Table 1 Potency and maximal response of the 36 identified GPR139 agonists in calcium mobilization assay in CHO-GPR139 cells.

From: Identification of a novel scaffold for a small molecule GPR139 receptor agonist

ID

Enamine ID

EC50 μM

pEC50 ± S.E.M.

Emax ± S.E.M.

n

Matches*

AC224

Z30029744

0.09

7.03 ± 0.02

106 ± 1

3

6

AC177

Z1618891443

0.09

7.02 ± 0.11

103 ± 1

4

5

AC183

Z352587398

0.18

6.74 ± 0.19

110 ± 10

3

5

AC197

Z16669083

0.19

6.71 ± 0.14

103 ± 1

3

5

AC194

Z18052622

0.21

6.68 ± 0.02

106 ± 4

3

5

AC4

Z446416294

0.22

6.66 ± 0.06

116 ± 3

5

3

AC225

Z13589494

0.28

6.56 ± 0.05

120 ± 5

3

5

AC178

Z1618764723

0.28

6.55 ± 0.07

97 ± 5

3

5

AC209

Z18053107

0.29

6.54 ± 0.17

107 ± 3

4

5

AC82

Z352587564

0.29

6.54 ± 0.08

102 ± 6

3

4

AC202

Z16669106

0.34

6.47 ± 0.09

102 ± 2

3

4

AC233

Z14078826

0.34

6.47 ± 0.19

80 ± 6

3

5

AC191

Z18052722

0.35

6.46 ± 0.16

99 ± 2

3

5

AC243

Z14078663

0.35

6.45 ± 0.11

86 ± 5

3

4

AC206

Z16668711

0.38

6.42 ± 0.06

94 ± 3

3

5

AC234

Z14075523

0.38

6.42 ± 0.07

99 ± 3

3

5

AC7

Z16668610

0.39

6.41 ± 0.12

112 ± 5

4

4

AC186

Z14077796

0.41

6.39 ± 0.12

89 ± 5

3

4

AC241

Z165543100

0.42

6.38 ± 0.06

88 ± 3

3

5

AC229

Z14075450

0.43

6.36 ± 0.16

95 ± 2

4

4

AC205

Z18052636

0.44

6.36 ± 0.14

100 ± 3

3

5

AC200

Z18052594

0.46

6.34 ± 0.11

111 ± 5

3

5

AC220

Z16668660

0.49

6.31 ± 0.01

103 ± 3

3

5

AC230

Z14075785

0.49

6.31 ± 0.27

89 ± 1

3

4

AC137

Z16669312

0.54

6.27 ± 0.08

92 ± 3

3

5

AC77

Z336570670

0.60

6.22 ± 0.17

102 ± 4

3

5

AC210

Z18052723

0.63

6.20 ± 0.24

115 ± 8

4

5

AC123

Z54783382

0.74

6.13 ± 0.14

104 ± 1

3

5

AC187

Z14077801

0.74

6.13 ± 0.22

102 ± 5

4

4

AC192

Z16669294

0.75

6.12 ± 0.13

95 ± 1

3

4

AC14

Z336589160

0.78

6.11 ± 0.12

93 ± 3

3

5

AC138

Z16668376

0.79

6.10 ± 0.14

100 ± 5

4

5

AC134

Z16669311

0.80

6.09 ± 0.15

103 ± 5

4

5

AC208

Z18053097

0.88

6.05 ± 0.60

134 ± 26

3

5

AC76

Z336570672

0.94

6.03 ± 0.10

97 ± 4

3

5

AC136

Z16669296

0.99

6.01 ± 0.03

67 ± 6

3

5

  1. The data is based on at least three independent full concentration-response curves in duplicate, normalized to buffer (0%) and 8 μM 1a (100%). *Number of matching pharmacophore elements from Supplementary Fig. S3.