Assay Detail
Functional
CHEMBL4828349
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
44
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of G Protein-Biased Antagonists against 5-HT<sub>7</sub>R.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 5.73 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL282199 | — | — | 2 | 9.30 |
| CHEMBL4877603 | — | — | 2 | 6.16 |
| CHEMBL4858338 | — | — | 2 | 6.05 |
| CHEMBL4848305 | — | — | 2 | 6.04 |
| CHEMBL4876193 | — | — | 2 | 5.98 |
| CHEMBL4859827 | — | — | 2 | 5.93 |
| CHEMBL4863036 | — | — | 2 | 5.80 |
| CHEMBL4852622 | — | — | 2 | 5.79 |
| CHEMBL4863868 | — | — | 2 | 5.76 |
| CHEMBL4856702 | — | — | 2 | 5.63 |
| CHEMBL4854605 | — | — | 2 | 5.63 |
| CHEMBL4866412 | — | — | 2 | 5.61 |
| CHEMBL4867560 | — | — | 2 | 5.41 |
| CHEMBL4877051 | — | — | 2 | 5.40 |
| CHEMBL4876036 | — | — | 2 | 5.39 |
| CHEMBL4862745 | — | — | 2 | 5.34 |
| CHEMBL4874854 | — | — | 2 | 5.26 |
| CHEMBL4868035 | — | — | 2 | 5.20 |
| CHEMBL4871980 | — | — | 2 | 5.20 |
| CHEMBL4869695 | — | — | 2 | 5.14 |
| CHEMBL4870675 | — | — | 2 | 5.07 |
| CHEMBL4860503 | — | — | 2 | 5.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL282199 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL282199 | — | IC50 | = | 0.93 | nM | 9.03 |
| CHEMBL4877603 | — | IC50 | = | 691.83 | nM | 6.16 |
| CHEMBL4877603 | — | IC50 | = | 686.0 | nM | 6.16 |
| CHEMBL4858338 | — | IC50 | = | 891.25 | nM | 6.05 |
| CHEMBL4858338 | — | IC50 | = | 888.0 | nM | 6.05 |
| CHEMBL4848305 | — | IC50 | = | 912.01 | nM | 6.04 |
| CHEMBL4848305 | — | IC50 | = | 909.0 | nM | 6.04 |
| CHEMBL4876193 | — | IC50 | = | 1047.13 | nM | 5.98 |
| CHEMBL4876193 | — | IC50 | = | 1053.0 | nM | 5.98 |
| CHEMBL4859827 | — | IC50 | = | 1174.9 | nM | 5.93 |
| CHEMBL4859827 | — | IC50 | = | 1177.0 | nM | 5.93 |
| CHEMBL4863036 | — | IC50 | = | 1569.0 | nM | 5.80 |
| CHEMBL4863036 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4852622 | — | IC50 | = | 1621.81 | nM | 5.79 |
| CHEMBL4852622 | — | IC50 | = | 1624.0 | nM | 5.79 |
| CHEMBL4863868 | — | IC50 | = | 1741.0 | nM | 5.76 |
| CHEMBL4863868 | — | IC50 | = | 1737.8 | nM | 5.76 |
| CHEMBL4856702 | — | IC50 | = | 2344.23 | nM | 5.63 |
| CHEMBL4856702 | — | IC50 | = | 2319.0 | nM | 5.63 |
| CHEMBL4854605 | — | IC50 | = | 2344.23 | nM | 5.63 |
| CHEMBL4854605 | — | IC50 | = | 2329.0 | nM | 5.63 |
| CHEMBL4866412 | — | IC50 | = | 2445.0 | nM | 5.61 |
| CHEMBL4866412 | — | IC50 | = | 2454.71 | nM | 5.61 |
| CHEMBL4867560 | — | IC50 | = | 3935.0 | nM | 5.41 |
| CHEMBL4877051 | — | IC50 | = | 3977.0 | nM | 5.40 |
| CHEMBL4877051 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4867560 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4876036 | — | IC50 | = | 4073.8 | nM | 5.39 |
| CHEMBL4876036 | — | IC50 | = | 4061.0 | nM | 5.39 |
| CHEMBL4862745 | — | IC50 | = | 4518.0 | nM | 5.34 |
| CHEMBL4862745 | — | IC50 | = | 4570.88 | nM | 5.34 |
| CHEMBL4874854 | — | IC50 | = | 5495.41 | nM | 5.26 |
| CHEMBL4874854 | — | IC50 | = | 5473.0 | nM | 5.26 |
| CHEMBL4868035 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL4868035 | — | IC50 | = | 6264.0 | nM | 5.20 |
| CHEMBL4871980 | — | IC50 | = | 6356.0 | nM | 5.20 |
| CHEMBL4871980 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL4869695 | — | IC50 | = | 7244.36 | nM | 5.14 |
| CHEMBL4869695 | — | IC50 | = | 7246.0 | nM | 5.14 |
| CHEMBL4870675 | — | IC50 | = | 8596.0 | nM | 5.07 |
| CHEMBL4870675 | — | IC50 | = | 8709.64 | nM | 5.06 |
| CHEMBL4860503 | — | IC50 | = | 8912.51 | nM | 5.05 |
| CHEMBL4860503 | — | IC50 | = | 8893.0 | nM | 5.05 |