Assay Detail
Functional
CHEMBL770811
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Relative binding affinity in rabbit saphenous vein functional assay compared to 5-HT
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Tissue | Saphenous vein |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 14 | 5.72 | 6.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2368261 | — | — | 1 | 6.77 |
| CHEMBL2368253 | — | — | 1 | 6.62 |
| CHEMBL2368260 | — | — | 1 | 6.23 |
| CHEMBL2368262 | — | — | 1 | 6.05 |
| CHEMBL350637 | — | — | 1 | 6.02 |
| CHEMBL159470 | — | — | 1 | 5.90 |
| CHEMBL3084967 | — | — | 1 | 5.73 |
| CHEMBL2368263 | — | — | 1 | 5.72 |
| CHEMBL2368255 | — | — | 1 | 5.57 |
| CHEMBL350277 | — | — | 1 | 5.41 |
| CHEMBL159536 | — | — | 1 | 5.18 |
| CHEMBL161694 | — | — | 1 | 5.12 |
| CHEMBL2368258 | — | — | 1 | 5.03 |
| CHEMBL348811 | — | — | 1 | 4.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2368261 | — | Kd | = | 169.82 | nM | 6.77 |
| CHEMBL2368253 | — | Kd | = | 239.88 | nM | 6.62 |
| CHEMBL2368260 | — | Kd | = | 588.84 | nM | 6.23 |
| CHEMBL2368262 | — | Kd | = | 891.25 | nM | 6.05 |
| CHEMBL350637 | — | Kd | = | 954.99 | nM | 6.02 |
| CHEMBL159470 | — | Kd | = | 1258.93 | nM | 5.90 |
| CHEMBL3084967 | — | Kd | = | 1862.09 | nM | 5.73 |
| CHEMBL2368263 | — | Kd | = | 1905.46 | nM | 5.72 |
| CHEMBL2368255 | — | Kd | = | 2691.53 | nM | 5.57 |
| CHEMBL350277 | — | Kd | = | 3890.45 | nM | 5.41 |
| CHEMBL159536 | — | Kd | = | 6606.93 | nM | 5.18 |
| CHEMBL161694 | — | Kd | = | 7585.78 | nM | 5.12 |
| CHEMBL2368258 | — | Kd | = | 9332.54 | nM | 5.03 |
| CHEMBL348811 | — | Kd | = | 16595.87 | nM | 4.78 |