Assay Detail
Functional
CHEMBL751789
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In vitro functional activity towards Neurokinin NK2 receptor on isolated rabbit urinary bladder (RUB)
14
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Insertion of 2-carboxysuccinate and tricarballylic acid fragments into cyclic-pseudopeptides: new antagonists for the human tachykinin NK-2 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 14 | 8.61 | 9.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2112925 | — | — | 1 | 9.20 |
| CHEMBL2112922 | — | — | 2 | 9.10 |
| CHEMBL161242 | — | — | 1 | 9.00 |
| CHEMBL2112923 | — | — | 1 | 9.00 |
| CHEMBL159449 | — | — | 1 | 8.60 |
| CHEMBL2112926 | — | — | 1 | 8.50 |
| CHEMBL346285 | — | — | 1 | 8.50 |
| CHEMBL345402 | — | — | 1 | 8.40 |
| CHEMBL159585 | — | — | 1 | 8.40 |
| CHEMBL435324 | — | — | 1 | 8.30 |
| CHEMBL161288 | — | — | 1 | 8.20 |
| CHEMBL2112924 | — | — | 1 | 8.20 |
| CHEMBL350596 | — | — | 1 | 8.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2112925 | — | Kd | = | 0.631 | nM | 9.20 |
| CHEMBL2112922 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL2112922 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL161242 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL2112923 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL159449 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL2112926 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL346285 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL345402 | — | Kd | = | 3.981 | nM | 8.40 |
| CHEMBL159585 | — | Kd | = | 3.981 | nM | 8.40 |
| CHEMBL435324 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL161288 | — | Kd | = | 6.31 | nM | 8.20 |
| CHEMBL2112924 | — | Kd | = | 6.31 | nM | 8.20 |
| CHEMBL350596 | — | Kd | = | 7.943 | nM | 8.10 |