Assay Detail
Functional
CHEMBL3887514
Review assay metadata, readout intent, target linkage, and publication context from the same page.
GPR6 In Vitro Assay (A.1): This cell based assay measures the ability of compounds to inhibit the constitutive cAMP activity of GPR6 receptor expressed in CHO-K1 cells. CHO cells were stably expressed with GPR6 receptor, whose expression is controlled by a tetracycline inducable element. The cells were cultured in medium containing F12K, 10% FBS, 1% PennStrep, 200 ug/mL Hygromycin. GPR6 receptor expression was induced for 20 hrs with 1 ug/ml doxycycline (sigma D9891) in growth media. After addition of doxycycline cells were plated at a density of 250-500 cells per well in half-volume black clear bottom plates (Costar) and place in an incubator (37° C, 5% C(O)2) for 20 hours prior to cAMP assays.Culture media was removed from cells and they were washed with 50 uL of Ringer's Buffer (MgCl2 0.047 mg/mL, NaH2PO4 0.18 mg/mL, Na2HPO4 0.1 mg/mL, KCl 0.34 mg/mL, NaHC(O)3 1.26 mg/mL, D-glucose 1.8 mg/mL, NaCl 7 mg/mL; pH=7.4). Compounds suspended in DMSO were diluted in Ringer's Buffer.
69
Total Activities
69
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Substituted pyrido[3,4-b]pyrazines as GPR6 modulators
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 69 | 10.42 | 10.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3892898 | — | — | 1 | 10.98 |
| CHEMBL3909497 | — | — | 1 | 10.98 |
| CHEMBL3931736 | — | — | 1 | 10.94 |
| CHEMBL3905204 | — | — | 1 | 10.92 |
| CHEMBL3962092 | — | — | 1 | 10.87 |
| CHEMBL3955078 | — | — | 1 | 10.86 |
| CHEMBL3915516 | — | — | 1 | 10.86 |
| CHEMBL3982858 | — | — | 1 | 10.86 |
| CHEMBL3971468 | — | — | 1 | 10.86 |
| CHEMBL3957710 | — | — | 1 | 10.83 |
| CHEMBL3935897 | — | — | 1 | 10.82 |
| CHEMBL3976386 | — | — | 1 | 10.78 |
| CHEMBL3943282 | — | — | 1 | 10.77 |
| CHEMBL3967591 | — | — | 1 | 10.76 |
| CHEMBL3908467 | — | — | 1 | 10.75 |
| CHEMBL3963072 | — | — | 1 | 10.74 |
| CHEMBL4113017 | — | — | 1 | 10.73 |
| CHEMBL3986433 | — | — | 1 | 10.71 |
| CHEMBL3925720 | — | — | 1 | 10.71 |
| CHEMBL3943478 | — | — | 1 | 10.70 |
| CHEMBL3949818 | — | — | 1 | 10.68 |
| CHEMBL3905140 | — | — | 1 | 10.66 |
| CHEMBL3923125 | — | — | 1 | 10.64 |
| CHEMBL3985327 | — | — | 1 | 10.63 |
| CHEMBL3921525 | — | — | 1 | 10.63 |
| CHEMBL3967336 | — | — | 1 | 10.62 |
| CHEMBL3945233 | — | — | 1 | 10.60 |
| CHEMBL3948026 | — | — | 1 | 10.60 |
| CHEMBL4111582 | — | — | 1 | 10.58 |
| CHEMBL3911615 | — | — | 1 | 10.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3892898 | — | IC50 | = | 0.0104 | nM | 10.98 |
| CHEMBL3909497 | — | IC50 | = | 0.0104 | nM | 10.98 |
