Assay Detail
Functional
CHEMBL1786003
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SK-N-SH |
| 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 | 6.27 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1783959 | — | — | 1 | 7.00 |
| CHEMBL1783963 | — | — | 1 | 6.96 |
| CHEMBL1783957 | — | — | 1 | 6.92 |
| CHEMBL1783964 | — | — | 1 | 6.92 |
| CHEMBL1783967 | — | — | 1 | 6.92 |
| CHEMBL589390 | LATREPIRDINE | 3.0 | 1 | 6.80 |
| CHEMBL1783965 | — | — | 1 | 6.80 |
| CHEMBL1783968 | — | — | 1 | 6.66 |
| CHEMBL1783970 | — | — | 1 | 6.50 |
| CHEMBL1783966 | — | — | 1 | 6.41 |
| CHEMBL1783954 | — | — | 1 | 6.30 |
| CHEMBL1783960 | — | — | 1 | 6.30 |
| CHEMBL1783958 | — | — | 1 | 6.25 |
| CHEMBL1783961 | — | — | 1 | 6.19 |
| CHEMBL1783956 | — | — | 1 | 6.03 |
| CHEMBL1783971 | — | — | 1 | 5.89 |
| CHEMBL1783953 | — | — | 1 | 5.74 |
| CHEMBL1783974 | — | — | 1 | 5.55 |
| CHEMBL1783955 | — | — | 1 | 5.33 |
| CHEMBL1783972 | — | — | 1 | 5.14 |
| CHEMBL1783975 | — | — | 1 | 5.12 |
| CHEMBL1783962 | — | — | 1 | - |
| CHEMBL1783969 | — | — | 1 | - |
| CHEMBL1783973 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1783959 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1783963 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1783957 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1783964 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1783967 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL589390 | LATREPIRDINE | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1783965 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1783968 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1783970 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL1783966 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL1783954 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1783960 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1783958 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL1783961 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL1783956 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL1783971 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL1783953 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL1783974 | — | IC50 | = | 2790.0 | nM | 5.55 |
| CHEMBL1783955 | — | IC50 | = | 4670.0 | nM | 5.33 |
| CHEMBL1783972 | — | IC50 | = | 7160.0 | nM | 5.14 |
| CHEMBL1783975 | — | IC50 | = | 7570.0 | nM | 5.12 |
| CHEMBL1783962 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1783969 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1783973 | — | IC50 | > | 10000.0 | nM | - |