Assay Detail
Binding
CHEMBL857872
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Binding affinity by displacement of radiolabeled GR-100679 from Tachykinin receptor 2 from homogenized rat colon
9
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
GR159897 and related analogues as highly potent, orally active non-peptide neurokinin NK2 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.01 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2110370 | — | — | 1 | 10.00 |
| CHEMBL59413 | — | — | 2 | 9.50 |
| CHEMBL60064 | 4-BENZENESULFINYLMETHYL-1-[2-(5-FLUORO-1H-INDOL-3-YL)-ETHYL]-PIPERIDIN-4-OL (STRUCTURAL MIX) | — | 2 | 9.30 |
| CHEMBL60459 | — | — | 1 | 7.50 |
| CHEMBL294336 | — | — | 1 | 7.50 |
| CHEMBL300174 | — | — | 1 | 6.00 |
| CHEMBL59594 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2110370 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL59413 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL60064 | 4-BENZENESULFINYLMETHYL-1-[2-(5-FLUORO-1H-INDOL-3-YL)-ETHYL]-PIPERIDIN-4-OL (STRUCTURAL MIX) | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL59413 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL60064 | 4-BENZENESULFINYLMETHYL-1-[2-(5-FLUORO-1H-INDOL-3-YL)-ETHYL]-PIPERIDIN-4-OL (STRUCTURAL MIX) | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL60459 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL294336 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL300174 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL59594 | — | Ki | = | 1584.89 | nM | 5.80 |