Assay Detail
Binding
CHEMBL1059633
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and structure-activity relationships of phenothiazine carboxylic acids having pyrimidine-dione as novel histamine H(1) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.33 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1633 | KETOTIFEN FUMARATE | 4.0 | 1 | 9.00 |
| CHEMBL564370 | — | — | 1 | 7.64 |
| CHEMBL559665 | — | — | 1 | 7.64 |
| CHEMBL560120 | — | — | 1 | 7.55 |
| CHEMBL552057 | — | — | 1 | 7.46 |
| CHEMBL551457 | — | — | 1 | 7.43 |
| CHEMBL559664 | — | — | 1 | 7.40 |
| CHEMBL563647 | — | — | 1 | 7.39 |
| CHEMBL551394 | — | — | 1 | 7.39 |
| CHEMBL563520 | — | — | 1 | 7.34 |
| CHEMBL561377 | — | — | 1 | 7.28 |
| CHEMBL560061 | — | — | 1 | 7.16 |
| CHEMBL565083 | — | — | 1 | 7.14 |
| CHEMBL914 | FEXOFENADINE | 4.0 | 1 | 7.11 |
| CHEMBL563271 | — | — | 1 | 7.06 |
| CHEMBL560917 | — | — | 1 | 6.98 |
| CHEMBL564168 | — | — | 1 | 6.91 |
| CHEMBL562676 | — | — | 1 | 6.91 |
| CHEMBL562792 | — | — | 1 | 6.49 |
| CHEMBL560517 | — | — | 1 | - |
| CHEMBL561981 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1633 | KETOTIFEN FUMARATE | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL564370 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL559665 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL560120 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL552057 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL551457 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL559664 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL563647 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL551394 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL563520 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL561377 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL560061 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL565083 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL914 | FEXOFENADINE | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL563271 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL560917 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL564168 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL562676 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL562792 | — | IC50 | = | 323.0 | nM | 6.49 |
| CHEMBL560517 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL561981 | — | IC50 | > | 500.0 | nM | - |