Assay Detail
Binding
CHEMBL750227
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Inhibition of [3H]-SP radioligand binding to NK1 receptor from bovine retina
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
SAR of 2-benzyl-4-aminopiperidines: CGP 49823, an orally and centrally active non-peptide NK1 antagonist
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 7.04 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL295425 | — | — | 1 | 8.05 |
| CHEMBL43912 | — | — | 1 | 8.00 |
| CHEMBL290043 | — | — | 1 | 8.00 |
| CHEMBL16192 | CP-96345 | — | 1 | 8.00 |
| CHEMBL418697 | — | — | 1 | 7.96 |
| CHEMBL289026 | — | — | 1 | 7.92 |
| CHEMBL290364 | — | — | 1 | 7.89 |
| CHEMBL416983 | — | — | 1 | 7.77 |
| CHEMBL296213 | — | — | 1 | 7.72 |
| CHEMBL44474 | — | — | 1 | 7.72 |
| CHEMBL290926 | — | — | 1 | 7.70 |
| CHEMBL297833 | — | — | 1 | 7.62 |
| CHEMBL43744 | — | — | 1 | 7.58 |
| CHEMBL295122 | — | — | 1 | 7.52 |
| CHEMBL418438 | — | — | 1 | 7.27 |
| CHEMBL416436 | — | — | 1 | 7.22 |
| CHEMBL42800 | — | — | 1 | 7.21 |
| CHEMBL42050 | — | — | 1 | 7.14 |
| CHEMBL435367 | — | — | 1 | 7.04 |
| CHEMBL43432 | — | — | 1 | 6.96 |
| CHEMBL297883 | — | — | 1 | 6.89 |
| CHEMBL42306 | — | — | 1 | 6.75 |
| CHEMBL40455 | — | — | 1 | 6.68 |
| CHEMBL43977 | — | — | 1 | 6.66 |
| CHEMBL297970 | — | — | 1 | 6.66 |
| CHEMBL40875 | — | — | 1 | 6.41 |
| CHEMBL43394 | — | — | 1 | 6.28 |
| CHEMBL42778 | — | — | 1 | 6.27 |
| CHEMBL40189 | — | — | 1 | 6.22 |
| CHEMBL42103 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL295425 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL43912 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL16192 | CP-96345 | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL290043 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL418697 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL289026 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL290364 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL416983 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL296213 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL44474 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL290926 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL297833 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL43744 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL295122 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL418438 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL416436 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL42800 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL42050 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL435367 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL43432 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL297883 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL42306 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL40455 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL43977 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL297970 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL40875 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL43394 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL42778 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL40189 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL42103 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL41057 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL444043 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL297134 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL289573 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL291298 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL296262 | — | IC50 | > | 10000.0 | nM | - |