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] |
The geometric mean of replicate experiments is reported.