Compile Data Set for Download or QSAR
Report error Found 70 Enz. Inhib. hit(s) with all data for entry = 50012030
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553404(Ciforadenant | V81444 | CPI-444 | V-81444)
Affinity DataEC50: >1.00E+4nMAssay Description:Antagonist activity at adenosine 2A receptor (unknown origin) in presence of high adenosineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553410(CHEMBL4741609)
Affinity DataIC50: 0.5nMAssay Description:Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins follow...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553411(CHEMBL4760867)
Affinity DataIC50: 0.600nMAssay Description:Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins follow...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50382493(CHEMBL2024116)
Affinity DataIC50: 0.790nMAssay Description: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 f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553410(CHEMBL4741609)
Affinity DataIC50: 2nMAssay Description:Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins follow...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553411(CHEMBL4760867)
Affinity DataIC50: 2nMAssay Description:Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins follow...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Rat)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50382493(CHEMBL2024116)
Affinity DataIC50: 9.70nMAssay Description:Antagonist activity at rat adenosine 2A receptor assessed as reduction in cAMP level in presence of 0.1 uM adenosineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50382493(CHEMBL2024116)
Affinity DataIC50: 10nMAssay Description:Antagonist activity at adenosine 2A receptor (unknown origin) in presence of 1 uM adenosineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553405(CHEMBL4762582)
Affinity DataIC50: 10nMAssay Description:Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in NECA-induced cAMP level incubated for 15 mins b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553407(CHEMBL4765154)
Affinity DataIC50: 10nMAssay Description:Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in NECA-induced cAMP level incubated for 15 mins b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553406(CHEMBL4786207)
Affinity DataIC50: 10nMAssay Description:Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in NECA-induced cAMP level incubated for 15 mins b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553403(CHEMBL4747929)
Affinity DataIC50: 17nMAssay Description:Antagonist activity at adenosine 2A receptor in human whole blood assessed as reduction in phosphorylated CREB level preincubated for 20 mins followe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553404(Ciforadenant | V81444 | CPI-444 | V-81444)
Affinity DataIC50: 17nMAssay Description:Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP by immunoassayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553410(CHEMBL4741609)
Affinity DataIC50: 20nMAssay Description:Antagonist activity at adenosine 2A receptor in human peripheral blood lymphocytes assessed as reduction in NECA-stimulated CREB phosphorylation by f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM128295(US8796284, 1)
Affinity DataIC50: 25nMAssay Description:Antagonist activity at adenosine 2A receptor (unknown origin) expressed in CHO cells assessed as reduction in intracellular cAMP level preincubated f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553411(CHEMBL4760867)
Affinity DataIC50: 25nMAssay Description:Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins follow...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Mouse)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553412(CHEMBL4740766)
Affinity DataIC50: 40nMAssay Description:Antagonist activity at adenosine 2A receptor in BALB/c mouse T cells assessed as reduction in CGS-21680-induced suppression of IFN-gamma secretion in...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Mouse)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553412(CHEMBL4740766)
Affinity DataIC50: 40nMAssay Description:Antagonist activity at adenosine 2A receptor in BALB/c mouse T cells assessed as reduction in CGS-21680-induced suppression of IL-2 secretion incubat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553410(CHEMBL4741609)
Affinity DataIC50: 49nMAssay Description:Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in cAMP production preincubated for 10 mins follow...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553404(Ciforadenant | V81444 | CPI-444 | V-81444)
Affinity DataIC50: 70nMAssay Description: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 as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553400(CHEMBL4782266)
Affinity DataIC50: 77nMAssay Description:Antagonist activity at adenosine 2A receptor in human PBMC assessed as reversal of NECA/CD3/CD28-stimulated IL-2 release incubated for 24 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553401(CHEMBL4778265)
Affinity DataIC50: 77nMAssay Description:Antagonist activity at adenosine 2A receptor in human PBMC assessed as reversal of NECA/CD3/CD28-stimulated IL-2 release incubated for 24 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Rat)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50382493(CHEMBL2024116)
Affinity DataIC50: 97nMAssay Description:Antagonist activity at rat adenosine 2A receptor assessed as reduction in cAMP level in presence of 10 uM adenosineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553409(CHEMBL4779911)
Affinity DataIC50: 100nMAssay Description:Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in NECA-induced cAMP level incubated for 15 mins b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553408(CHEMBL4750504)
Affinity DataIC50: 100nMAssay Description:Antagonist activity at human adenosine 2A receptor expressed in HEK293 cells assessed as reduction in NECA-induced cAMP level incubated for 15 mins b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50382493(CHEMBL2024116)
Affinity DataIC50: 143nMAssay Description: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 fl...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553401(CHEMBL4778265)
Affinity DataIC50: 200nMAssay Description:Antagonist activity at adenosine 2A receptor in human blood assessed as reversal of NECA/LPS-stimulated TNF-alpha release incubated for 5 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553402(CHEMBL4759461)
Affinity DataIC50: 200nMAssay Description:Antagonist activity at adenosine 2A receptor in human blood assessed as reversal of NECA/LPS-stimulated TNF-alpha release incubated for 5 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553403(CHEMBL4747929)
Affinity DataIC50: 200nMAssay Description:Antagonist activity at adenosine 2A receptor in human blood assessed as reversal of NECA/LPS-stimulated TNF-alpha release incubated for 5 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553400(CHEMBL4782266)
Affinity DataIC50: 200nMAssay Description:Antagonist activity at adenosine 2A receptor in human blood assessed as reversal of NECA/LPS-stimulated TNF-alpha release incubated for 5 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553403(CHEMBL4747929)
Affinity DataKi:  0.0780nMAssay Description:Inhibition of FRET-labelled CA200645 binding to human adenosine 2A receptor expressed in CHO cells incubated for 2 hr by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553401(CHEMBL4778265)
Affinity DataKi:  0.110nMAssay Description:Inhibition of FRET-labelled CA200645 binding to human adenosine 2A receptor expressed in CHO cells incubated for 2 hr by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM21190(CHEMBL113142 | 4-(2-{[5-amino-2-(furan-2-yl)-[1,2,...)
