Assay Detail
Functional
CHEMBL4192665
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Antagonist activity at His6-tagged NK1 receptor (unknown origin) expressed in CHO cells assessed as inhibition of substance-P-induced IP1 accumulation preincubated for 10 mins followed by substance-P addition measured after 30 mins by HTRF-FRET assay
4
Total Activities
4
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 | Autocuration |
Publication
Design, synthesis and biological studies of a library of NK1-Receptor Ligands Based on a 5-arylthiosubstituted 2-amino-4,6-diaryl-3-cyano-4H-pyran core: Switch from antagonist to agonist effect by chemical modification.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.28 | 8.47 |
| Kinact | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4206396 | — | — | 1 | 8.47 |
| CHEMBL419500 | — | — | 1 | 4.09 |
| CHEMBL4214013 | — | — | 1 | - |
| CHEMBL16192 | CP-96345 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4206396 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL419500 | — | IC50 | = | 81000.0 | nM | 4.09 |
| CHEMBL4214013 | — | IC50 | = | 200000.0 | nM | - |
| CHEMBL16192 | CP-96345 | Kinact | = | 3.65 | 10'-9M | - |