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Assay Detail

CHEMBL5042682

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

Binding
Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO-K1 cells by radioligand binding assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development and Application of Subtype-Selective Fluorescent Antagonists for the Study of the Human Adenosine A<sub>1</sub> Receptor in Living Cells.
Comeo E, Trinh P, Nguyen AT, Nowell CJ, Kindon ND, Soave M, Stoddart LA, White JM, Hill SJ, Kellam B, Halls ML, May LT, Scammells PJ.
J Med Chem (2021) 64 : 6670 -6695
PubMed 33724031 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.23 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4204703 1 9.00
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 7.40
CHEMBL464859 NECA 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4204703 Ki = 1.0 nM 9.00
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 39.81 nM 7.40
CHEMBL464859 NECA Ki = 5011.87 nM 5.30