC(=O)CC3)ccc1C2=O 10.1016/j.bmcl.2010.03.042
CHEMBL1099028 9075 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at adenosine A2A receptorAntagonist activity at adenosine A2A receptor
ChEMBL 399 4 2 7 2.6 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(CNN3CCC(=O)CC3)ccc1C2=O 10.1016/j.bmcl.2010.03.042
20605044 93992 None 1 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 283 3 1 8 1.7 CCCn1cnc2c1nc(N)n1nc(-c3ccco3)nc21 10.1016/j.bmcl.2006.12.104
CHEMBL248298 93992 None 1 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human adenosine A2A receptorAntagonist activity at human adenosine A2A receptor
ChEMBL 283 3 1 8 1.7 CCCn1cnc2c1nc(N)n1nc(-c3ccco3)nc21 10.1016/j.bmcl.2006.12.104
135433923 97787 None 0 Guinea pig Functional pKi = 7.3 7.3 - 0
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 328 5 2 6 2.1 CCCn1c(=O)c2nc(-c3ccc(O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm00382a018
CHEMBL27155 97787 None 0 Guinea pig Functional pKi = 7.3 7.3 - 0
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 328 5 2 6 2.1 CCCn1c(=O)c2nc(-c3ccc(O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm00382a018
10193 3010 None 42 Human Functional pKi = 7.3 7.3 56 2
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 10.1016/j.ejmech.2021.113907
53466958 3010 None 42 Human Functional pKi = 7.3 7.3 56 2
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 10.1016/j.ejmech.2021.113907
53466958.0 3010 None 42 Human Functional pKi = 7.3 7.3 56 2
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 10.1016/j.ejmech.2021.113907
CHEMBL3638684 3010 None 42 Human Functional pKi = 7.3 7.3 56 2
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 10.1016/j.ejmech.2021.113907
CHEMBL3694769 3010 None 42 Human Functional pKi = 7.3 7.3 56 2
Antagonist activity at adenosine A2A receptor (unknown origin)Antagonist activity at adenosine A2A receptor (unknown origin)
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 10.1016/j.ejmech.2021.113907
53467187 131965 None 0 Human Functional pKi = 7.3 7.3 - 0
cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).
ChEMBL 282 2 1 6 1.1 CN(C)c1nc(-n2cccn2)nc(N)c1Br nan
CHEMBL3694776 131965 None 0 Human Functional pKi = 7.3 7.3 - 0
cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).cAMP Production Assay: hese assays were performed at adenosine receptors transfected using a cAMP enzymeimmunoassay kit (Amersham Biosciences). CHO-A2A cells were seeded (10000 cells/well) in 96-well culture plates and incubated at 37 C. in an atmosphere with 5% CO2 in Dulbecco's Modified Eagle's Medium Nutrient Mixture F-12 (DMEM F-12), containing 10% Foetal Calf Serum (FCS) and 1% L-Glutamine. Cells were washed 3x with 200 ul assay medium (DMEM-F12 and 25 mM HEPES pH=7.4) and pre-incubated with assay medium containing 30 uM rolipram and test compounds at 37 C. for 15 min. 1 uM NECA was incubated for 15 min at 37 C. (total incubation time 30 min). Reaction was stopped with lysis buffer supplied in the kit and the enzymeimmunoassay was carried out for detection of intracellular cAMP at 450 nm in an Ultra Evolution detector (Tecan).
ChEMBL 282 2 1 6 1.1 CN(C)c1nc(-n2cccn2)nc(N)c1Br nan
46889255 7621 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 406 7 1 6 3.8 CCN(CC)CCOc1ccc2c(c1)-c1nc(N)nc(-c3ccc(F)cc3)c1C2=O 10.1016/j.bmcl.2010.03.024
CHEMBL1088132 7621 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonistic activity at adenosine A2A receptorAntagonistic activity at adenosine A2A receptor
ChEMBL 406 7 1 6 3.8 CCN(CC)CCOc1ccc2c(c1)-c1nc(N)nc(-c3ccc(F)cc3)c1C2=O 10.1016/j.bmcl.2010.03.024
45278784 109293 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 367 3 1 7 3.4 N#Cc1cccc(-c2nc(N)c3cc(CN4CCSCC4)sc3n2)c1 10.1039/C1MD00082A
CHEMBL3217865 109293 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 367 3 1 7 3.4 N#Cc1cccc(-c2nc(N)c3cc(CN4CCSCC4)sc3n2)c1 10.1039/C1MD00082A
62188326 89780 None 21 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 227 1 1 4 2.9 Nc1nc(-c2ccccc2)nc2sccc12 10.1016/j.bmcl.2013.02.078
CHEMBL2377086 89780 None 21 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at human adenosine A2a receptor expressed in CHOK1 cells assessed as inhibition of NECA/forskolin-induced cAMP accumulation incubated for 15 mins prior to NECA/forskolin challenge measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 227 1 1 4 2.9 Nc1nc(-c2ccccc2)nc2sccc12 10.1016/j.bmcl.2013.02.078
12905388 91803 None 0 Guinea pig Functional pKi = 5.3 5.3 - 1
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 194 1 1 5 -0.6 CCn1c(=O)c2nc[nH]c2n(C)c1=O 10.1021/jm00157a035
CHEMBL24107 91803 None 0 Guinea pig Functional pKi = 5.3 5.3 - 1
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 194 1 1 5 -0.6 CCn1c(=O)c2nc[nH]c2n(C)c1=O 10.1021/jm00157a035
96448 100045 None 5 Guinea pig Functional pKi = 5.3 5.3 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 222 2 0 6 -0.2 CCCn1c(=O)c2c(ncn2C)n(C)c1=O 10.1021/jm00157a035
CHEMBL286680 100045 None 5 Guinea pig Functional pKi = 5.3 5.3 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 222 2 0 6 -0.2 CCCn1c(=O)c2c(ncn2C)n(C)c1=O 10.1021/jm00157a035
22995178 100064 None 2 Guinea pig Functional pKi = 5.3 5.3 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 232 4 1 5 0.3 C=CCn1c(=O)c2nc[nH]c2n(CC=C)c1=O 10.1021/jm00157a035
