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. 2022 Dec 30;6(1):151–170. doi: 10.1021/acsptsci.2c00202

Figure 2.

Figure 2

Functional profiling of ML321 against an array of 168 known GPCRs. A single high concentration (10 μM) of ML321 was screened using a β-arrestin recruitment assay in the DiscoverX gpcrMAX assay panel in both antagonist (A) or agonist (B) modes as described in the Methods. Data represent the percent maximum stimulation (agonist mode) observed by a reference agonist for each GPCR or the percent inhibition (antagonist mode) of a response produced by an EC80 concentration of a reference agonist for each GPCR. A complete key to the GPCR array and numerical results are provided in Table S2. Only responses that deviated >20% from the baseline are considered to be significant. In panel (A), these include the following receptors (% activity): D2RL (98%), D2RS (98%), D3R (72%), 5-HT2A (48%), 5-HT2C (35%), BLT1 (leukotriene B4) (LTB4R) (37%), sphingosine-1-phosphate 4 (S1PR4) (36%), α2C-adrenergic (31%); and in panel (B), CB2 cannabinoid (44%).