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Table 1 EC50 determination of (1R,2R)-2-PCCA analogues

From: Development and validation of a high-throughput calcium mobilization assay for the orphan receptor GPR88

Compda X R1 R2 pEC50 (EC50, nM)b
(1R,2R)-2-PCCA (1a) N Propyl   6.33 ± 0.06 (468)
1b C Propyl   5.90 ± 0.08 (1260)
1c C Cyclohexyl   6.10 ± 0.04 (794)
1d C CONH2   NAc
2a    (S)-NH2 5.88 ± 0.03 (1320)
2b    (R)-NH2 5.58 ± 0.04 (2630)
2c    H NAc
3     NAc
  1. aAll compounds were tested as the HCl salt
  2. bpEC50 values are means ± standard error of at least three independent experiments performed in duplicate
  3. cEC50 > 10 μM, tested in two independent experiments performed in duplicate