Assay Detail
Binding
CHEMBL750304
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Binding affinity against human NK2 receptors from HSKR-1 cells using [125I]-Iodohistidyl NKA
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HSKR-1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.72 | 9.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL308148 | SAREDUTANT | 3.0 | 1 | 9.36 |
| CHEMBL176811 | — | — | 1 | 8.39 |
| CHEMBL176951 | — | — | 1 | 8.16 |
| CHEMBL362394 | — | — | 1 | 8.15 |
| CHEMBL330366 | — | — | 1 | 8.08 |
| CHEMBL444086 | — | — | 1 | 7.93 |
| CHEMBL173245 | — | — | 1 | 7.92 |
| CHEMBL367528 | — | — | 1 | 7.87 |
| CHEMBL176682 | — | — | 1 | 7.78 |
| CHEMBL82386 | — | — | 1 | 7.73 |
| CHEMBL176769 | — | — | 1 | 7.72 |
| CHEMBL173420 | — | — | 1 | 7.47 |
| CHEMBL369174 | — | — | 1 | 7.37 |
| CHEMBL368159 | — | — | 1 | 7.27 |
| CHEMBL172676 | — | — | 1 | 7.26 |
| CHEMBL172915 | — | — | 1 | 7.13 |
| CHEMBL176860 | — | — | 1 | 7.02 |
| CHEMBL369498 | — | — | 1 | 6.26 |
| CHEMBL16192 | CP-96345 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL308148 | SAREDUTANT | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL176811 | — | IC50 | = | 4.04 | nM | 8.39 |
| CHEMBL176951 | — | IC50 | = | 6.94 | nM | 8.16 |
| CHEMBL362394 | — | IC50 | = | 7.02 | nM | 8.15 |
| CHEMBL330366 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL444086 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL173245 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL367528 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL176682 | — | IC50 | = | 16.7 | nM | 7.78 |
| CHEMBL82386 | — | IC50 | = | 18.8 | nM | 7.73 |
| CHEMBL176769 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL173420 | — | IC50 | = | 34.2 | nM | 7.47 |
| CHEMBL369174 | — | IC50 | = | 42.4 | nM | 7.37 |
| CHEMBL368159 | — | IC50 | = | 53.2 | nM | 7.27 |
| CHEMBL172676 | — | IC50 | = | 55.5 | nM | 7.26 |
| CHEMBL172915 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL176860 | — | IC50 | = | 96.3 | nM | 7.02 |
| CHEMBL369498 | — | IC50 | = | 548.0 | nM | 6.26 |
| CHEMBL16192 | CP-96345 | IC50 | > | 10000.0 | nM | - |