Assay Detail
Functional
CHEMBL3097343
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human histamine H3 receptor expressed in CHOK1 cells assessed as inhibition of GTPgammaS binding
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 | 33 | 9.44 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3092823 | — | — | 1 | 10.10 |
| CHEMBL3092828 | — | — | 1 | 10.00 |
| CHEMBL3092650 | GSK239512 | 2.0 | 1 | 10.00 |
| CHEMBL3092820 | — | — | 1 | 10.00 |
| CHEMBL3092826 | — | — | 1 | 9.90 |
| CHEMBL3092825 | — | — | 1 | 9.90 |
| CHEMBL3092834 | — | — | 1 | 9.80 |
| CHEMBL3092651 | — | — | 1 | 9.80 |
| CHEMBL517140 | GSK189254 | 2.0 | 1 | 9.70 |
| CHEMBL1783890 | — | — | 1 | 9.70 |
| CHEMBL3092827 | — | — | 1 | 9.70 |
| CHEMBL3092821 | — | — | 1 | 9.70 |
| CHEMBL3092838 | — | — | 1 | 9.70 |
| CHEMBL3092840 | — | — | 1 | 9.60 |
| CHEMBL3092643 | — | — | 1 | 9.60 |
| CHEMBL3092649 | — | — | 1 | 9.60 |
| CHEMBL3092822 | — | — | 1 | 9.50 |
| CHEMBL3092824 | — | — | 1 | 9.50 |
| CHEMBL3092829 | — | — | 1 | 9.30 |
| CHEMBL3092648 | — | — | 1 | 9.30 |
| CHEMBL3092831 | — | — | 1 | 9.30 |
| CHEMBL3092833 | — | — | 1 | 9.30 |
| CHEMBL3092835 | — | — | 1 | 9.30 |
| CHEMBL3092839 | — | — | 1 | 9.30 |
| CHEMBL3092832 | — | — | 1 | 9.20 |
| CHEMBL3091477 | — | — | 1 | 9.20 |
| CHEMBL3092837 | — | — | 1 | 9.10 |
| CHEMBL3092836 | — | — | 1 | 9.00 |
| CHEMBL3092830 | — | — | 1 | 8.90 |
| CHEMBL3092647 | — | — | 1 | 8.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3092823 | — | Ki | = | 0.07943 | nM | 10.10 |
| CHEMBL3092828 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3092820 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3092650 | GSK239512 | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3092826 | — | Ki | = | 0.1259 | nM | 9.90 |
| CHEMBL3092825 | — | Ki | = | 0.1259 | nM | 9.90 |
| CHEMBL3092834 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL3092651 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL517140 | GSK189254 | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL1783890 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL3092827 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL3092821 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL3092838 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL3092649 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL3092643 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL3092840 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL3092822 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL3092824 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL3092829 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL3092648 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL3092831 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL3092833 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL3092835 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL3092839 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL3092832 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL3091477 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL3092837 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL3092836 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3092830 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL3092647 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL3092645 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL3092646 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL3092644 | — | Ki | = | 3.162 | nM | 8.50 |