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Assay Detail

CHEMBL1286671

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Binding
Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO-A1 cells after 60 mins
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-A1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A1 (CHEMBL226)
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 26 6.65 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 8.49
CHEMBL1277025 1 7.99
CHEMBL1277116 1 7.94
CHEMBL1277925 1 7.55
CHEMBL1277845 1 7.36
CHEMBL1278010 1 7.32
CHEMBL1277846 1 7.14
CHEMBL1278102 1 7.07
CHEMBL1276939 1 7.03
CHEMBL213425 1 6.98
CHEMBL1276938 1 6.91
CHEMBL1278011 1 6.74
CHEMBL1277926 1 6.72
CHEMBL1277024 1 6.72
CHEMBL1276852 1 6.60
CHEMBL1278104 1 6.57
CHEMBL1278194 1 6.32
CHEMBL1277480 1 6.25
CHEMBL1276851 1 5.84
CHEMBL1277302 1 5.80
CHEMBL1276853 1 5.79
CHEMBL1277301 1 5.62
CHEMBL1277390 1 5.61
CHEMBL1277207 1 5.51
CHEMBL1277667 1 5.49
CHEMBL382494 1 5.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 3.2 nM 8.49
CHEMBL1277025 Ki = 10.2 nM 7.99
CHEMBL1277116 Ki = 11.4 nM 7.94
CHEMBL1277925 Ki = 28.3 nM 7.55
CHEMBL1277845 Ki = 43.6 nM 7.36
CHEMBL1278010 Ki = 47.4 nM 7.32
CHEMBL1277846 Ki = 71.8 nM 7.14
CHEMBL1278102 Ki = 85.3 nM 7.07
CHEMBL1276939 Ki = 92.7 nM 7.03
CHEMBL213425 Ki = 104.3 nM 6.98
CHEMBL1276938 Ki = 122.9 nM 6.91
CHEMBL1278011 Ki = 180.2 nM 6.74
CHEMBL1277926 Ki = 192.3 nM 6.72
CHEMBL1277024 Ki = 188.5 nM 6.72
CHEMBL1276852 Ki = 252.3 nM 6.60
CHEMBL1278104 Ki = 267.4 nM 6.57
CHEMBL1278194 Ki = 475.2 nM 6.32
CHEMBL1277480 Ki = 563.5 nM 6.25
CHEMBL1276851 Ki = 1432.0 nM 5.84
CHEMBL1277302 Ki = 1595.0 nM 5.80
CHEMBL1276853 Ki = 1616.0 nM 5.79
CHEMBL1277301 Ki = 2385.0 nM 5.62
CHEMBL1277390 Ki = 2445.0 nM 5.61
CHEMBL1277207 Ki = 3080.0 nM 5.51
CHEMBL1277667 Ki = 3245.0 nM 5.49
CHEMBL382494 Ki = 3250.0 nM 5.49