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. 2022 Jun 6;13(7):1172–1181. doi: 10.1021/acsmedchemlett.2c00099

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
a

ka, on-rate; kd, off-rate; KD, affinity; Ki, inhibition constant from literature.