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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
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Journal of Biomedical Science

ISSN: 1423-0127