Assay Detail
Functional
CHEMBL1769655
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 8.29 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1767137 | — | — | 1 | 10.00 |
| CHEMBL1767138 | — | — | 1 | 9.80 |
| CHEMBL1767136 | — | — | 1 | 9.80 |
| CHEMBL1767141 | — | — | 1 | 9.70 |
| CHEMBL1767149 | — | — | 1 | 9.60 |
| CHEMBL1767134 | — | — | 1 | 9.60 |
| CHEMBL1767154 | — | — | 1 | 9.50 |
| CHEMBL1767140 | — | — | 1 | 9.50 |
| CHEMBL1767145 | — | — | 1 | 9.30 |
| CHEMBL1767148 | — | — | 1 | 9.10 |
| CHEMBL1767156 | — | — | 1 | 9.00 |
| CHEMBL639 | AZELASTINE | 4.0 | 1 | 8.90 |
| CHEMBL1767153 | — | — | 1 | 8.80 |
| CHEMBL1767146 | — | — | 1 | 8.80 |
| CHEMBL1767147 | — | — | 1 | 8.70 |
| CHEMBL1767158 | — | — | 1 | 8.60 |
| CHEMBL1767139 | — | — | 1 | 8.30 |
| CHEMBL1767155 | — | — | 1 | 8.20 |
| CHEMBL1767165 | — | — | 1 | 8.10 |
| CHEMBL1767164 | GSK-1004723 | 2.0 | 1 | 8.00 |
| CHEMBL1767135 | — | — | 1 | 8.00 |
| CHEMBL1767167 | — | — | 1 | 7.90 |
| CHEMBL1767166 | — | — | 1 | 7.90 |
| CHEMBL1767160 | — | — | 1 | 7.80 |
| CHEMBL1765111 | — | — | 1 | 7.80 |
| CHEMBL1767161 | — | — | 1 | 7.70 |
| CHEMBL1767168 | — | — | 1 | 7.60 |
| CHEMBL1767152 | — | — | 1 | 7.50 |
| CHEMBL1767163 | — | — | 1 | 7.40 |
| CHEMBL1767162 | — | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1767137 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL1767138 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL1767136 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL1767141 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL1767149 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL1767134 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL1767154 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL1767140 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL1767145 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL1767148 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL1767156 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL639 | AZELASTINE | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL1767153 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL1767146 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL1767147 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL1767158 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL1767139 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL1767155 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL1767165 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL1767135 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1767164 | GSK-1004723 | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1767167 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL1767166 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL1767160 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL1765111 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL1767161 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL1767168 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL1767152 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL1767163 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL1767162 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL1767159 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL1767157 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL1767151 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL1767142 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL1767143 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL1767150 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL1767144 | — | Ki | > | 1584.89 | nM | - |