Table 1.
a K D (μM) | |||
---|---|---|---|
Protein | Ligand | bITC or SPR | c Tm |
dBASE1 | Cmpd 3 | 14 ± 1.4 | 5.9 ± 0.59 |
Cmpd 4 | 5.4 ± 0.54 | 5 ± 0.5 | |
Cmpd 5 | 4.8 ± 0.48 | 3.1 ± 0.31 | |
Cmpd 6 | 3 ± 0.3 | 1.2 ± 0.12 | |
Cmpd 7 | 2.9 ± 0.29 | 0.9 ± 0.09 | |
Cmpd 8 | 2.9 ± 0.29 | 1.8 ± 0.18 | |
Cmpd 9 | 1.2 ± 0.12 | 2.3 ± 0.23 | |
Cmpd 10 | 0.6 ± 0.06 | 1.4 ± 0.14 | |
ecGAS | PF‐06928215 | 6.7 ± 0.67 | 3.2 ± 0.32 |
Cmpd 17 | 0.2 ± 0.02 | 0.4 ± 0.04 | |
Cmpd 18 | 2.7 ± 0.27 | 3.1 ± 0.31 | |
Cmpd 19 | 13 ± 1.3 | 12 ± 1.2 | |
fNBD1 | ADP | 19 ± 1.9 | 6 ± 0.6 |
AMPPNP | 11 ± 1.1 | 5 ± 0.5 | |
ATP | 2.4 ± 0.24 | 1.2 ± 0.12 | |
PhET‐ATP | 0.3 ± 0.03 | 0.3 ± 0.03 |
Standard error is estimated at 10% of values.
Affinities were determined by ITC for BASE1 and by SPR for cGAS and NBD1.
Slope and intercept values for ΔTm‐derived affinities were determined without data for the proteins they were to fit.
Without BASE1, the global slope and intercept values are −130.3 (±5.4) and −1.9 (±0.21).
Without cGAS, the global slope and intercept values are −131.2 (±5.3) and −1.9 (±0.20).
Without NBD1, the global slope and intercept values are −129.7 (±5.2) and −2.0(±0.20).