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. Author manuscript; available in PMC: 2020 Sep 3.
Published in final edited form as: Mol Pharm. 2019 Aug 16;16(9):3831–3841. doi: 10.1021/acs.molpharmaceut.9b00464

Table 1:

IC50 of compounds 1a-1h for PSMAα,β,γ.

graphic file with name nihms-1045022-t0009.jpg

Entry R IC50 (nM) Entry R IC50 (nM)
1a graphic file with name nihms-1045022-t0010.jpg 130.3±28.9 1f graphic file with name nihms-1045022-t0015.jpg 555.5±79.3
1b graphic file with name nihms-1045022-t0011.jpg 318.4±21.1 1g graphic file with name nihms-1045022-t0016.jpg 45.7±6.7
1c graphic file with name nihms-1045022-t0012.jpg 363.8±8.7 1h graphic file with name nihms-1045022-t0017.jpg 128.0±8.4
1d graphic file with name nihms-1045022-t0013.jpg 20.3±2.4 control 2-PMPA 523.5±84.0
1e graphic file with name nihms-1045022-t0014.jpg 536.8±58.7
α

Cell line in all cases is 22Rv1.

β

The competitive binding compound is 68Ga-PSMA-11.

γ

Cells were plated 48 h before testing (in triplicate). Various concentration (0.01–100000 nM) of compounds with 10 μCi of 68Ga-PSMA-11 were added to cells and incubated for 1h. Cells were washed and lysed. A gamma counter was used to measure the bound fraction to the lysed cells.