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Assay Detail

CHEMBL1211413

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Functional
Antagonist activity against human adenosine A2A receptor
22
Total Activities
22
Compounds Tested
2
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

Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.
Cheng F, Cheng F, Xu Z, Liu G, Tang Y.
Eur J Med Chem (2010) 45 : 3459 -3471
PubMed 20537438 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 6.35 7.39
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL468701 1 7.39
CHEMBL461007 1 7.14
CHEMBL17002 1 6.95
CHEMBL209230 1 6.79
CHEMBL411452 1 6.57
CHEMBL261526 1 6.51
CHEMBL485862 1 6.48
CHEMBL1210734 1 6.40
CHEMBL260975 1 6.35
CHEMBL212625 1 6.32
CHEMBL273807 1 6.30
CHEMBL405901 1 6.30
CHEMBL474058 1 6.21
CHEMBL275149 1 6.19
CHEMBL461656 1 6.08
CHEMBL378598 1 5.85
CHEMBL278039 1 5.29
CHEMBL474207 1 5.22
CHEMBL251876 1 -
CHEMBL252048 1 -
CHEMBL260331 1 -
CHEMBL1210733 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL468701 Ki = 41.0 nM 7.39
CHEMBL461007 Ki = 73.0 nM 7.14
CHEMBL17002 Ki = 112.0 nM 6.95
CHEMBL209230 Ki = 162.0 nM 6.79
CHEMBL411452 Ki = 272.0 nM 6.57
CHEMBL261526 Ki = 312.0 nM 6.51
CHEMBL485862 Ki = 328.0 nM 6.48
CHEMBL1210734 Ki = 400.0 nM 6.40
CHEMBL260975 Ki = 450.0 nM 6.35
CHEMBL212625 Ki = 484.0 nM 6.32
CHEMBL273807 Ki = 503.0 nM 6.30
CHEMBL405901 Ki = 496.0 nM 6.30
CHEMBL474058 Ki = 620.0 nM 6.21
CHEMBL275149 Ki = 642.0 nM 6.19
CHEMBL461656 Ki = 832.0 nM 6.08
CHEMBL378598 Ki = 1400.0 nM 5.85
CHEMBL278039 Ki = 5140.0 nM 5.29
CHEMBL474207 Ki = 6000.0 nM 5.22
CHEMBL251876 Ki > 5000.0 nM -
CHEMBL252048 Ki > 5000.0 nM -
CHEMBL260331 Ki > 1000.0 nM -
CHEMBL1210733 Activity = 12.0 % -