Table 1. Control Compound Affinities/Kinetic Parameters Binding to Adenosine Receptors A1, A2A, A2B, and A3a.
receptor | compound | ka (M–1 s–1) | kd (s–1) | KD | Ki (literature) | figure |
---|---|---|---|---|---|---|
A2A | adenosine | 9.53(±0.05) × 105 | 0.016(±0.008) | 17.3(±0.1) nM | 150 nM | 1A |
A2A | ZM 241385 | 2.42(±0.08) × 106 | 6.92(±0.03) × 10–4 | 286(±1) pM | 395 pM | |
A2A | theophylline | N/A | N/A | 3.63(±0.05) μM | N/A | 1B |
A2A | allopurinol | N/A | N/A | 77(±3) μM | N/A | |
A2A | caffeine | N/A | N/A | 5.51(±0.08) μM | N/A | |
A1 | SLV320 | 6.27(±0.01) × 105 | 0.0034(±0.0004) | 5.46(±0.01) nM | 1 nM | 2C–F |
A2A | CV1808 | 2.93(±0.03) × 106 | 0.027(±0.002) | 9.1(±0.1) nM | 76 nM | |
A2B | LUF5834 | 1.10(±0.06) × 105 | 0.0086(±0.0004) | 78.2(±0.03) nM | 12 nM | |
A3 | adenosine | 2.49(±0.03) × 104 | 0.077(±0.007) | 3.07(±0.01) μM | 290 nM |
ka, on-rate; kd, off-rate; KD, affinity; Ki, inhibition constant from literature.