Assay Detail
Binding
CHEMBL4770539
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Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 60 mins by radioligand binding assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Privileged scaffold-based design to identify a novel drug-like 5-HT receptor-preferring agonist to target Fragile X syndrome.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 7.57 | 9.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18840 | — | — | 1 | 9.46 |
| CHEMBL4781863 | — | — | 1 | 7.88 |
| CHEMBL4799274 | — | — | 1 | 7.83 |
| CHEMBL4789865 | — | — | 1 | 7.82 |
| CHEMBL4794688 | — | — | 1 | 7.80 |
| CHEMBL4780452 | — | — | 1 | 7.79 |
| CHEMBL4783043 | — | — | 1 | 7.75 |
| CHEMBL4795056 | — | — | 1 | 7.70 |
| CHEMBL4785158 | — | — | 1 | 7.63 |
| CHEMBL4791805 | — | — | 1 | 7.60 |
| CHEMBL4797980 | — | — | 1 | 7.59 |
| CHEMBL4792307 | — | — | 1 | 7.58 |
| CHEMBL4778946 | — | — | 1 | 7.45 |
| CHEMBL4782879 | — | — | 1 | 7.44 |
| CHEMBL4784089 | — | — | 1 | 7.37 |
| CHEMBL4788259 | — | — | 1 | 7.35 |
| CHEMBL4793310 | — | — | 1 | 7.34 |
| CHEMBL4779459 | — | — | 1 | 7.33 |
| CHEMBL4777209 | — | — | 1 | 7.21 |
| CHEMBL4784167 | — | — | 1 | 7.20 |
| CHEMBL4781056 | — | — | 1 | 7.13 |
| CHEMBL4798874 | — | — | 1 | 6.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18840 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL4781863 | — | Ki | = | 13.2 | nM | 7.88 |
| CHEMBL4799274 | — | Ki | = | 14.7 | nM | 7.83 |
| CHEMBL4789865 | — | Ki | = | 15.2 | nM | 7.82 |
| CHEMBL4794688 | — | Ki | = | 15.7 | nM | 7.80 |
| CHEMBL4780452 | — | Ki | = | 16.1 | nM | 7.79 |
| CHEMBL4783043 | — | Ki | = | 17.7 | nM | 7.75 |
| CHEMBL4795056 | — | Ki | = | 19.9 | nM | 7.70 |
| CHEMBL4785158 | — | Ki | = | 23.6 | nM | 7.63 |
| CHEMBL4791805 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL4797980 | — | Ki | = | 25.7 | nM | 7.59 |
| CHEMBL4792307 | — | Ki | = | 26.5 | nM | 7.58 |
| CHEMBL4778946 | — | Ki | = | 35.8 | nM | 7.45 |
| CHEMBL4782879 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL4784089 | — | Ki | = | 42.9 | nM | 7.37 |
| CHEMBL4788259 | — | Ki | = | 44.3 | nM | 7.35 |
| CHEMBL4793310 | — | Ki | = | 45.8 | nM | 7.34 |
| CHEMBL4779459 | — | Ki | = | 47.3 | nM | 7.33 |
| CHEMBL4777209 | — | Ki | = | 61.4 | nM | 7.21 |
| CHEMBL4784167 | — | Ki | = | 62.8 | nM | 7.20 |
| CHEMBL4781056 | — | Ki | = | 74.5 | nM | 7.13 |
| CHEMBL4798874 | — | Ki | = | 410.0 | nM | 6.39 |