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Assay Detail

CHEMBL1286673

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]ZM241385 from human adenosine A2a receptor expressed in HeLa cells after 30 mins
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands.
Giovannoni MP, Vergelli C, Cilibrizzi A, Crocetti L, Biancalani C, Graziano A, Dal Piaz V, Loza MI, Cadavid MI, Díaz JL, Gavaldà A.
Bioorg Med Chem (2010) 18 : 7890 -7899
PubMed 20937560 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.97 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1277025 1 7.17
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 6.58
CHEMBL1277845 1 6.30
CHEMBL1278104 1 6.24
CHEMBL1277925 1 6.11
CHEMBL1277116 1 6.09
CHEMBL1278010 1 5.67
CHEMBL1277846 1 5.60
CHEMBL1276853 1 5.50
CHEMBL1277926 1 5.29
CHEMBL1278102 1 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1277025 Ki = 67.9 nM 7.17
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 260.0 nM 6.58
CHEMBL1277845 Ki = 501.2 nM 6.30
CHEMBL1278104 Ki = 572.1 nM 6.24
CHEMBL1277925 Ki = 772.5 nM 6.11
CHEMBL1277116 Ki = 805.1 nM 6.09
CHEMBL1278010 Ki = 2115.0 nM 5.67
CHEMBL1277846 Ki = 2490.0 nM 5.60
CHEMBL1276853 Ki = 3150.0 nM 5.50
CHEMBL1277926 Ki = 5190.0 nM 5.29
CHEMBL1278102 Ki = 7365.0 nM 5.13