Compile Data Set for Download or QSAR
Report error Found 23030 Enz. Inhib. hit(s) with Target = 'Adenosine receptor A2'
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50451379(CHEMBL43299)
Affinity DataEC50:  0.00100nMAssay Description:AE maximal score at Adenosine A2A receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50449640(CHEMBL4172399)
Affinity DataIC50: 0.00160nMAssay Description:Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50449648(CHEMBL4161758)
Affinity DataIC50: 0.00170nMAssay Description:Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50211087(CHEMBL3958838)
Affinity DataIC50: 0.00190nMAssay Description:Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/11/2018
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50550812(CHEMBL4756283)
Affinity DataKi:  0.00380nMAssay Description:Displacement of [3H]MSX2 from human adenosine receptor A2A expressed in HEK293 cell membranes incubated for 30 mins by radioligand competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50493145(CHEMBL2419149)
Affinity DataKi:  0.00420nMAssay Description:Displacement of [3H]ZM241385 from human A2A receptor expressed in HEK293 cell membranes after 60 mins by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50493145(CHEMBL2419149)
Affinity DataKi:  0.00420nMAssay Description:Binding affinity to human adenosine A2A receptor expressed in HEK293T cells measured by radioligand binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50493145(CHEMBL2419149)
Affinity DataKi:  0.00420nMAssay Description:Displacement of [3H]MSX2 from human adenosine receptor A2A expressed in HEK293 cell membranes incubated for 30 mins by radioligand competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50493144(CHEMBL2419144)
Affinity DataKi:  0.00470nMAssay Description:Displacement of [3H]ZM241385 from human A2A receptor expressed in HEK293 cell membranes after 60 mins by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50449652(CHEMBL4172264)
Affinity DataIC50: 0.00640nMAssay Description:Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Rat)
University of Camerino

Curated by ChEMBL
LigandPNGBDBM50369087(CHEMBL605065)
Affinity DataEC50:  0.00800nMAssay Description:Functional activity against adenosine A2a receptor from rat aorta.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/31/2012
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50315548(8-(2-Thioxo-7(3-m-iodophenyl)-2-(2-furyl)thiazolo[...)
Affinity DataKi:  0.00820nMAssay Description:Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by rapid filtration assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50211078(CHEMBL3904408)
Affinity DataIC50: 0.00830nMAssay Description:Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/11/2018
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50493151(CHEMBL2419139)
Affinity DataKi:  0.0100nMAssay Description:Displacement of [3H]ZM241385 from human A2A receptor expressed in HEK293 cell membranes after 60 mins by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50449634(CHEMBL4167125)
Affinity DataIC50: 0.0110nMAssay Description:Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50315541(8-(2-Thioxo-7(3-allyl)-2-(2-furyl)thiazole[4,3-e]1...)
Affinity DataKi:  0.0160nMAssay Description:Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by rapid filtration assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50493157(CHEMBL2419146)
Affinity DataKi:  0.0270nMAssay Description:Displacement of [3H]ZM241385 from human A2A receptor expressed in HEK293 cell membranes after 60 mins by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50493154(CHEMBL2419147)
Affinity DataKi:  0.0300nMAssay Description:Displacement of [3H]ZM241385 from human A2A receptor expressed in HEK293 cell membranes after 60 mins by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50085666((2S,3S,4R,5R)-5-{6-(2,2-Diphenyl-ethylamino)-2-[2-...)
Affinity DataKi:  0.0300nMAssay Description:In vitro inhibition of human neutrophil activation via Adenosine A2A receptor.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/2/2012
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50449648(CHEMBL4161758)
Affinity DataIC50: 0.0360nMAssay Description:Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50315545(8-(2-Thioxo-7(3-m-chlorophenyl)-2-(2-furyl)thiazol...)
Affinity DataKi:  0.0380nMAssay Description:Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by rapid filtration assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM761402(N-[4-(3-Cyanophenyl)-5-(4-methyl-6-quinolyl)thiazo...)
Affinity DataKi:  0.0400nMMore data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
TBA
Entry Details
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50449640(CHEMBL4172399)
Affinity DataIC50: 0.0400nMAssay Description:Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50496138(CHEMBL3121727)
Affinity DataKi:  0.0420nMAssay Description:Displacement of [3H]-NECA from human recombinant adenosine A2A receptor expressed in CHO cell membranes after 3 hrs by microbeta counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50449652(CHEMBL4172264)
Affinity DataIC50: 0.0450nMAssay Description:Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50496133(CHEMBL3121725)
Affinity DataKi:  0.0450nMAssay Description:Displacement of [3H]-NECA from human recombinant adenosine A2A receptor expressed in CHO cell membranes after 3 hrs by microbeta counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50094037(SCH-442416 | 2-Furan-2-yl-7-[3-(4-methoxy-phenyl)-...)
Affinity DataKi: >0.0480nMAssay Description:Binding affinity to human adenosine A2a receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/14/2011
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Rat)
University of Camerino

