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Assay Detail

CHEMBL1120795

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
27
Total Activities
27
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

Novel N2-substituted pyrazolo[3,4-d]pyrimidine adenosine A3 receptor antagonists: inhibition of A3-mediated human glioblastoma cell proliferation.
Taliani S, La Motta C, Mugnaini L, Simorini F, Salerno S, Marini AM, Da Settimo F, Cosconati S, Cosimelli B, Greco G, Limongelli V, Marinelli L, Novellino E, Ciampi O, Daniele S, Trincavelli ML, Martini C.
J Med Chem (2010) 53 : 3954 -3963
PubMed 20408530 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.58 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 8.41
CHEMBL464859 NECA 1 7.85
CHEMBL1098075 1 7.57
CHEMBL1094143 1 7.28
CHEMBL515442 1 6.92
CHEMBL1094132 1 6.54
CHEMBL1094987 1 6.51
CHEMBL1096754 1 6.48
CHEMBL1096753 1 6.23
CHEMBL1098108 1 5.98
CHEMBL1096409 1 5.98
CHEMBL1098109 1 5.97
CHEMBL1096410 1 5.77
CHEMBL1097050 1 5.62
CHEMBL1097737 1 5.60
CHEMBL1096693 1 -
CHEMBL1096692 1 -
CHEMBL1094442 1 -
CHEMBL1095748 1 -
CHEMBL1095747 1 -
CHEMBL1097736 1 -
CHEMBL1096078 1 -
CHEMBL1094131 1 -
CHEMBL1099102 1 -
CHEMBL1098759 1 -
CHEMBL1098758 1 -
CHEMBL1098445 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 3.9 nM 8.41
CHEMBL464859 NECA Ki = 14.0 nM 7.85
CHEMBL1098075 Ki = 27.0 nM 7.57
CHEMBL1094143 Ki = 53.0 nM 7.28
CHEMBL515442 Ki = 120.0 nM 6.92
CHEMBL1094132 Ki = 290.0 nM 6.54
CHEMBL1094987 Ki = 312.0 nM 6.51
CHEMBL1096754 Ki = 334.0 nM 6.48
CHEMBL1096753 Ki = 584.7 nM 6.23
CHEMBL1098108 Ki = 1037.0 nM 5.98
CHEMBL1096409 Ki = 1050.0 nM 5.98
CHEMBL1098109 Ki = 1081.6 nM 5.97
CHEMBL1096410 Ki = 1700.0 nM 5.77
CHEMBL1097050 Ki = 2400.0 nM 5.62
CHEMBL1097737 Ki = 2500.0 nM 5.60
CHEMBL1096693 Ki > 10000.0 nM -
CHEMBL1096692 Ki > 10000.0 nM -
CHEMBL1094442 Ki > 10000.0 nM -
CHEMBL1095748 Ki > 10000.0 nM -
CHEMBL1095747 Ki > 10000.0 nM -
CHEMBL1097736 Ki > 10000.0 nM -
CHEMBL1096078 Ki > 10000.0 nM -
CHEMBL1094131 Ki > 10000.0 nM -
CHEMBL1099102 Ki > 10000.0 nM -
CHEMBL1098759 Ki > 10000.0 nM -
CHEMBL1098758 Ki > 10000.0 nM -
CHEMBL1098445 Ki > 10000.0 nM -