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Assay Detail

CHEMBL4018971

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

Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of 2-Cl-IB-MECA-induced [35S]GTPgammaS binding preincubated with or without for 60 mins followed by addition of 2-Cl-IB-MECA and [35S]GTPgammaS measured after 30 mins
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structure-Affinity Relationships and Structure-Kinetics Relationships of Pyrido[2,1-f]purine-2,4-dione Derivatives as Human Adenosine A3 Receptor Antagonists.
Xia L, Burger WAC, van Veldhoven JPD, Kuiper BJ, van Duijl TT, Lenselink EB, Paasman E, Heitman LH, IJzerman AP.
J Med Chem (2017) 60 : 7555 -7568
PubMed 28806076 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 6.80 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL322968 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL322968 Kd = 158.49 nM 6.80