Assay Detail
Functional
CHEMBL1786004
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of novel gamma-carboline analogues of Dimebon as potent 5-HT6 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.46 | 6.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1783965 | — | — | 1 | 6.43 |
| CHEMBL1783960 | — | — | 1 | 6.36 |
| CHEMBL1783954 | — | — | 1 | 6.07 |
| CHEMBL589390 | LATREPIRDINE | 3.0 | 1 | 6.05 |
| CHEMBL1783957 | — | — | 1 | 5.98 |
| CHEMBL1783958 | — | — | 1 | 5.80 |
| CHEMBL1783970 | — | — | 1 | 5.69 |
| CHEMBL1783956 | — | — | 1 | 5.53 |
| CHEMBL1783967 | — | — | 1 | 5.49 |
| CHEMBL1783966 | — | — | 1 | 5.36 |
| CHEMBL1783962 | — | — | 1 | 5.24 |
| CHEMBL1783959 | — | — | 1 | 5.22 |
| CHEMBL1783968 | — | — | 1 | 5.19 |
| CHEMBL1783971 | — | — | 1 | 5.13 |
| CHEMBL1783955 | — | — | 1 | 5.08 |
| CHEMBL1783964 | — | — | 1 | 5.05 |
| CHEMBL1783963 | — | — | 1 | 4.97 |
| CHEMBL1783953 | — | — | 1 | 4.80 |
| CHEMBL1783972 | — | — | 1 | 4.37 |
| CHEMBL1783961 | — | — | 1 | - |
| CHEMBL1783969 | — | — | 1 | - |
| CHEMBL1783973 | — | — | 1 | - |
| CHEMBL1783974 | — | — | 1 | - |
| CHEMBL1783975 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1783965 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL1783960 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL1783954 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL589390 | LATREPIRDINE | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL1783957 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL1783958 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL1783970 | — | IC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL1783956 | — | IC50 | = | 2980.0 | nM | 5.53 |
| CHEMBL1783967 | — | IC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL1783966 | — | IC50 | = | 4340.0 | nM | 5.36 |
| CHEMBL1783962 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL1783959 | — | IC50 | = | 5990.0 | nM | 5.22 |
| CHEMBL1783968 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL1783971 | — | IC50 | = | 7470.0 | nM | 5.13 |
| CHEMBL1783955 | — | IC50 | = | 8360.0 | nM | 5.08 |
| CHEMBL1783964 | — | IC50 | = | 8910.0 | nM | 5.05 |
| CHEMBL1783963 | — | IC50 | = | 10690.0 | nM | 4.97 |
| CHEMBL1783953 | — | IC50 | = | 15750.0 | nM | 4.80 |
| CHEMBL1783972 | — | IC50 | = | 43200.0 | nM | 4.37 |
| CHEMBL1783961 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1783969 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1783973 | — | IC50 | - | — | - | |
| CHEMBL1783974 | — | IC50 | - | — | - | |
| CHEMBL1783975 | — | IC50 | - | — | - |