Curated by ChEMBL
LigandPNGBDBM50094037(SCH-442416 | 2-Furan-2-yl-7-[3-(4-methoxy-phenyl)-...)
Affinity DataKd:  0.0480nMAssay Description:Binding affinity to adenosine receptor A2a in rat striatumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/8/2015
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50094037(SCH-442416 | 2-Furan-2-yl-7-[3-(4-methoxy-phenyl)-...)
Affinity DataKi:  0.0480nMAssay Description:Inhibitory activity against human adenosine A2A receptor expressed in HEK293 cells by displacement of [3H]SCH-58261More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50094037(SCH-442416 | 2-Furan-2-yl-7-[3-(4-methoxy-phenyl)-...)
Affinity DataKi:  0.0480nMAssay Description:Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/24/2016
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Rat)
University of Camerino

Curated by ChEMBL
LigandPNGBDBM50457085(CHEMBL4203542)
Affinity DataKi:  0.0500nMAssay Description:Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM618729(US20230293517, Example 4.7)
Affinity DataKi:  0.0500nMAssay Description:All FRET binding experiments were conducted at room temperature in white 384-well plates, in assay binding buffer containing 1×LabMed (Cisbio, France...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2023
Entry Details
US Patent

TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50085674((2S,3S,4R,5R)-5-[2-(4-Amino-cyclohexylamino)-6-(2,...)
Affinity DataKi:  0.0500nMAssay Description:In vitro inhibition of human neutrophil activation via Adenosine A2A receptor.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/2/2012
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM618748(US20230293517, Example 4.26)
Affinity DataKi:  0.0500nMAssay Description:All FRET binding experiments were conducted at room temperature in white 384-well plates, in assay binding buffer containing 1×LabMed (Cisbio, France...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2023
Entry Details
US Patent

TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50211087(CHEMBL3958838)
Affinity DataIC50: 0.0510nMAssay Description:Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/11/2018
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50449634(CHEMBL4167125)
Affinity DataIC50: 0.0590nMAssay Description:Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Rat)
University of Camerino

Curated by ChEMBL
LigandPNGBDBM50457098(CHEMBL4217582)
Affinity DataKi:  0.0600nMAssay Description:Antagonist activity at rat A2A receptor assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 mins followed by CGS-21680 addition m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50457098(CHEMBL4217582)
Affinity DataKi:  0.0600nMAssay Description:Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50493156(CHEMBL2419150)
Affinity DataKi:  0.0670nMAssay Description:Displacement of [3H]ZM241385 from human A2A receptor expressed in HEK293 cell membranes after 60 mins by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM550787(7-Phenyl-8-(quinolin-6-yl)-[1,2,4]triazolo[4,3-c]p...)
Affinity DataIC50: 0.0700nMAssay Description:CHO-K1/A2aR cells were cultured in DMEM/F12 medium containing 10% fetal bovine serum and 800 μg/ml bleomycin. The cells were digested with the c...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2022
Entry Details
US Patent

TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50457084(CHEMBL4217248)
Affinity DataKi:  0.0700nMAssay Description:Antagonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as reduction in CGS-21680-induced cAMP level pretreated for 15 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM761416(N-[4-(3-Cyanophenyl)-5-(3-methylbenzimidazol-5-yl)...)
Affinity DataKi:  0.0700nMMore data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
TBA
Entry Details
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM761364(4-Cyano-N-[4-(3-cyanophenyl)-5-(4-methylquinazolin...)
Affinity DataKi:  0.0700nMMore data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
TBA
Entry Details
TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM550787(7-Phenyl-8-(quinolin-6-yl)-[1,2,4]triazolo[4,3-c]p...)
Affinity DataIC50: 0.0700nMAssay Description:CHO-K1/A2aR cells were cultured in DMEM/F12 medium containing 10% fetal bovine serum and 800 μg/ml bleomycin. The cells were digested with the c...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2022
Entry Details
US Patent

TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM50496134(CHEMBL3121726)
Affinity DataKi:  0.0720nMAssay Description:Displacement of [3H]-NECA from human recombinant adenosine A2A receptor expressed in CHO cell membranes after 3 hrs by microbeta counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2020
Entry Details Article
PubMed
TargetAdenosine receptor A2a(Human)
University of Virginia

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)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM616065(US20230271964, Example 1-22)
Affinity DataKi:  0.0790nMAssay Description:Inhibition binding assays were performed using 0.2 µg of membranes prepared from HEK293 cells infected with BacMam human adenosine A2A receptor or 1....More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/16/2023
Entry Details
US Patent

TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM616103(US20230271964, Example 1-60 | US20230271964, Examp...)
Affinity DataKi:  0.0790nMAssay Description:Inhibition binding assays were performed using 0.2 µg of membranes prepared from HEK293 cells infected with BacMam human adenosine A2A receptor or 1....More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/16/2023
Entry Details
US Patent

TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM550788(8-(2-Chloro-6-methylpyridin-4-yl)-7-phenyl-[1,2,4]...)
Affinity DataIC50: 0.0800nMAssay Description:CHO-K1/A2aR cells were cultured in DMEM/F12 medium containing 10% fetal bovine serum and 800 μg/ml bleomycin. The cells were digested with the c...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2022
Entry Details
US Patent

TargetAdenosine receptor A2a(Human)
University of Virginia

Curated by ChEMBL
LigandPNGBDBM683511(US20240217978, Example 166 | (2S)-2-((7-amino-2-(f...)
Affinity DataIC50: 0.0800nMAssay Description:A radioligand binding test was conducted by using [3H]-NECA (5′-N-[adenine-2,8-3H]-ethylcarboxamidoadenosine) and an adenosine A2a membrane. As...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2024
Entry Details
US Patent

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