Assay Detail
Binding
CHEMBL2404383
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Binding affinity to human recombinant 5HT3 receptor
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 4.49 | 5.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2402896 | — | — | 1 | 5.90 |
| CHEMBL1729 | CISAPRIDE | 4.0 | 1 | 5.70 |
| CHEMBL76370 | TEGASEROD | 4.0 | 1 | 5.60 |
| CHEMBL2402894 | — | — | 1 | 5.10 |
| CHEMBL2402895 | — | — | 1 | 4.80 |
| CHEMBL2402888 | — | — | 1 | 4.70 |
| CHEMBL2402893 | — | — | 1 | 4.40 |
| CHEMBL2402899 | — | — | 1 | 4.40 |
| CHEMBL2402901 | — | — | 1 | 4.30 |
| CHEMBL2402892 | — | — | 1 | 4.30 |
| CHEMBL2402887 | — | — | 1 | 4.30 |
| CHEMBL2402902 | — | — | 1 | 4.20 |
| CHEMBL2402889 | — | — | 1 | 4.20 |
| CHEMBL2402898 | — | — | 1 | 4.10 |
| CHEMBL2402900 | — | — | 1 | 4.10 |
| CHEMBL2402891 | — | — | 1 | 4.10 |
| CHEMBL2402890 | — | — | 1 | 4.10 |
| CHEMBL2402897 | — | — | 1 | 4.00 |
| CHEMBL2402903 | — | — | 1 | 4.00 |
| CHEMBL2402904 | FELCISETRAG | 2.0 | 1 | 4.00 |
| CHEMBL2401750 | — | — | 1 | 4.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2402896 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL1729 | CISAPRIDE | Ki | = | 1995.26 | nM | 5.70 |
| CHEMBL76370 | TEGASEROD | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL2402894 | — | Ki | = | 7943.28 | nM | 5.10 |
| CHEMBL2402895 | — | Ki | = | 15848.93 | nM | 4.80 |
| CHEMBL2402888 | — | Ki | = | 19952.62 | nM | 4.70 |
| CHEMBL2402893 | — | Ki | = | 39810.72 | nM | 4.40 |
| CHEMBL2402899 | — | Ki | = | 39810.72 | nM | 4.40 |
| CHEMBL2402901 | — | Ki | = | 50118.72 | nM | 4.30 |
| CHEMBL2402892 | — | Ki | = | 50118.72 | nM | 4.30 |
| CHEMBL2402887 | — | Ki | = | 50118.72 | nM | 4.30 |
| CHEMBL2402902 | — | Ki | = | 63095.73 | nM | 4.20 |
| CHEMBL2402889 | — | Ki | = | 63095.73 | nM | 4.20 |
| CHEMBL2402898 | — | Ki | = | 79432.82 | nM | 4.10 |
| CHEMBL2402900 | — | Ki | = | 79432.82 | nM | 4.10 |
| CHEMBL2402891 | — | Ki | = | 79432.82 | nM | 4.10 |
| CHEMBL2402890 | — | Ki | = | 79432.82 | nM | 4.10 |
| CHEMBL2402897 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL2402903 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL2402904 | FELCISETRAG | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL2401750 | — | Ki | = | 100000.0 | nM | 4.00 |