Assay Detail
ADMET
CHEMBL4736129
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Displacement of [3H]-8-OH-DPAT from human 5HT2A expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Imidazopyridine-Based 5-HT Receptor Neutral Antagonists: Impact of N-Benzyl and N-Phenylsulfonyl Fragments on Different Receptor Conformational States.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.65 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1083390 | INTEPIRDINE | 3.0 | 1 | 7.58 |
| CHEMBL4742804 | — | — | 1 | 6.62 |
| CHEMBL4760105 | — | — | 1 | 6.58 |
| CHEMBL4777550 | — | — | 1 | 6.45 |
| CHEMBL4799851 | — | — | 1 | 6.39 |
| CHEMBL4756814 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1083390 | INTEPIRDINE | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL4742804 | — | Ki | = | 239.0 | nM | 6.62 |
| CHEMBL4760105 | — | Ki | = | 264.0 | nM | 6.58 |
| CHEMBL4777550 | — | Ki | = | 355.0 | nM | 6.45 |
| CHEMBL4799851 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL4756814 | — | Ki | = | 562.0 | nM | 6.25 |