Assay Detail
Binding
CHEMBL3887282
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Methods of treatment of histamine H-4 receptor-related pruritus
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 4.82 | 5.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL534 | KETOTIFEN | 4.0 | 1 | 5.64 |
| CHEMBL1197564 | NORKETOTIFEN | 2.0 | 1 | 4.96 |
| CHEMBL1172 | DESLORATADINE | 4.0 | 1 | 4.80 |
| CHEMBL3929465 | — | — | 1 | 4.77 |
| CHEMBL4115693 | — | — | 1 | 4.64 |
| CHEMBL657 | DIPHENHYDRAMINE | 4.0 | 1 | 4.08 |
| CHEMBL998 | LORATADINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL534 | KETOTIFEN | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL1197564 | NORKETOTIFEN | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1172 | DESLORATADINE | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL3929465 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4115693 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL657 | DIPHENHYDRAMINE | IC50 | = | 84000.0 | nM | 4.08 |
| CHEMBL998 | LORATADINE | IC50 | = | 1500000.0 | nM | - |