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. Author manuscript; available in PMC: 2020 Aug 10.
Published in final edited form as: Nature. 2020 Feb 10;579(7800):609–614. doi: 10.1038/s41586-020-2027-0

Extended Data Table 4:

Probe pairs of in vivo tested molecules

Active Selective Probe (Sigma RefCode) hMT1 pEC50a (% Emax) n hMT2 pEC50b (% Emax) n Inactive analog (Sigma RefCode) hMT1 pEC50a hMT2 pEC50b
graphic file with name nihms-1555350-t0046.jpg
ZINC555417447
(SML2751)		 Inverse 7.4 ± 0.10
(Inverse 62 ± 13)
n=8		 Inverse 5.7 ± 0.10
(Inverse 84 ± 9)
n=8		 graphic file with name nihms-1555350-t0047.jpg
ZINC37781618
(SML2752)		 <4.5
n=3		 <4.5
n=3
graphic file with name nihms-1555350-t0048.jpg
ZINC 128734226
(SML2753)		 6.8 ±0.2
(79 ± 3) n=4		 8.2 ±0.1
(89 ± 3) n=4		 graphic file with name nihms-1555350-t0049.jpg
Z3670677764
(SML2754)		 <4.5
n=3 		<4.5
n=3
a, b.

The log half maximal concentration (pEC50) for inhibition of isoproterenol-stimulated cAMP production on hMT1 or hMT2 melatonin receptors transiently expressed in HEK cells. Values in parenthesis represent the percentage of the maximal inhibition normalized to % melatonin response for ‘4226, and to % basal activity for ‘7447. Compounds were tested at concentrations up to 30μM. Data represent mean ± s.e.m. from the indicated number (n) of biologically independent experiments run in triplicate.

UCSF4226 (‘4226), UCSF7447 (‘7447)