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. 2025 Jul 9;68(14):14195–14222. doi: 10.1021/acs.jmedchem.5c00781

9. Affinity of NLRP3 Inhibitors from Cell-Based NanoBRET Tracer Competition Binding Experiments in Human HEK293 Cells.

  binding affinity K i  (nM) (n) [pK i ± SD]
inhibitor MCC950 analogue as tracer 28 as tracer
MCC950 14 (5) [7.6 ± 0.3] 19 (6) [7.7 ± 0.2]
4 18 (5) [7.8 ± 0.3] 11 (6) [7.9 ± 0.1]
17 2.7 (3) [8.6 ± 0.1] 4.0 (6) [8.4 ± 0.1]
21 4.3 (5) [8.4 ± 0.2] 2.3 (5) [8.6 ± 0.1]
25 14 (5) [7.9 ± 0.3] 16 (6) [7.8 ± 0.1]
a

The geometric mean of replicate experiments is reported.