Assay Detail
Functional
CHEMBL1038010
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
15
Total Activities
15
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 activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.20 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL592753 | — | — | 1 | 7.52 |
| CHEMBL603049 | — | — | 1 | 7.51 |
| CHEMBL589150 | — | — | 1 | 7.50 |
| CHEMBL599913 | — | — | 1 | 7.48 |
| CHEMBL591803 | — | — | 1 | 7.46 |
| CHEMBL589148 | — | — | 1 | 7.40 |
| CHEMBL592752 | MARITUPIRDINE | 2.0 | 1 | 7.40 |
| CHEMBL589147 | — | — | 1 | 7.18 |
| CHEMBL589388 | — | — | 1 | 7.17 |
| CHEMBL605405 | — | — | 1 | 7.16 |
| CHEMBL606036 | — | — | 1 | 7.01 |
| CHEMBL589389 | — | — | 1 | 6.98 |
| CHEMBL605081 | — | — | 1 | 6.95 |
| CHEMBL589390 | LATREPIRDINE | 3.0 | 1 | 6.80 |
| CHEMBL591568 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL592753 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL603049 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL589150 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL599913 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL591803 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL589148 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL592752 | MARITUPIRDINE | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL589147 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL589388 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL605405 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL606036 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL589389 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL605081 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL589390 | LATREPIRDINE | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL591568 | — | IC50 | = | 345.0 | nM | 6.46 |