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Assay Detail

CHEMBL5155956

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-ethylcarboxamidoadenosine from human A2A receptor stably expressed in HEK293 cell membrane by radioligand inhibition assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A<sub>3</sub> adenosine receptor agonists containing dopamine moieties for enhanced interspecies affinity.
Tosh DK, Salmaso V, Campbell RG, Rao H, Bitant A, Pottie E, Stove CP, Liu N, Gavrilova O, Gao ZG, Auchampach JA, Jacobson KA.
Eur J Med Chem (2022) 228 : 113983 -113983
PubMed 34844790 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.35 6.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5202349 1 6.23
CHEMBL5178814 1 5.33
CHEMBL5175945 1 5.31
CHEMBL5183720 1 5.30
CHEMBL5176856 1 5.23
CHEMBL5196916 1 5.09
CHEMBL5181821 1 4.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5202349 Ki = 588.0 nM 6.23
CHEMBL5178814 Ki = 4720.0 nM 5.33
CHEMBL5175945 Ki = 4860.0 nM 5.31
CHEMBL5183720 Ki = 5050.0 nM 5.30
CHEMBL5176856 Ki = 5860.0 nM 5.23
CHEMBL5196916 Ki = 8210.0 nM 5.09
CHEMBL5181821 Ki = 10200.0 nM 4.99