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Assay Detail

CHEMBL4426297

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

Binding
Displacement of [3H]-ZM241385 from wild type human adenosine receptor A2a expressed in HEK293 cell membranes after 240 mins by scintillation counting
5
Total Activities
5
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

Controlling the Dissociation of Ligands from the Adenosine A2A Receptor through Modulation of Salt Bridge Strength.
Segala E, Guo D, Cheng RK, Bortolato A, Deflorian F, Doré AS, Errey JC, Heitman LH, IJzerman AP, Marshall FH, Cooke RM.
J Med Chem (2016) 59 : 6470 -6479
PubMed 27312113 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.74 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL184061 1 9.48
CHEMBL113142 ZM-241385 1 9.40
CHEMBL187810 1 8.89
CHEMBL3937413 1 8.42
CHEMBL3934661 1 7.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL184061 Ki = 0.33 nM 9.48
CHEMBL113142 ZM-241385 Ki = 0.4 nM 9.40
CHEMBL187810 Ki = 1.3 nM 8.89
CHEMBL3937413 Ki = 3.8 nM 8.42
CHEMBL3934661 Ki = 31.0 nM 7.51