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Assay Detail

CHEMBL894344

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

Binding
Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells
9
Total Activities
9
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 Expert

Target

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

Publication

New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.
Colotta V, Catarzi D, Varano F, Capelli F, Lenzi O, Filacchioni G, Martini C, Trincavelli L, Ciampi O, Pugliese AM, Pedata F, Schiesaro A, Morizzo E, Moro S.
J Med Chem (2007) 50 : 4061 -4074
PubMed 17665891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.16 7.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL320805 1 7.04
CHEMBL107446 1 6.64
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 6.58
CHEMBL106346 1 6.48
CHEMBL388458 1 6.31
CHEMBL105913 1 5.97
CHEMBL388459 1 5.82
CHEMBL242424 1 5.54
CHEMBL1355736 THEOPHYLLINE 4.0 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL320805 Ki = 91.0 nM 7.04
CHEMBL107446 Ki = 228.0 nM 6.64
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 260.0 nM 6.58
CHEMBL106346 Ki = 329.0 nM 6.48
CHEMBL388458 Ki = 486.0 nM 6.31
CHEMBL105913 Ki = 1060.0 nM 5.97
CHEMBL388459 Ki = 1500.0 nM 5.82
CHEMBL242424 Ki = 2860.0 nM 5.54
CHEMBL1355736 THEOPHYLLINE Ki = 7900.0 nM 5.10