Assay Detail
Functional
CHEMBL855750
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist potency at human bradykinin B2 receptor assessed as effect on inositol monophosphate accumulation in CHOdhfr- cells
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of novel sulfonamide-containing bradykinin hB2 receptor antagonists. 2. Synthesis and structure-activity relationships of alpha,alpha-cycloalkylglycine sulfonamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 34 | 8.97 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL218427 | FASITIBANT | 2.0 | 1 | 10.30 |
| CHEMBL415366 | — | — | 1 | 9.80 |
| CHEMBL373607 | — | — | 1 | 9.60 |
| CHEMBL375689 | — | — | 1 | 9.60 |
| CHEMBL387452 | — | — | 1 | 9.50 |
| CHEMBL207939 | — | — | 1 | 9.40 |
| CHEMBL249235 | — | — | 1 | 9.30 |
| CHEMBL373459 | — | — | 1 | 9.30 |
| CHEMBL375576 | — | — | 1 | 9.30 |
| CHEMBL221285 | — | — | 1 | 9.20 |
| CHEMBL380273 | — | — | 1 | 9.10 |
| CHEMBL375820 | — | — | 1 | 9.10 |
| CHEMBL220595 | — | — | 1 | 9.10 |
| CHEMBL267493 | — | — | 1 | 9.10 |
| CHEMBL218636 | — | — | 1 | 8.90 |
| CHEMBL220478 | — | — | 1 | 8.90 |
| CHEMBL374273 | — | — | 1 | 8.90 |
| CHEMBL415151 | — | — | 1 | 8.80 |
| CHEMBL375354 | — | — | 1 | 8.80 |
| CHEMBL220693 | — | — | 1 | 8.80 |
| CHEMBL386794 | — | — | 1 | 8.80 |
| CHEMBL266493 | — | — | 1 | 8.80 |
| CHEMBL220596 | — | — | 1 | 8.80 |
| CHEMBL221683 | — | — | 1 | 8.70 |
| CHEMBL220591 | — | — | 1 | 8.70 |
| CHEMBL222156 | — | — | 1 | 8.70 |
| CHEMBL376866 | — | — | 1 | 8.70 |
| CHEMBL218540 | — | — | 1 | 8.60 |
| CHEMBL205093 | — | — | 1 | 8.60 |
| CHEMBL374272 | — | — | 1 | 8.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL218427 | FASITIBANT | Kd | = | 0.05012 | nM | 10.30 |
| CHEMBL415366 | — | Kd | = | 0.1585 | nM | 9.80 |
| CHEMBL373607 | — | Kd | = | 0.2512 | nM | 9.60 |
| CHEMBL375689 | — | Kd | = | 0.2512 | nM | 9.60 |
| CHEMBL387452 | — | Kd | = | 0.3162 | nM | 9.50 |
| CHEMBL207939 | — | Kd | = | 0.3981 | nM | 9.40 |
| CHEMBL249235 | — | Kd | = | 0.5012 | nM | 9.30 |
| CHEMBL373459 | — | Kd | = | 0.5012 | nM | 9.30 |
| CHEMBL375576 | — | Kd | = | 0.5012 | nM | 9.30 |
| CHEMBL221285 | — | Kd | = | 0.631 | nM | 9.20 |
| CHEMBL380273 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL267493 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL220595 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL375820 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL374273 | — | Kd | = | 1.259 | nM | 8.90 |
| CHEMBL218636 | — | Kd | = | 1.259 | nM | 8.90 |
| CHEMBL220478 | — | Kd | = | 1.259 | nM | 8.90 |
| CHEMBL415151 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL220596 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL266493 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL386794 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL220693 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL375354 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL221683 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL220591 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL222156 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL376866 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL218540 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL205093 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL374272 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL383167 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL415152 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL222167 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL374224 | — | Kd | = | 6.31 | nM | 8.20 |