Our potent and selective hA_2A adenosine receptor fluorescent antagonist shows high affinity and selectivity for hA_2A receptor (K_i = 10.9 nM for hA_2A, 40 %, 47 % and 20 % of displacement at 1 µM concentration for hA₁, hA_2B, and hA₃, respectively in radioligand binding assay). It enables the performance of NanoBRET® competition binding assays (see our application note in collaboration with Promega and the University of Western Australia – App Note Promega-Celtarys), cell visualization in fluorescence microscopy, confocal microscopy, and high-content imaging experiments.