Assay Detail
Functional
CHEMBL853235
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at human B2 receptor transfected in CHO cells assessed as ability to antagonize BK-induced inositol-phosphate accumulation
21
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of novel sulfonamide-containing bradykinin hB2 receptor antagonists. 1. Synthesis and SAR of alpha,alpha-dimethylglycine sulfonamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 18 | 7.99 | 9.10 |
| pA2 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL380273 | — | — | 1 | 9.10 |
| CHEMBL378237 | — | — | 1 | 8.60 |
| CHEMBL205093 | — | — | 1 | 8.60 |
| CHEMBL210788 | — | — | 1 | 8.60 |
| CHEMBL383167 | — | — | 1 | 8.50 |
| CHEMBL206312 | — | — | 1 | 8.10 |
| CHEMBL209719 | — | — | 1 | 8.10 |
| CHEMBL206474 | — | — | 1 | 8.10 |
| CHEMBL209346 | — | — | 1 | 7.96 |
| CHEMBL206938 | — | — | 1 | 7.95 |
| CHEMBL377612 | — | — | 1 | 7.70 |
| CHEMBL209038 | — | — | 1 | 7.70 |
| CHEMBL378189 | — | — | 1 | 7.60 |
| CHEMBL209773 | — | — | 1 | 7.60 |
| CHEMBL379063 | — | — | 1 | 7.40 |
| CHEMBL383989 | — | — | 1 | 7.40 |
| CHEMBL377800 | — | — | 1 | 7.40 |
| CHEMBL211017 | — | — | 1 | 7.40 |
| CHEMBL437491 | — | — | 1 | - |
| CHEMBL378567 | — | — | 1 | - |
| CHEMBL209130 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL380273 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL378237 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL205093 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL210788 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL383167 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL206312 | — | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL209719 | — | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL206474 | — | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL209346 | — | Kd | = | 10.96 | nM | 7.96 |
| CHEMBL206938 | — | Kd | = | 11.22 | nM | 7.95 |
| CHEMBL377612 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL209038 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL378189 | — | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL209773 | — | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL379063 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL383989 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL377800 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL211017 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL437491 | — | pA2 | - | — | - | |
| CHEMBL378567 | — | pA2 | - | — | - | |
| CHEMBL209130 | — | pA2 | - | — | - |