Assay Detail
Binding
CHEMBL748492
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Tested against cloned human NK1 receptor by displacement of 125 I -labeled substance P expressed in CHO cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.99 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL16192 | CP-96345 | — | 1 | 9.70 |
| CHEMBL22870 | L-732138 | — | 1 | 8.80 |
| CHEMBL23129 | L-708568 | — | 1 | 7.17 |
| CHEMBL281804 | — | — | 1 | 6.90 |
| CHEMBL24549 | — | — | 1 | 6.88 |
| CHEMBL24314 | — | — | 1 | 6.55 |
| CHEMBL429395 | — | — | 1 | 6.38 |
| CHEMBL23715 | — | — | 1 | 6.26 |
| CHEMBL279050 | — | — | 1 | 5.81 |
| CHEMBL26623 | — | — | 1 | 5.42 |
| CHEMBL278555 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL16192 | CP-96345 | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL22870 | L-732138 | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL23129 | L-708568 | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL281804 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL24549 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL24314 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL429395 | — | IC50 | = | 413.0 | nM | 6.38 |
| CHEMBL23715 | — | IC50 | = | 553.0 | nM | 6.26 |
| CHEMBL279050 | — | IC50 | = | 1533.0 | nM | 5.81 |
| CHEMBL26623 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL278555 | — | IC50 | > | 10000.0 | nM | - |