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Assay Detail

CHEMBL644669

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

Binding
Displacement of [3H]NECA from human adenosine A2A receptor in stably transfected CHO cells
11
Total Activities
11
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

2-(N-acyl) and 2-N-acyl-N(6)-substituted analogues of adenosine and their affinity at the human adenosine receptors.
Jagtap PG, Chen Z, Szabó C, Klotz KN.
Bioorg Med Chem Lett (2004) 14 : 1495 -1498
PubMed 15006389 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.47 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288258 1 5.75
CHEMBL36320 1 5.71
CHEMBL36786 1 5.70
CHEMBL36098 1 5.66
CHEMBL284969 1 5.64
CHEMBL36789 1 5.62
CHEMBL285251 1 5.39
CHEMBL289982 1 5.34
CHEMBL279391 1 5.25
CHEMBL36160 1 5.11
CHEMBL36734 1 4.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288258 Ki = 1780.0 nM 5.75
CHEMBL36320 Ki = 1940.0 nM 5.71
CHEMBL36786 Ki = 2000.0 nM 5.70
CHEMBL36098 Ki = 2180.0 nM 5.66
CHEMBL284969 Ki = 2270.0 nM 5.64
CHEMBL36789 Ki = 2410.0 nM 5.62
CHEMBL285251 Ki = 4100.0 nM 5.39
CHEMBL289982 Ki = 4570.0 nM 5.34
CHEMBL279391 Ki = 5660.0 nM 5.25
CHEMBL36160 Ki = 7750.0 nM 5.11
CHEMBL36734 Ki = 10800.0 nM 4.97