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. Author manuscript; available in PMC: 2023 Feb 24.
Published in final edited form as: J Med Chem. 2022 Feb 4;65(4):3218–3228. doi: 10.1021/acs.jmedchem.1c01709

Table 1.

In vitro Potency of Compounds 1a-t as MRGPRX1 PAMsa,b

Cmpd Structure EC50 (μM)a
(Emax)b 		Cmpd Structure EC50 (μM)a
(Emax)b
1a graphic file with name nihms-1810113-t0002.jpg 0.48 ± 0.04
(118%)		 1k graphic file with name nihms-1810113-t0003.jpg >100
1b graphic file with name nihms-1810113-t0004.jpg 14.5 ± 1.1
(88%)		 1l graphic file with name nihms-1810113-t0005.jpg 4.2 ± 1.1
(95%)
1c graphic file with name nihms-1810113-t0006.jpg 1.6 ± 0.4
(89%)		 1m graphic file with name nihms-1810113-t0007.jpg 1.7 ± 0.2
(94%)
1d graphic file with name nihms-1810113-t0008.jpg 25
(40%)		 1n graphic file with name nihms-1810113-t0009.jpg 1.5 ± 0.2
(90%)
1e graphic file with name nihms-1810113-t0010.jpg 2.7 ± 1.5
(88%)		 1o graphic file with name nihms-1810113-t0011.jpg 2.1 ± 0.4
(94%)
1f graphic file with name nihms-1810113-t0012.jpg 0.22 ± 0.02
(112%)		 1p graphic file with name nihms-1810113-t0013.jpg 0.32 ± 0.06
(105%)
1g graphic file with name nihms-1810113-t0014.jpg 30
(55%)		 1q graphic file with name nihms-1810113-t0015.jpg 0.34 ± 0.07
(95%)
1h graphic file with name nihms-1810113-t0016.jpg 1.1 ± 0.2
(83%)		 1r graphic file with name nihms-1810113-t0017.jpg 0.30 ± 0.13
(145%)
1i graphic file with name nihms-1810113-t0018.jpg 0.52 ± 0.03
(95%)		 1s graphic file with name nihms-1810113-t0019.jpg 0.23 ± 0.05
(143%)
1j graphic file with name nihms-1810113-t0020.jpg >100 1t graphic file with name nihms-1810113-t0021.jpg 0.10 ± 0.01
(114%)
a

Values are mean ± standard error of the mean (SEM) of at least three independent experiments performed in quadruplicate.

b

Emax values were defined as response elicited by maximum concentration of test compounds in the presence of EC20 concentration of BAM8–22 normalized to that elicited by 250 nM (>EC100) of BAM8–22 alone.