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Assay Detail

CHEMBL2073178

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

Binding
Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells after 120 mins by scintillation counter
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Water-soluble pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines as human A₃ adenosine receptor antagonists.
Baraldi PG, Saponaro G, Romagnoli R, Aghazadeh Tabrizi M, Baraldi S, Moorman AR, Cosconati S, Di Maro S, Marinelli L, Gessi S, Merighi S, Varani K, Borea PA, Preti D.
J Med Chem (2012) 55 : 5380 -5390
PubMed 22568637 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 6.12 6.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2071045 1 6.95
CHEMBL2070891 1 6.78
CHEMBL2069325 1 6.74
CHEMBL118923 1 6.46
CHEMBL2071038 1 6.46
CHEMBL2070892 1 6.43
CHEMBL2071048 1 6.40
CHEMBL2071046 1 6.39
CHEMBL2071044 1 6.28
CHEMBL2071047 1 6.21
CHEMBL2071049 1 6.20
CHEMBL2070886 1 6.15
CHEMBL2070888 1 6.14
CHEMBL2071041 1 6.13
CHEMBL2071042 1 6.12
CHEMBL2070884 1 6.10
CHEMBL2071043 1 6.09
CHEMBL2070887 1 5.98
CHEMBL302765 1 5.96
CHEMBL2071051 1 5.95
CHEMBL2070890 1 5.94
CHEMBL2070894 1 5.92
CHEMBL2071050 1 5.89
CHEMBL2071040 1 5.88
CHEMBL2070893 1 5.88
CHEMBL2070889 1 5.83
CHEMBL2071039 1 5.82
CHEMBL2070882 1 5.55
CHEMBL2070885 1 5.47
CHEMBL2070883 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2071045 Ki = 112.0 nM 6.95
CHEMBL2070891 Ki = 166.0 nM 6.78
CHEMBL2069325 Ki = 182.0 nM 6.74
CHEMBL118923 Ki = 350.0 nM 6.46
CHEMBL2071038 Ki = 348.0 nM 6.46
CHEMBL2070892 Ki = 371.0 nM 6.43
CHEMBL2071048 Ki = 396.0 nM 6.40
CHEMBL2071046 Ki = 408.0 nM 6.39
CHEMBL2071044 Ki = 525.0 nM 6.28
CHEMBL2071047 Ki = 614.0 nM 6.21
CHEMBL2071049 Ki = 635.0 nM 6.20
CHEMBL2070886 Ki = 703.0 nM 6.15
CHEMBL2070888 Ki = 724.0 nM 6.14
CHEMBL2071041 Ki = 744.0 nM 6.13
CHEMBL2071042 Ki = 761.0 nM 6.12
CHEMBL2070884 Ki = 802.0 nM 6.10
CHEMBL2071043 Ki = 805.0 nM 6.09
CHEMBL2070887 Ki = 1049.0 nM 5.98
CHEMBL302765 Ki = 1100.0 nM 5.96
CHEMBL2071051 Ki = 1123.0 nM 5.95
CHEMBL2070890 Ki = 1156.0 nM 5.94
CHEMBL2070894 Ki = 1188.0 nM 5.92
CHEMBL2071050 Ki = 1299.0 nM 5.89
CHEMBL2071040 Ki = 1324.0 nM 5.88
CHEMBL2070893 Ki = 1329.0 nM 5.88
CHEMBL2070889 Ki = 1478.0 nM 5.83
CHEMBL2071039 Ki = 1500.0 nM 5.82
CHEMBL2070882 Ki = 2794.0 nM 5.55
CHEMBL2070885 Ki = 3408.0 nM 5.47
CHEMBL2070883 Ki = 3357.0 nM 5.47
CHEMBL2070880 Ki > 5000.0 nM -
CHEMBL2070881 Ki > 5000.0 nM -