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Assay Detail

CHEMBL646636

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

Binding
Binding affinity towards Adenosine A3 receptor (W243 mutant receptor)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.
Gao ZG, Kim SK, Biadatti T, Chen W, Lee K, Barak D, Kim SG, Johnson CR, Jacobson KA.
J Med Chem (2002) 45 : 4471 -4484
PubMed 12238926 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.25 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL342873 1 8.89
CHEMBL307199 1 8.62
CHEMBL284969 1 7.00
CHEMBL344698 1 6.09
CHEMBL111545 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL342873 Ki = 1.3 nM 8.89
CHEMBL307199 Ki = 2.4 nM 8.62
CHEMBL284969 Ki = 100.0 nM 7.00
CHEMBL344698 Ki = 818.0 nM 6.09
CHEMBL111545 Ki = 2150.0 nM 5.67