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Assay Detail

CHEMBL644953

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

Binding
Binding affinity against human recombinant Adenosine A3 receptor stably expressed in HEK293 cells by displacing [125I]AB-MECA radioligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.
Müller CE, Thorand M, Qurishi R, Diekmann M, Jacobson KA, Padgett WL, Daly JW.
J Med Chem (2002) 45 : 3440 -3450
PubMed 12139454 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.35 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1625681 1 8.64
CHEMBL1788234 1 8.01
CHEMBL117962 1 7.33
CHEMBL1788230 1 6.19
CHEMBL2112561 1 5.77
CHEMBL117899 1 5.48
CHEMBL113 CAFFEINE 4.0 1 4.88
CHEMBL2111766 1 4.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1625681 Ki = 2.3 nM 8.64
CHEMBL1788234 Ki = 9.8 nM 8.01
CHEMBL117962 Ki = 47.0 nM 7.33
CHEMBL1788230 Ki = 640.0 nM 6.19
CHEMBL2112561 Ki = 1700.0 nM 5.77
CHEMBL117899 Ki = 3330.0 nM 5.48
CHEMBL113 CAFFEINE Ki = 13300.0 nM 4.88
CHEMBL2111766 Ki = 30600.0 nM 4.51