Assay Detail
Binding
CHEMBL961024
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Displacement of [3H]MDL from rat 5HT2A receptor expressed in GF62 cells by liquid scintillation analyser
22
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | GF62 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 8.23 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL489621 | — | — | 1 | 9.60 |
| CHEMBL492069 | — | — | 1 | 9.51 |
| CHEMBL74355 | VOLINANSERIN | 3.0 | 2 | 9.42 |
| CHEMBL515472 | — | — | 1 | 9.14 |
| CHEMBL62919 | ALTANSERIN | 2.0 | 1 | 9.14 |
| CHEMBL490847 | — | — | 1 | 8.91 |
| CHEMBL489624 | — | — | 1 | 8.87 |
| CHEMBL490846 | — | — | 1 | 8.79 |
| CHEMBL476839 | — | — | 1 | 8.74 |
| CHEMBL489634 | — | — | 1 | 8.69 |
| CHEMBL516088 | — | — | 1 | 8.49 |
| CHEMBL490632 | — | — | 1 | 8.34 |
| CHEMBL402143 | — | — | 1 | 8.04 |
| CHEMBL476838 | — | — | 1 | 7.58 |
| CHEMBL492068 | — | — | 1 | 7.26 |
| CHEMBL490633 | — | — | 1 | 7.23 |
| CHEMBL522982 | — | — | 1 | 7.05 |
| CHEMBL490634 | — | — | 1 | 6.93 |
| CHEMBL489408 | — | — | 1 | 6.82 |
| CHEMBL490845 | — | — | 1 | 5.70 |
| CHEMBL489618 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL489621 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL492069 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL74355 | VOLINANSERIN | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL62919 | ALTANSERIN | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL515472 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL490847 | — | Ki | = | 1.24 | nM | 8.91 |
| CHEMBL489624 | — | Ki | = | 1.34 | nM | 8.87 |
| CHEMBL490846 | — | Ki | = | 1.63 | nM | 8.79 |
| CHEMBL476839 | — | Ki | = | 1.83 | nM | 8.74 |
| CHEMBL489634 | — | Ki | = | 2.06 | nM | 8.69 |
| CHEMBL74355 | VOLINANSERIN | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL516088 | — | Ki | = | 3.23 | nM | 8.49 |
| CHEMBL490632 | — | Ki | = | 4.56 | nM | 8.34 |
| CHEMBL402143 | — | Ki | = | 9.02 | nM | 8.04 |
| CHEMBL476838 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL492068 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL490633 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL522982 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL490634 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL489408 | — | Ki | = | 153.0 | nM | 6.82 |
| CHEMBL490845 | — | Ki | = | 1987.0 | nM | 5.70 |
| CHEMBL489618 | — | Ki | > | 1000.0 | nM | - |