Assay Detail
Functional
CHEMBL823939
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In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and antihistaminic activity of some thiazolidin-4-ones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 16 | 6.76 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL511 | PYRILAMINE | 4.0 | 1 | 9.00 |
| CHEMBL1202934 | — | — | 1 | 8.70 |
| CHEMBL1202938 | — | — | 1 | 8.30 |
| CHEMBL1202942 | — | — | 1 | 7.70 |
| CHEMBL1202936 | — | — | 1 | 7.40 |
| CHEMBL1202937 | — | — | 1 | 7.40 |
| CHEMBL1202939 | — | — | 1 | 7.10 |
| CHEMBL1202932 | — | — | 1 | 6.40 |
| CHEMBL1202933 | — | — | 1 | 6.40 |
| CHEMBL1202941 | — | — | 1 | 6.40 |
| CHEMBL319829 | — | — | 1 | 6.20 |
| CHEMBL1202935 | — | — | 1 | 6.00 |
| CHEMBL100486 | — | — | 1 | 5.60 |
| CHEMBL1202940 | — | — | 1 | 5.40 |
| CHEMBL1202943 | — | — | 1 | 5.20 |
| CHEMBL1202929 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL511 | PYRILAMINE | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL1202934 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL1202938 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL1202942 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL1202936 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL1202937 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL1202939 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL1202932 | — | Kd | = | 398.11 | nM | 6.40 |
| CHEMBL1202933 | — | Kd | = | 398.11 | nM | 6.40 |
| CHEMBL1202941 | — | Kd | = | 398.11 | nM | 6.40 |
| CHEMBL319829 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL1202935 | — | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL100486 | — | Kd | = | 2511.89 | nM | 5.60 |
| CHEMBL1202940 | — | Kd | = | 3981.07 | nM | 5.40 |
| CHEMBL1202943 | — | Kd | = | 6309.57 | nM | 5.20 |
| CHEMBL1202929 | — | Kd | = | 10000.0 | nM | 5.00 |