Fig. 7: Pharmacological characterisation of proposed A2A ligands. | Nature Communications

Fig. 7: Pharmacological characterisation of proposed A2A ligands.

From: Identification of nanomolar adenosine A2A receptor ligands using reinforcement learning and structure-based drug design

Fig. 7: Pharmacological characterisation of proposed A2A ligands.

Compounds of interest were tested in cAMP accumulation assays (Cisbio) in A2A (a, b) and A2B (c, d) CHO-K1 cells. Compounds were tested alone to determine agonist activity (a, c) or in the presence of an EC80 of NECA (b, d). Overexpression of the wild-type A2A receptor resulted in high levels of constitutive activity. Agonist data was normalised to DMSO control and 10 µM NECA, and was plotted using GraphPad Prism v10, using non-linear regression (four parameter fit). Antagonist data were normalised to assay controls, where 100% response equalled 6 nM NECA (A2A) or 19 nM NECA (A2B) and 0% response equalled 10 μM literature antagonist AB928 (A2A) or GS6201 (A2B). a–d Three technical replicates (n = 3) were conducted with the mean and standard deviation shown. Source data are provided as a Source Data file.

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