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Assay Detail

CHEMBL3267336

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Binding
Binding affinity to human recombinant adenosine receptor A2a
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Adenosine A2A receptor as a drug discovery target.
de Lera Ruiz M, Lim YH, Zheng J.
J Med Chem (2014) 57 : 3623 -3650
PubMed 24164628 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.40 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1950649 APADENOSON 3.0 1 9.30
CHEMBL3260724 1 8.40
CHEMBL3350613 1 8.19
CHEMBL464859 NECA 1 7.70
CHEMBL331372 CGS-21680 1 7.57
CHEMBL186113 GW-328267 1.0 1 7.34
CHEMBL487497 1 6.78
CHEMBL285819 1 6.75
CHEMBL1950554 BINODENOSON 3.0 1 6.57
CHEMBL317052 REGADENOSON ANHYDROUS 4.0 1 6.54
CHEMBL1950553 SONEDENOSON 2.0 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1950649 APADENOSON Ki = 0.5 nM 9.30
CHEMBL3260724 Ki = 4.0 nM 8.40
CHEMBL3350613 Ki = 6.4 nM 8.19
CHEMBL464859 NECA Ki = 20.0 nM 7.70
CHEMBL331372 CGS-21680 Ki = 27.0 nM 7.57
CHEMBL186113 GW-328267 Ki = 46.0 nM 7.34
CHEMBL487497 Ki = 167.0 nM 6.78
CHEMBL285819 Ki = 180.0 nM 6.75
CHEMBL1950554 BINODENOSON Ki = 270.0 nM 6.57
CHEMBL317052 REGADENOSON ANHYDROUS Ki = 290.0 nM 6.54
CHEMBL1950553 SONEDENOSON Ki = 490.0 nM 6.31