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Assay Detail

CHEMBL3749017

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

Binding
Displacement of [3H]2-[p(2-carboxyethyl)phenyl-ethylamino]-5'-N-ethylcarboxamido-adenosine from human adenosine A2A receptor stably expressed in HEK293 cell membrane by radioligand binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Design, Synthesis by Click Chemistry and in Vivo Activity of Highly Selective A3 Adenosine Receptor Agonists.
Tosh DK, Paoletta S, Chen Z, Crane S, Lloyd J, Gao ZG, Gizewski ET, Auchampach JA, Salvemini D, Jacobson KA.
Medchemcomm (2015) 6 : 555 -563
PubMed 26236460 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.76 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3747209 1 5.96
CHEMBL3746487 1 5.56
CHEMBL3745851 1 -
CHEMBL3746886 1 -
CHEMBL3746784 1 -
CHEMBL3746890 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3747209 Ki = 1110.0 nM 5.96
CHEMBL3746487 Ki = 2770.0 nM 5.56
CHEMBL3745851 Ki > 10000.0 nM -
CHEMBL3746886 Ki > 10000.0 nM -
CHEMBL3746784 Ki > 10000.0 nM -
CHEMBL3746890 Ki > 10000.0 nM -