Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1024667

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

Binding
Displacement of [3H]SCH58261 from human adenosine A2A receptor expressed in HEK293 cells
30
Total Activities
30
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

Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines.
Neustadt BR, Liu H, Hao J, Greenlee WJ, Stamford AW, Foster C, Arik L, Lachowicz J, Zhang H, Bertorelli R, Fredduzzi S, Varty G, Cohen-Williams M, Ng K.
Bioorg Med Chem Lett (2009) 19 : 967 -971
PubMed 19109019 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 8.66 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL480570 1 9.52
CHEMBL480542 1 9.52
CHEMBL470942 1 9.52
CHEMBL514939 1 9.30
CHEMBL480380 1 9.15
CHEMBL473440 1 9.15
CHEMBL512337 1 9.10
CHEMBL473431 1 9.05
CHEMBL363660 1 9.00
CHEMBL519271 1 9.00
CHEMBL521242 1 8.85
CHEMBL473439 1 8.82
CHEMBL361687 1 8.82
CHEMBL480568 1 8.82
CHEMBL475445 1 8.80
CHEMBL482329 1 8.74
CHEMBL481736 1 8.74
CHEMBL520286 1 8.70
CHEMBL480756 1 8.60
CHEMBL480556 1 8.55
CHEMBL481737 1 8.55
CHEMBL482161 1 8.52
CHEMBL520766 1 8.24
CHEMBL471976 1 8.24
CHEMBL480397 1 8.22
CHEMBL480749 1 8.02
CHEMBL471974 1 7.94
CHEMBL482328 1 7.60
CHEMBL475592 1 7.40
CHEMBL471975 1 7.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL480570 Ki = 0.3 nM 9.52
CHEMBL480542 Ki = 0.3 nM 9.52
CHEMBL470942 Ki = 0.3 nM 9.52
CHEMBL514939 Ki = 0.5 nM 9.30
CHEMBL480380 Ki = 0.7 nM 9.15
CHEMBL473440 Ki = 0.7 nM 9.15
CHEMBL512337 Ki = 0.8 nM 9.10
CHEMBL473431 Ki = 0.9 nM 9.05
CHEMBL363660 Ki = 1.0 nM 9.00
CHEMBL519271 Ki = 1.0 nM 9.00
CHEMBL521242 Ki = 1.4 nM 8.85
CHEMBL473439 Ki = 1.5 nM 8.82
CHEMBL361687 Ki = 1.5 nM 8.82
CHEMBL480568 Ki = 1.5 nM 8.82
CHEMBL475445 Ki = 1.6 nM 8.80
CHEMBL482329 Ki = 1.8 nM 8.74
CHEMBL481736 Ki = 1.8 nM 8.74
CHEMBL520286 Ki = 2.0 nM 8.70
CHEMBL480756 Ki = 2.5 nM 8.60
CHEMBL480556 Ki = 2.8 nM 8.55
CHEMBL481737 Ki = 2.8 nM 8.55
CHEMBL482161 Ki = 3.0 nM 8.52
CHEMBL520766 Ki = 5.8 nM 8.24
CHEMBL471976 Ki = 5.7 nM 8.24
CHEMBL480397 Ki = 6.0 nM 8.22
CHEMBL480749 Ki = 9.5 nM 8.02
CHEMBL471974 Ki = 11.5 nM 7.94
CHEMBL482328 Ki = 25.0 nM 7.60
CHEMBL475592 Ki = 40.0 nM 7.40
CHEMBL471975 Ki = 46.0 nM 7.34