| CHEMBL3931736 | — | IC50 | = | 0.0115 | nM | 10.94 |
| CHEMBL3905204 | — | IC50 | = | 0.012 | nM | 10.92 |
| CHEMBL3962092 | — | IC50 | = | 0.0134 | nM | 10.87 |
| CHEMBL3955078 | — | IC50 | = | 0.0138 | nM | 10.86 |
| CHEMBL3915516 | — | IC50 | = | 0.0138 | nM | 10.86 |
| CHEMBL3982858 | — | IC50 | = | 0.0137 | nM | 10.86 |
| CHEMBL3971468 | — | IC50 | = | 0.0138 | nM | 10.86 |
| CHEMBL3957710 | — | IC50 | = | 0.0149 | nM | 10.83 |
| CHEMBL3935897 | — | IC50 | = | 0.0152 | nM | 10.82 |
| CHEMBL3976386 | — | IC50 | = | 0.0166 | nM | 10.78 |
| CHEMBL3943282 | — | IC50 | = | 0.0168 | nM | 10.77 |
| CHEMBL3967591 | — | IC50 | = | 0.0173 | nM | 10.76 |
| CHEMBL3908467 | — | IC50 | = | 0.0179 | nM | 10.75 |
| CHEMBL3963072 | — | IC50 | = | 0.018 | nM | 10.74 |
| CHEMBL4113017 | — | IC50 | = | 0.0185 | nM | 10.73 |
| CHEMBL3986433 | — | IC50 | = | 0.0195 | nM | 10.71 |
| CHEMBL3925720 | — | IC50 | = | 0.0197 | nM | 10.71 |
| CHEMBL3943478 | — | IC50 | = | 0.0199 | nM | 10.70 |
| CHEMBL3949818 | — | IC50 | = | 0.0209 | nM | 10.68 |
| CHEMBL3905140 | — | IC50 | = | 0.0221 | nM | 10.66 |
| CHEMBL3923125 | — | IC50 | = | 0.023 | nM | 10.64 |
| CHEMBL3985327 | — | IC50 | = | 0.0232 | nM | 10.63 |
| CHEMBL3921525 | — | IC50 | = | 0.0237 | nM | 10.63 |
| CHEMBL3967336 | — | IC50 | = | 0.0239 | nM | 10.62 |
| CHEMBL3948026 | — | IC50 | = | 0.0249 | nM | 10.60 |
| CHEMBL3945233 | — | IC50 | = | 0.0249 | nM | 10.60 |
| CHEMBL4111582 | — | IC50 | = | 0.0265 | nM | 10.58 |
| CHEMBL3911615 | — | IC50 | = | 0.0266 | nM | 10.58 |
| CHEMBL3924362 | — | IC50 | = | 0.0269 | nM | 10.57 |
| CHEMBL3945303 | — | IC50 | = | 0.0298 | nM | 10.53 |
| CHEMBL3975976 | — | IC50 | = | 0.0314 | nM | 10.50 |
| CHEMBL3927473 | — | IC50 | = | 0.0327 | nM | 10.49 |
| CHEMBL3951645 | — | IC50 | = | 0.0325 | nM | 10.49 |
| CHEMBL3935030 | — | IC50 | = | 0.035 | nM | 10.46 |
| CHEMBL3902681 | — | IC50 | = | 0.0387 | nM | 10.41 |
| CHEMBL3909048 | — | IC50 | = | 0.052 | nM | 10.28 |
| CHEMBL3939970 | — | IC50 | = | 0.0552 | nM | 10.26 |
| CHEMBL3987027 | — | IC50 | = | 0.0572 | nM | 10.24 |
| CHEMBL3912262 | — | IC50 | = | 0.0626 | nM | 10.20 |
| CHEMBL4113797 | — | IC50 | = | 0.064 | nM | 10.19 |
| CHEMBL3980074 | — | IC50 | = | 0.068 | nM | 10.17 |
| CHEMBL3961475 | — | IC50 | = | 0.076 | nM | 10.12 |
| CHEMBL3923277 | — | IC50 | = | 0.0788 | nM | 10.10 |
| CHEMBL3965124 | — | IC50 | = | 0.085 | nM | 10.07 |
| CHEMBL3980789 | — | IC50 | = | 0.087 | nM | 10.06 |
| CHEMBL3940326 | — | IC50 | = | 0.088 | nM | 10.06 |
| CHEMBL3902976 | — | IC50 | = | 0.0866 | nM | 10.06 |
| CHEMBL3927786 | — | IC50 | = | 0.091 | nM | 10.04 |