Affinity DataKi:  0.800nMAssay Description:Antagonist activity at human adenosine 2A receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50202986(SCH-420814 | 7-(2-(4-(2,4-difluorophenyl)piperazin...)
Affinity DataKi:  1.10nMAssay Description:Displacement of [3H]SCH58261 from human adenosine 2A receptor expressed in HEK293 cell membranes incubated for 1.5 hrs by radioligand competition bin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50048466(CHEMBL17127 | SCH58261 | 2-(furan-2-yl)-7-phenethy...)
Affinity DataKi:  1.10nMAssay Description:Antagonist activity at human adenosine 2A receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553402(CHEMBL4759461)
Affinity DataKi:  1.30nMAssay Description:Inhibition of FRET-labelled CA200645 binding to human adenosine 2A receptor expressed in CHO cells incubated for 2 hr by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A1(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553401(CHEMBL4778265)
Affinity DataKi:  1.70nMAssay Description:Inhibition of FRET-labelled CA200645 binding to human adenosine A1 receptor expressed in CHO cells incubated for 2 hr by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50382493(CHEMBL2024116)
Affinity DataKi:  1.70nMAssay Description:Antagonist activity at human adenosine 2A receptor expressed in HEK293T cells by radioligand competition binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553400(CHEMBL4782266)
Affinity DataKi:  3.30nMAssay Description:Inhibition of FRET-labelled CA200645 binding to human adenosine 2A receptor expressed in CHO cells incubated for 2 hr by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553404(Ciforadenant | V81444 | CPI-444 | V-81444)
Affinity DataKi:  3.40nMAssay Description:Displacement of [3H]CGS-21680 from human adenosine 2A receptor expressed in HEK293 cells incubated for 90 mins by scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50011294(Ro-4494351-002 | Ro-4494351 | SYN-115 | Ro-4494351...)
Affinity DataKi:  5nMAssay Description:Antagonist activity at human adenosine 2A receptor (409 to 412 residues) expressed in CHO cells using Ysi-poly-1-lysine as substrate incubated for 1 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetAdenosine receptor A2b(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553403(CHEMBL4747929)
Affinity DataKi:  5.40nMAssay Description:Inhibition of FRET-labelled CA200645 binding to human adenosine 2B receptor expressed in CHO cells incubated for 2 hr by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A3(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553401(CHEMBL4778265)
Affinity DataKi:  11nMAssay Description:Inhibition of FRET-labelled CA200645 binding to human adenosine A3 receptor expressed in CHO cells incubated for 2 hr by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM128295(US8796284, 1)
Affinity DataKi:  12nMAssay Description:Displacement of [3H]ZM241385 from human adenosine 2A receptor transfected in human HeLa cells incubated for 30 mins by competition radioligand bindin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50176050(8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-1H-pu...)
Affinity DataKi:  36nMAssay Description:Antagonist activity at human adenosine 2A receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetAdenosine receptor A2b(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM21190(CHEMBL113142 | 4-(2-{[5-amino-2-(furan-2-yl)-[1,2,...)
Affinity DataKi:  50nMAssay Description:Inhibition of human adenosine 2B receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553413(CHEMBL4747570)
Affinity DataKi:  50nMAssay Description:Displacement of [3H]-ZM241385 from human adenosine 2A receptor expressed in HEK293 cells incubated for 1.5 hrs by beta scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A3(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50553402(CHEMBL4759461)
Affinity DataKi:  62nMAssay Description:Inhibition of FRET-labelled CA200645 binding to human adenosine A3 receptor expressed in CHO cells incubated for 2 hr by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2b(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50382493(CHEMBL2024116)
Affinity DataKi:  64nMAssay Description:Antagonist activity at human adenosine A2b receptor expressed in HEK293T cells by radioligand competition binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetAdenosine receptor A1(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM50382493(CHEMBL2024116)
Affinity DataKi:  160nMAssay Description:Antagonist activity at human adenosine A1 receptor expressed in CHO cells by radioligand competition binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
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