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Assay Detail

CHEMBL888473

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

Binding
Displacement of [3H]CCPA from human adenosine A1 receptor in CHO cells
7
Total Activities
7
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 A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4'-thioadenosine derivatives without 4'-hydroxymethyl group as highly potent and selective antagonists.
Jeong LS, Choe SA, Gunaga P, Kim HO, Lee HW, Lee SK, Tosh DK, Patel A, Palaniappan KK, Gao ZG, Jacobson KA, Moon HR.
J Med Chem (2007) 50 : 3159 -3162
PubMed 17555308 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.94 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388145 1 7.26
CHEMBL200732 1 6.71
CHEMBL431733 NAMODENOSON 3.0 1 6.65
CHEMBL413686 1 5.60
CHEMBL373065 1 5.23
CHEMBL436485 1 5.21
CHEMBL344187 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388145 Ki = 55.4 nM 7.26
CHEMBL200732 Ki = 193.0 nM 6.71
CHEMBL431733 NAMODENOSON Ki = 222.0 nM 6.65
CHEMBL413686 Ki = 2490.0 nM 5.60
CHEMBL373065 Ki = 5870.0 nM 5.23
CHEMBL436485 Ki = 6220.0 nM 5.21
CHEMBL344187 Ki = 12100.0 nM 4.92