Table 2 The affinities of antagonists and labelled probes described in this study
From: Characterisation of IL-23 receptor antagonists and disease relevant mutants using fluorescent probes
Probe | Assay | Constructs expressed | Ki or Kd | N |
|---|---|---|---|---|
IL12p40 | IL23-TMR Competition (Fig. 1) | NL-IL23R and IL12Rβ1 | 12.4 ± 1.4 nM | 5 |
IL12p40 | P630-TMR Competition (Fig. 5) | NL-IL23R and IL12Rβ1 | Did not displace labelled probe | 5 |
TEEEQQLY | IL23-TMR Competition (Fig. 1) | NL-IL23R and IL12Rβ1 | Did not displace labelled probe | 5 |
TEEEQQLY | P630-TMR Competition (Fig. 5) | NL-IL23R and IL12Rβ1 | Did not displace labelled probe | 3 |
P630 | IL23-TMR Competition (Fig. 1) | NL-IL23R and IL12Rβ1 | 21.8 ± 3.4 nM | 5 |
P630 | P630-TMR Competition (Fig. 5) | NL-IL23R and IL12Rβ1 | 6.32 ± 1.06 nM | 5 |
IL12p80 | IL23-TMR Competition (Fig. 1) | NL-IL23R and IL12Rβ1 | 469 ± 210 pM | 5 |
IL12p80 | P630-TMR Competition (Fig. 5) | NL-IL23R and IL12Rβ1 | Did not displace labelled probe | 5 |
IL-23 | IL23-TMR Competition (Fig. 1) | NL-IL23R and IL12Rβ1 | 31.6 ± 7.7 pM (Lay et al.24) | 13 |
IL-23 | P630-TMR Competition (Fig. 5) | NL-IL23R and IL12Rβ1 | 22.6 ± 5.2 pM | 5 |
P630-TMR | NL-IL23R and IL12Rβ1 | 51.1 ± 7.3 nM | 5 | |
P630-TMR | NL-IL23R | 101 ± 4 nM | 5 | |
P630-TMR | NL-IL12Rβ1 and IL23R | 55.2 ± 10.5 nM | 5 | |
P630-TMR | NL-IL12Rβ1 | Did not bind | 3 | |
P630-TMR | HiBit-IL23R and LgBit- IL12Rβ1 | 53.5 ± 4.4 nM | 3 |
