Assay Detail
Binding
CHEMBL1909156
Review assay metadata, readout intent, target linkage, and publication context from the same page.
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-K1 |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 871 | 7.22 | 9.38 |
| Ki | 871 | 8.14 | 10.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1626 | CLEMASTINE | 4.0 | 2 | 10.31 |
| CHEMBL1628227 | DOXEPIN | 4.0 | 2 | 10.18 |
| CHEMBL534 | KETOTIFEN | 4.0 | 2 | 9.86 |
| CHEMBL6437 | MIANSERIN | 4.0 | 2 | 9.76 |
| CHEMBL643 | PROMETHAZINE | 4.0 | 2 | 9.48 |
| CHEMBL1201203 | BENZTROPINE | 4.0 | 2 | 9.43 |
| CHEMBL564 | PROMAZINE | 4.0 | 2 | 9.40 |
| CHEMBL516 | CYPROHEPTADINE | 4.0 | 2 | 9.37 |
| CHEMBL511 | PYRILAMINE | 4.0 | 2 | 9.37 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 2 | 9.26 |
| CHEMBL42 | CLOZAPINE | 4.0 | 2 | 9.24 |
| CHEMBL1201353 | DEXCHLORPHENIRAMINE | 4.0 | 2 | 9.14 |
| CHEMBL21731 | MAPROTILINE | 4.0 | 2 | 8.99 |
| CHEMBL1172 | DESLORATADINE | 4.0 | 2 | 8.94 |
| CHEMBL1909072 | PIPAMAZINE | 4.0 | 2 | 8.94 |
| CHEMBL715 | OLANZAPINE | 4.0 | 2 | 8.83 |
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 2 | 8.79 |
| CHEMBL1411979 | METHAPYRILENE | 4.0 | 2 | 8.74 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 2 | 8.71 |
| CHEMBL17157 | TERFENADINE | 4.0 | 2 | 8.59 |
| CHEMBL728 | PROCHLORPERAZINE | 4.0 | 2 | 8.55 |
| CHEMBL85 | RISPERIDONE | 4.0 | 2 | 8.54 |
| CHEMBL395110 | MEPAZINE | 4.0 | 2 | 8.51 |
| CHEMBL305660 | EBASTINE | 4.0 | 2 | 8.48 |
| CHEMBL648 | CYCLIZINE | 4.0 | 2 | 8.35 |
| CHEMBL716 | QUETIAPINE | 4.0 | 2 | 8.34 |
| CHEMBL726 | FLUPHENAZINE | 4.0 | 2 | 8.33 |
| CHEMBL445 | NORTRIPTYLINE | 4.0 | 2 | 8.23 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 2 | 8.07 |
| CHEMBL43064 | CINNARIZINE | 2.0 | 2 | 8.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1626 | CLEMASTINE | Ki | = | 0.049 | nM | 10.31 |
| CHEMBL1628227 | DOXEPIN | Ki | = | 0.066 | nM | 10.18 |
| CHEMBL534 | KETOTIFEN | Ki | = | 0.138 | nM | 9.86 |
| CHEMBL6437 | MIANSERIN | Ki | = | 0.175 | nM | 9.76 |
| CHEMBL643 | PROMETHAZINE | Ki | = | 0.334 | nM | 9.48 |
| CHEMBL1201203 | BENZTROPINE | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL564 | PROMAZINE | Ki | = | 0.399 | nM | 9.40 |
| CHEMBL1626 | CLEMASTINE | IC50 | = | 0.421 | nM | 9.38 |
| CHEMBL511 | PYRILAMINE | Ki | = | 0.432 | nM | 9.37 |
| CHEMBL516 | CYPROHEPTADINE | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 0.555 | nM | 9.26 |
| CHEMBL42 | CLOZAPINE | Ki | = | 0.571 | nM | 9.24 |
| CHEMBL1628227 | DOXEPIN | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL1201353 | DEXCHLORPHENIRAMINE | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL21731 | MAPROTILINE | Ki | = | 1.021 | nM | 8.99 |
| CHEMBL1172 | DESLORATADINE | Ki | = | 1.159 | nM | 8.94 |
| CHEMBL1909072 | PIPAMAZINE | Ki | = | 1.154 | nM | 8.94 |
| CHEMBL534 | KETOTIFEN | IC50 | = | 1.188 | nM | 8.93 |
| CHEMBL715 | OLANZAPINE | Ki | = | 1.473 | nM | 8.83 |
| CHEMBL6437 | MIANSERIN | IC50 | = | 1.506 | nM | 8.82 |
| CHEMBL296419 | ASTEMIZOLE | Ki | = | 1.611 | nM | 8.79 |
| CHEMBL1411979 | METHAPYRILENE | Ki | = | 1.802 | nM | 8.74 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 1.957 | nM | 8.71 |
| CHEMBL17157 | TERFENADINE | Ki | = | 2.587 | nM | 8.59 |
| CHEMBL728 | PROCHLORPERAZINE | Ki | = | 2.794 | nM | 8.55 |
| CHEMBL643 | PROMETHAZINE | IC50 | = | 2.871 | nM | 8.54 |
| CHEMBL85 | RISPERIDONE | Ki | = | 2.87 | nM | 8.54 |
| CHEMBL395110 | MEPAZINE | Ki | = | 3.126 | nM | 8.51 |
| CHEMBL1201203 | BENZTROPINE | IC50 | = | 3.183 | nM | 8.50 |
| CHEMBL305660 | EBASTINE | Ki | = | 3.287 | nM | 8.48 |
| CHEMBL564 | PROMAZINE | IC50 | = | 3.435 | nM | 8.46 |
| CHEMBL511 | PYRILAMINE | IC50 | = | 3.721 | nM | 8.43 |
| CHEMBL516 | CYPROHEPTADINE | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL648 | CYCLIZINE | Ki | = | 4.443 | nM | 8.35 |
| CHEMBL716 | QUETIAPINE | Ki | = | 4.599 | nM | 8.34 |
| CHEMBL726 | FLUPHENAZINE | Ki | = | 4.662 | nM | 8.33 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 4.782 | nM | 8.32 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 4.912 | nM | 8.31 |
| CHEMBL445 | NORTRIPTYLINE | Ki | = | 5.862 | nM | 8.23 |
| CHEMBL1201353 | DEXCHLORPHENIRAMINE | IC50 | = | 6.288 | nM | 8.20 |
| CHEMBL479 | THIORIDAZINE | Ki | = | 8.412 | nM | 8.07 |
| CHEMBL43064 | CINNARIZINE | Ki | = | 8.622 | nM | 8.06 |
| CHEMBL21731 | MAPROTILINE | IC50 | = | 8.792 | nM | 8.06 |
| CHEMBL415 | CLOMIPRAMINE | Ki | = | 9.827 | nM | 8.01 |
| CHEMBL1172 | DESLORATADINE | IC50 | = | 9.977 | nM | 8.00 |
| CHEMBL1909072 | PIPAMAZINE | IC50 | = | 9.939 | nM | 8.00 |
| CHEMBL1113 | AMOXAPINE | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL715 | OLANZAPINE | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1411979 | METHAPYRILENE | IC50 | = | 16.0 | nM | 7.80 |