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Assay Detail

CHEMBL641314

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

Binding
Displacement of [3H]-CGS-21,680 or [3H]ZM-241385 binding in adenosine A2A receptor of rat striatal membrane was determined
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL302)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists.
van Muijlwijk-Koezen JE, Timmerman H, Vollinga RC, Frijtag von Drabbe Künzel J, de Groote M, Visser S, IJzerman AP.
J Med Chem (2001) 44 : 749 -762
PubMed 11262085 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.64 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL164745 1 6.24
CHEMBL164422 1 6.04
CHEMBL162808 1 5.89
CHEMBL163040 1 5.89
CHEMBL165971 2 5.72
CHEMBL60156 1 5.72
CHEMBL305322 1 5.64
CHEMBL165783 1 5.36
CHEMBL164087 1 5.06
CHEMBL354004 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL164745 Ki = 570.0 nM 6.24
CHEMBL164422 Ki = 920.0 nM 6.04
CHEMBL162808 Ki = 1300.0 nM 5.89
CHEMBL163040 Ki = 1300.0 nM 5.89
CHEMBL165971 Ki = 1900.0 nM 5.72
CHEMBL60156 Ki = 1900.0 nM 5.72
CHEMBL165971 Ki = 2000.0 nM 5.70
CHEMBL305322 Ki = 2300.0 nM 5.64
CHEMBL165783 Ki = 4400.0 nM 5.36
CHEMBL164087 Ki = 8700.0 nM 5.06
CHEMBL354004 Ki = 15000.0 nM 4.82