| SAR Analysis for GPR7 |
 | Potency (uM) mean ± S.E.M. | Target to Antitarget Fold Selectivity | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Entry | CID | SID | Center Internal Number | P/S* | Ar† | X | Y | Target GPR7 | Antitarget MCH1 | |||
| n** | IC50 | n** | IC50 | |||||||||
| 1 | 46172919 | 96021160 | SR-02000000372-1 | S |
 | OMe | Cl | 3 | 0.27 | 3 | 3.9 | 14.4 |
| 2 | 46172926 | 96021133 | SR-02000000346-1 | S |
 | OEt | Cl | 3 | 0.989 | 3 | 11 | 11.2 |
| 3 | 46172920 | 96021141 | SR-02000000354-1 | S |
| Et | Cl | 3 | 0.68 | 3 | 5.0 | 7.3 |
| 4 | 46172935 | 96021155 | SR-02000000367-1 | S |
 | OMe | Cl | 3 | 0.57 | 3 | 3.9 | 6.8 |
| 5 | 46835808 | 99218838 | SR-02000000448-1 | S |
 | OMe | Cl | 3 | 0.3 | 3 | 2.0 | 6.7 |
| 6 | 46846333 | 99234261 | SR-02000000477-1 | S |
| OMe |
 | 3 | 19.85 | 3 | 25.2 | 1.3 |
| 7 | 1479652 | 17409616 | SR-01000679408-1 | S |
| OMe | Cl | 3 | 2.94 | 3 | 23.62 | 8 |
| 93375574 | SR-01000679408-2 | S | 3 | 2.2 | 3 | 17 | 7.7 | |||||
| 8 | 46846334 | 99234259 | SR-02000000475-1 | S |
| OMe |
 | 3 | 39.35 | 3 | 20.0 | 0.5 |
| 9 | 46846336 | 99234260 | SR-02000000476-1 | S |
| OMe |
 | 3 | 14.28 | 3 | 13.5 | 0.9 |
| 10 | 46172934 | 96021139 | SR-02000000352-1 | S |
| OCF3 | Cl | 3 | 8.8 | 3 | 2.9 | 0.3 |
| 11 | 46835794 | 99218818 | SR-02000000428-1 | S |
 | OMe | Me | 3 | 7.5 | 3 | 9.8 | 1.3 |
| 12 | 46172939 | 96021145 | SR-02000000358-1 | S |
| OMe |
 | 3 | 6.20 | 3 | 5.4 | 0.87 |
| 13 | 46835810 | 99218831 | SR-02000000441-1 | S |
| OMe |
 | 3 | 6.2 | 3 | 4.8 | 0.8 |
| 14 | 46835802 | 99218821 | SR-02000000431-1 | S |
| OMe | CN | 3 | 4.2 | 3 | 7.5 | 1.8 |
| 15 | 46835813 | 99218824 | SR-02000000434-1 | S |
| OMe | COOMe | 3 | 2.7 | 3 | 6.9 | 2.6 |
| 16 | 46172929 | 96021135 | SR-02000000348-1 | S |
| CH2OH | Cl | 3 | 2.3 | 3 | 20.5 | 8.9 |
| 17 | 46172942 | 96021138 | SR-02000000351-1 | S |
| CF3 | Cl | 3 | 2.2 | 3 | 5.5 | 2.5 |
| 18 | 1484423 | 99239442 | SR-02000000358-1 | S |
| OMe | Br | 3 | 0.78 | 3 | 14.3 | 18.3 |
| 19 | 46172921 | 96021157 | SR-02000000369-1 | S |
 | OMe | Cl | 3 | 0.68 | 3 | 2.70 | 4.0 |
| 20 | 46172941 | 96021158 | SR-02000000370-1 | S |
 | OMe | Cl | 3 | 0.65 | 3 | 2.20 | 3.4 |
| 21 | 46835805 | 99218837 | SR-02000000447-1 | S |
 | OMe | Cl | 3 | 0.57 | 3 | 5.4 | 9.5 |
| 22 | 46835792 | 99218843 | SR-02000000453-1 | S |
 | OMe | Cl | 3 | 0.36 | 3 | 8.4 | 23.3 |
| 23 | 46172924 | 96021159 | SR-02000000371-1 | S |
 | OMe | Cl | 3 | 0.28 | 3 | 1.7 | 6.1 |
| 24 | 46846335 | 99234258 | SR-02000000474-1 | S |
| OMe | Cl | 3 | 0.27 | 3 | 3.1 | 11.5 |
P = Purchased; S = Synthesized
n = Number of Replicates
Ar = Aromatic group
From: Optimization and Characterization of an Antagonist for G-Protein Coupled Receptor 7 (GPR7)
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