Assay Detail
Binding
CHEMBL3887753
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | COS-7 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Benzamide derivatives
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 9.75 | 10.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3967117 | — | — | 1 | 10.41 |
| CHEMBL3950712 | DA-6886 | 1.0 | 1 | 10.17 |
| CHEMBL3934371 | — | — | 1 | 10.12 |
| CHEMBL3926377 | — | — | 1 | 9.99 |
| CHEMBL3890747 | — | — | 1 | 9.87 |
| CHEMBL3986866 | — | — | 1 | 9.79 |
| CHEMBL3957180 | — | — | 1 | 9.74 |
| CHEMBL3946162 | — | — | 1 | 9.65 |
| CHEMBL3928124 | — | — | 1 | 9.64 |
| CHEMBL3982522 | — | — | 1 | 9.57 |
| CHEMBL1729 | CISAPRIDE | 4.0 | 1 | 9.44 |
| CHEMBL3920018 | — | — | 1 | 9.43 |
| CHEMBL3915236 | — | — | 1 | 9.38 |
| CHEMBL3910849 | — | — | 1 | 9.34 |
| CHEMBL3922150 | — | — | 1 | - |
| CHEMBL3901228 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3967117 | — | IC50 | = | 0.039 | nM | 10.41 |
| CHEMBL3950712 | DA-6886 | IC50 | = | 0.067 | nM | 10.17 |
| CHEMBL3934371 | — | IC50 | = | 0.076 | nM | 10.12 |
| CHEMBL3926377 | — | IC50 | = | 0.103 | nM | 9.99 |
| CHEMBL3890747 | — | IC50 | = | 0.134 | nM | 9.87 |
| CHEMBL3986866 | — | IC50 | = | 0.164 | nM | 9.79 |
| CHEMBL3957180 | — | IC50 | = | 0.182 | nM | 9.74 |
| CHEMBL3946162 | — | IC50 | = | 0.226 | nM | 9.65 |
| CHEMBL3928124 | — | IC50 | = | 0.229 | nM | 9.64 |
| CHEMBL3982522 | — | IC50 | = | 0.267 | nM | 9.57 |
| CHEMBL1729 | CISAPRIDE | IC50 | = | 0.362 | nM | 9.44 |
| CHEMBL3920018 | — | IC50 | = | 0.375 | nM | 9.43 |
| CHEMBL3915236 | — | IC50 | = | 0.421 | nM | 9.38 |
| CHEMBL3910849 | — | IC50 | = | 0.454 | nM | 9.34 |
| CHEMBL3922150 | — | IC50 | = | 0.005 | nM | - |
| CHEMBL3901228 | — | IC50 | = | 0.002 | nM | - |