Assay Detail
Binding
CHEMBL4770540
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Displacement of [3H]-8-OH-DPAT from human 5-HT1A 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 | 6.54 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8618 | NAN-190 | — | 1 | 8.35 |
| CHEMBL4795056 | — | — | 1 | 8.06 |
| CHEMBL4780452 | — | — | 1 | 7.08 |
| CHEMBL4784167 | — | — | 1 | 6.98 |
| CHEMBL4799274 | — | — | 1 | 6.90 |
| CHEMBL4784089 | — | — | 1 | 6.87 |
| CHEMBL4781863 | — | — | 1 | 6.71 |
| CHEMBL4788259 | — | — | 1 | 6.58 |
| CHEMBL4791805 | — | — | 1 | 6.58 |
| CHEMBL4789865 | — | — | 1 | 6.54 |
| CHEMBL4794688 | — | — | 1 | 6.39 |
| CHEMBL4778946 | — | — | 1 | 6.35 |
| CHEMBL4783043 | — | — | 1 | 6.32 |
| CHEMBL4792307 | — | — | 1 | 6.32 |
| CHEMBL4785158 | — | — | 1 | 6.28 |
| CHEMBL4793310 | — | — | 1 | 6.09 |
| CHEMBL4779459 | — | — | 1 | 6.01 |
| CHEMBL4797980 | — | — | 1 | 5.90 |
| CHEMBL4781056 | — | — | 1 | 5.86 |
| CHEMBL4777209 | — | — | 1 | 5.62 |
| CHEMBL4782879 | — | — | 1 | 5.56 |
| CHEMBL4798874 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8618 | NAN-190 | Ki | = | 4.49 | nM | 8.35 |
| CHEMBL4795056 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL4780452 | — | Ki | = | 82.9 | nM | 7.08 |
| CHEMBL4784167 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL4799274 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL4784089 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL4781863 | — | Ki | = | 197.0 | nM | 6.71 |
| CHEMBL4788259 | — | Ki | = | 264.0 | nM | 6.58 |
| CHEMBL4791805 | — | Ki | = | 264.0 | nM | 6.58 |
| CHEMBL4789865 | — | Ki | = | 287.0 | nM | 6.54 |
| CHEMBL4794688 | — | Ki | = | 403.0 | nM | 6.39 |
| CHEMBL4778946 | — | Ki | = | 449.0 | nM | 6.35 |
| CHEMBL4783043 | — | Ki | = | 477.0 | nM | 6.32 |
| CHEMBL4792307 | — | Ki | = | 475.0 | nM | 6.32 |
| CHEMBL4785158 | — | Ki | = | 521.0 | nM | 6.28 |
| CHEMBL4793310 | — | Ki | = | 811.0 | nM | 6.09 |
| CHEMBL4779459 | — | Ki | = | 967.0 | nM | 6.01 |
| CHEMBL4797980 | — | Ki | = | 1270.0 | nM | 5.90 |
| CHEMBL4781056 | — | Ki | = | 1370.0 | nM | 5.86 |
| CHEMBL4777209 | — | Ki | = | 2394.0 | nM | 5.62 |
| CHEMBL4782879 | — | Ki | = | 2750.0 | nM | 5.56 |
| CHEMBL4798874 | — | Ki | > | 8000.0 | nM | - |