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. Author manuscript; available in PMC: 2024 Sep 20.
Published in final edited form as: J Am Chem Soc. 2023 Sep 11;145(37):20539–20550. doi: 10.1021/jacs.3c06703

Table 2.

PTHR1 β-arrestin-1 and −2 Recruitment and NLuc-PTHR1 Affinity for PTH(1-34) and α/β/γ-Analogues 1 and 2.

β-arrestin-1 Recruitment β-arrestin-2 Recruitment NLuc-PTHR1 Affinity
Peptide pEC50 EC50
(nM)
EC50
relative
% Max pEC50 EC50
(nM)
EC50
relative
% Max pIC50 IC50
(nM)
IC50
relative
PTH(1-34) 8.1 ± 0.1 7.2 1 101 ± 3 8.2 ± 0.1 6.8 1 101 ± 3 7.6 ± 0.1 22 1
1 7.0 ± 0.2 100 14 27 ± 3 7.0 ± 0.4 100 15 21 ± 4 6.9 ± 0.1 130 6
2 6.7 ± 0.3 190 26 39 ± 8 7.0 ± 0.4 110 16 30 ± 8 6.1 ± 0.1 720 33

For β-arrestin-1 recruitment, pEC50, EC50 and maximal response (% Max) values represent the average of ≥4 independent experiments. For β-arrestin-2 recruitment, pEC50, EC50 and % Max are the average of ≥3 independent experiments. pEC50 indicates the negative logarithm of the half-maximal effective concentration (EC50). NLuc-PTHR1 pIC50 and IC50 values are the average of 3 independent experiments. pIC50 indicates the negative logarithm of the half-maximal inhibitory concentration (IC50). EC50 and IC50 relative indicate β-arrestin-1 or −2 recruitment potency or NLuc-PTHR1 affinity normalized to PTH(1-34) by the quotient (α/β/γ-analogue/PTH(1-34)). pEC50, pIC50 and % Max uncertainties are expressed as SEM.