CHEMBL286785 100064 None 2 Guinea pig Functional pKi = 5.3 5.3 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 232 4 1 5 0.3 C=CCn1c(=O)c2nc[nH]c2n(CC=C)c1=O 10.1021/jm00157a035
2519 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00382a018
2519.0 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00382a018
407 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00382a018
463 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00382a018
CHEMBL113 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00382a018
DB00201 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00382a018
2519 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Antagonist activity at adenosine receptor A2A in [3H]-adenine-labeled guinea pig cerebral cortical slices assessed as inhibition of 2-chloroadenosine-mediated [3H]cAMP accumulationAntagonist activity at adenosine receptor A2A in [3H]-adenine-labeled guinea pig cerebral cortical slices assessed as inhibition of 2-chloroadenosine-mediated [3H]cAMP accumulation
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmcl.2016.10.086
2519.0 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Antagonist activity at adenosine receptor A2A in [3H]-adenine-labeled guinea pig cerebral cortical slices assessed as inhibition of 2-chloroadenosine-mediated [3H]cAMP accumulationAntagonist activity at adenosine receptor A2A in [3H]-adenine-labeled guinea pig cerebral cortical slices assessed as inhibition of 2-chloroadenosine-mediated [3H]cAMP accumulation
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmcl.2016.10.086
407 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Antagonist activity at adenosine receptor A2A in [3H]-adenine-labeled guinea pig cerebral cortical slices assessed as inhibition of 2-chloroadenosine-mediated [3H]cAMP accumulationAntagonist activity at adenosine receptor A2A in [3H]-adenine-labeled guinea pig cerebral cortical slices assessed as inhibition of 2-chloroadenosine-mediated [3H]cAMP accumulation
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmcl.2016.10.086
463 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Antagonist activity at adenosine receptor A2A in [3H]-adenine-labeled guinea pig cerebral cortical slices assessed as inhibition of 2-chloroadenosine-mediated [3H]cAMP accumulationAntagonist activity at adenosine receptor A2A in [3H]-adenine-labeled guinea pig cerebral cortical slices assessed as inhibition of 2-chloroadenosine-mediated [3H]cAMP accumulation
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmcl.2016.10.086
CHEMBL113 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Antagonist activity at adenosine receptor A2A in [3H]-adenine-labeled guinea pig cerebral cortical slices assessed as inhibition of 2-chloroadenosine-mediated [3H]cAMP accumulationAntagonist activity at adenosine receptor A2A in [3H]-adenine-labeled guinea pig cerebral cortical slices assessed as inhibition of 2-chloroadenosine-mediated [3H]cAMP accumulation
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmcl.2016.10.086
DB00201 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Antagonist activity at adenosine receptor A2A in [3H]-adenine-labeled guinea pig cerebral cortical slices assessed as inhibition of 2-chloroadenosine-mediated [3H]cAMP accumulationAntagonist activity at adenosine receptor A2A in [3H]-adenine-labeled guinea pig cerebral cortical slices assessed as inhibition of 2-chloroadenosine-mediated [3H]cAMP accumulation
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmcl.2016.10.086
2519 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00157a035
2519.0 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00157a035
407 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00157a035
463 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00157a035
CHEMBL113 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00157a035
DB00201 779 None 49 Guinea pig Functional pKi = 4.3 4.3 - 8
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm00157a035
6424576 94781 None 1 Guinea pig Functional pKi = 4.3 4.3 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 210 2 2 6 -1.6 Cn1c(=O)n(CCO)c(=O)c2[nH]cnc21 10.1021/jm00157a035
CHEMBL25303 94781 None 1 Guinea pig Functional pKi = 4.3 4.3 - 0
Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices.
ChEMBL 210 2 2 6 -1.6 Cn1c(=O)n(CCO)c(=O)c2[nH]cnc21 10.1021/jm00157a035
9819926 85368 None 1 Human Functional pKi = 5.3 5.3 - 0
Agonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cells
ChEMBL 353 4 3 9 0.0 O[C@@H]1[C@@H](CF)O[C@@H](n2cnc3c(NC4CCOCC4)ncnc32)[C@@H]1O 10.1007/s00044-004-0013-y
CHEMBL2261343 85368 None 1 Human Functional pKi = 5.3 5.3 - 0
Agonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cells
ChEMBL 353 4 3 9 0.0 O[C@@H]1[C@@H](CF)O[C@@H](n2cnc3c(NC4CCOCC4)ncnc32)[C@@H]1O 10.1007/s00044-004-0013-y
449 2643 None 38 Human Functional pKi = 6.3 6.3 -36 4
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2010.04.039
453 2643 None 38 Human Functional pKi = 6.3 6.3 -36 4
Antagonist activity against human adenosine A2A receptorAntagonist activity against human adenosine A2A receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.10