Assay Detail
Binding
CHEMBL3097342
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Displacement of [3H]-R-alpha-ethylhistamine from histamine H3 receptor in rat cerebral cortical tissue membranes after 45 mins by liquid scintillation spectrometry
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 8.76 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3092823 | — | — | 1 | 9.70 |
| CHEMBL3092650 | GSK239512 | 2.0 | 1 | 9.44 |
| CHEMBL3092834 | — | — | 1 | 9.30 |
| CHEMBL3092840 | — | — | 1 | 9.20 |
| CHEMBL3092826 | — | — | 1 | 9.20 |
| CHEMBL3092828 | — | — | 1 | 9.20 |
| CHEMBL3092651 | — | — | 1 | 9.10 |
| CHEMBL3092825 | — | — | 1 | 9.10 |
| CHEMBL1783890 | — | — | 1 | 9.08 |
| CHEMBL3092820 | — | — | 1 | 9.00 |
| CHEMBL3092827 | — | — | 1 | 9.00 |
| CHEMBL3092821 | — | — | 1 | 8.80 |
| CHEMBL3092839 | — | — | 1 | 8.70 |
| CHEMBL3092835 | — | — | 1 | 8.60 |
| CHEMBL3092824 | — | — | 1 | 8.60 |
| CHEMBL3092822 | — | — | 1 | 8.60 |
| CHEMBL3092649 | — | — | 1 | 8.60 |
| CHEMBL517140 | GSK189254 | 2.0 | 1 | 8.58 |
| CHEMBL3092648 | — | — | 1 | 8.50 |
| CHEMBL3092838 | — | — | 1 | 8.40 |
| CHEMBL3092832 | — | — | 1 | 8.40 |
| CHEMBL3092831 | — | — | 1 | 8.40 |
| CHEMBL3092829 | — | — | 1 | 8.30 |
| CHEMBL3092830 | — | — | 1 | 8.10 |
| CHEMBL3091477 | — | — | 1 | 8.00 |
| CHEMBL3092836 | — | — | 1 | 7.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3092823 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL3092650 | GSK239512 | Ki | = | 0.3631 | nM | 9.44 |
| CHEMBL3092834 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL3092840 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL3092826 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL3092828 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL3092651 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL3092825 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL1783890 | — | Ki | = | 0.8318 | nM | 9.08 |
| CHEMBL3092820 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3092827 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3092821 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL3092839 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL3092835 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL3092824 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL3092822 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL3092649 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL517140 | GSK189254 | Ki | = | 2.63 | nM | 8.58 |
| CHEMBL3092648 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL3092838 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL3092832 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL3092831 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL3092829 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL3092830 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL3091477 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3092836 | — | Ki | = | 12.59 | nM | 7.90 |