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Assay Detail

CHEMBL4262959

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

Binding
Displacement of MRS7416 from recombinant human adenosine receptor A1 expressed in HEK293 cell membranes after 1 hr by FACS analysis
2
Total Activities
2
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 A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bitopic fluorescent antagonists of the A2A adenosine receptor based on pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine functionalized congeners.
Duroux R, Ciancetta A, Mannes P, Yu J, Boyapati S, Gizewski E, Yous S, Ciruela F, Auchampach JA, Gao ZG, Jacobson KA.
Medchemcomm (2017) 8 : 1659 -1667
PubMed 29250307 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.09 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL136689 1 8.42
CHEMBL273094 XANTHINE AMINE CONGENER 1 7.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL136689 Ki = 3.8 nM 8.42
CHEMBL273094 XANTHINE AMINE CONGENER Ki = 17.2 nM 7.76