Assay Detail
Binding
CHEMBL813323
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Binding affinity towards Tachykinin receptor 1 in rat cerebral cortex membranes was determined by using 125 [I]-BHSP as radioligand
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
An SAR study for the non-peptide substance P receptor (NK1) antagonist, CP-96,345.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.70 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL235363 | SUBSTANCE P | 1.0 | 1 | 9.92 |
| CHEMBL217406 | NEUROKININ A | — | 1 | 7.51 |
| CHEMBL437797 | NEUROKININ B | — | 1 | 7.16 |
| CHEMBL356912 | — | — | 1 | 6.96 |
| CHEMBL346154 | — | — | 1 | 6.92 |
| CHEMBL346633 | — | — | 1 | 6.16 |
| CHEMBL345711 | — | — | 1 | 6.13 |
| CHEMBL419500 | — | — | 1 | 6.10 |
| CHEMBL152239 | — | — | 1 | 6.00 |
| CHEMBL357717 | — | — | 1 | 5.70 |
| CHEMBL153042 | — | — | 1 | 5.14 |
| CHEMBL358033 | — | — | 1 | - |
| CHEMBL449347 | — | — | 1 | - |
| CHEMBL152011 | — | — | 1 | - |
| CHEMBL152055 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL235363 | SUBSTANCE P | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL217406 | NEUROKININ A | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL437797 | NEUROKININ B | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL356912 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL346154 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL346633 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL345711 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL419500 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL152239 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL357717 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL153042 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL358033 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL449347 | — | IC50 | ~ | 10000.0 | nM | - |
| CHEMBL152011 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL152055 | — | IC50 | > | 10000.0 | nM | - |