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. 2022 Oct 20;65(21):14305–14325. doi: 10.1021/acs.jmedchem.2c01338

Table 1. High-Throughput Screen (HTS) to Identify Inhibitors of Recombinant Perforin.

no. of cmpds inhibition of SRBC lysis ≥60% at 20 μMa inhibition of SRBC lysis IC50 ≤ 20 μMb inhibition of Jurkat cell lysis ≥60% at 80 μMc inhibition of Jurkat cell lysis ≥60% at 1 μMd
101024 612 132 30 9
a

Inhibition of recombinant perforin-mediated lysis of SRBC by compounds at a final concentration of 20 μM as determined by measuring cell turbidity detected by absorbance at a wavelength of 650 nM.

b

An IC50 was calculated from a five-point dose–response curve from compound concentrations of 100, 20, 4, 0.8, and 0.16 μM.

c

Inhibition of recombinant perforin-mediated lysis of nucleated (Jurkat T lymphoma) cells by compounds at a final concentration of 80 μM as determined by a 51Cr release assay in the presence of 0.1% bovine serum albumin.

d

Inhibition of recombinant perforin-mediated lysis of nucleated (Jurkat T lymphoma) cells by compounds at a final concentration of 1 μM as determined by a 51Cr release assay in the presence of 0.1% bovine serum albumin.