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Assay Detail

CHEMBL5128611

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Functional
Antagonist activity at human adenosine A2A receptor
7
Total Activities
7
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 A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.
Zhong Z, He X, Ge J, Zhu J, Yao C, Cai H, Ye XY, Xie T, Bai R.
Eur J Med Chem (2022) 237 : 114378 -114378
PubMed 35462165 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.81 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5170337 1 9.66
CHEMBL184309 1 8.40
CHEMBL2105747 TOZADENANT 3.0 1 7.96
CHEMBL5182020 1 7.27
CHEMBL411329 (R,S)-MEFLOQUINE 1 7.21
CHEMBL426738 1 7.20
CHEMBL189192 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5170337 Ki = 0.22 nM 9.66
CHEMBL184309 Ki = 4.0 nM 8.40
CHEMBL2105747 TOZADENANT Ki = 11.0 nM 7.96
CHEMBL5182020 Ki = 54.0 nM 7.27
CHEMBL411329 (R,S)-MEFLOQUINE Ki = 61.0 nM 7.21
CHEMBL426738 Ki = 63.0 nM 7.20
CHEMBL189192 Ki = 100.0 nM 7.00