Assay Detail
Binding
CHEMBL1176402
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]methylspiperone from human cloned 5HT2A receptor expressed in HEK293 cells after 90 mins by liquid scintillation counting
34
Total Activities
34
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
Synthesis and structure-affinity relationships of novel small molecule natural product derivatives capable of discriminating between serotonin 5-HT1A, 5-HT2A, 5-HT2C receptor subtypes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 6.42 | 7.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL43916 | — | — | 1 | 7.20 |
| CHEMBL296090 | — | — | 1 | 7.20 |
| CHEMBL40726 | — | — | 1 | 7.00 |
| CHEMBL43929 | — | — | 1 | 7.00 |
| CHEMBL42463 | — | — | 1 | 6.90 |
| CHEMBL96883 | — | — | 1 | 6.80 |
| CHEMBL276673 | — | — | 1 | 6.80 |
| CHEMBL42024 | — | — | 1 | 6.80 |
| CHEMBL1172812 | — | — | 1 | 6.76 |
| CHEMBL328844 | — | — | 1 | 6.70 |
| CHEMBL1173820 | — | — | 1 | 6.63 |
| CHEMBL297043 | — | — | 1 | 6.60 |
| CHEMBL92656 | — | — | 1 | 6.60 |
| CHEMBL301784 | — | — | 1 | 6.60 |
| CHEMBL299726 | — | — | 1 | 6.50 |
| CHEMBL44095 | — | — | 1 | 6.40 |
| CHEMBL299530 | — | — | 1 | 6.30 |
| CHEMBL404232 | APLYSINOPSIN | — | 1 | 6.22 |
| CHEMBL289063 | — | — | 1 | 6.20 |
| CHEMBL1173408 | — | — | 1 | 6.18 |
| CHEMBL38911 | — | — | 1 | 6.10 |
| CHEMBL93850 | — | — | 1 | 6.10 |
| CHEMBL433060 | — | — | 1 | 5.80 |
| CHEMBL42276 | — | — | 1 | 5.60 |
| CHEMBL290395 | — | — | 1 | 5.60 |
| CHEMBL54769 | — | — | 1 | 5.40 |
| CHEMBL41347 | — | — | 1 | 5.30 |
| CHEMBL59097 | — | — | 1 | - |
| CHEMBL55958 | — | — | 1 | - |
| CHEMBL56232 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL43916 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL296090 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL40726 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL43929 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL42463 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL96883 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL276673 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL42024 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL1172812 | — | Ki | = | 173.0 | nM | 6.76 |
| CHEMBL328844 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL1173820 | — | Ki | = | 235.0 | nM | 6.63 |
| CHEMBL297043 | — | Ki | = | 251.0 | nM | 6.60 |
| CHEMBL92656 | — | Ki | = | 251.0 | nM | 6.60 |
| CHEMBL301784 | — | Ki | = | 251.0 | nM | 6.60 |
| CHEMBL299726 | — | Ki | = | 316.0 | nM | 6.50 |
| CHEMBL44095 | — | Ki | = | 398.0 | nM | 6.40 |
| CHEMBL299530 | — | Ki | = | 501.0 | nM | 6.30 |
| CHEMBL404232 | APLYSINOPSIN | Ki | = | 598.0 | nM | 6.22 |
| CHEMBL289063 | — | Ki | = | 631.0 | nM | 6.20 |
| CHEMBL1173408 | — | Ki | = | 655.0 | nM | 6.18 |
| CHEMBL38911 | — | Ki | = | 794.0 | nM | 6.10 |
| CHEMBL93850 | — | Ki | = | 794.0 | nM | 6.10 |
| CHEMBL433060 | — | Ki | = | 1585.0 | nM | 5.80 |
| CHEMBL42276 | — | Ki | = | 2512.0 | nM | 5.60 |
| CHEMBL290395 | — | Ki | = | 2512.0 | nM | 5.60 |
| CHEMBL54769 | — | Ki | = | 3981.0 | nM | 5.40 |
| CHEMBL41347 | — | Ki | = | 5012.0 | nM | 5.30 |
| CHEMBL59097 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL55958 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL56232 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL42327 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1173334 | — | Ki | - | — | - | |
| CHEMBL463249 | — | Ki | - | — | - | |
| CHEMBL1173333 | — | Ki | - | — | - |