Assay Detail
Binding
CHEMBL616444
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Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
26
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-K1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
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 |
|---|---|---|---|
| IC50 | 26 | 6.75 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL128 | SUMATRIPTAN | 4.0 | 1 | 9.30 |
| CHEMBL1185 | ZOLMITRIPTAN | 4.0 | 1 | 8.21 |
| CHEMBL2368254 | — | — | 1 | 8.02 |
| CHEMBL159332 | — | — | 1 | 7.84 |
| CHEMBL2110299 | — | — | 1 | 7.74 |
| CHEMBL2368256 | — | — | 1 | 7.49 |
| CHEMBL158638 | — | — | 1 | 7.35 |
| CHEMBL2368253 | — | — | 1 | 7.01 |
| CHEMBL2368257 | — | — | 2 | 7.01 |
| CHEMBL2110300 | — | — | 3 | 6.95 |
| CHEMBL3084967 | — | — | 1 | 6.85 |
| CHEMBL2368261 | — | — | 1 | 6.69 |
| CHEMBL350277 | — | — | 1 | 6.58 |
| CHEMBL2368259 | — | — | 1 | 6.56 |
| CHEMBL159470 | — | — | 1 | 6.50 |
| CHEMBL350637 | — | — | 1 | 6.08 |
| CHEMBL2368255 | — | — | 1 | 5.95 |
| CHEMBL2368262 | — | — | 1 | 5.92 |
| CHEMBL348811 | — | — | 1 | 5.87 |
| CHEMBL161694 | — | — | 1 | 5.82 |
| CHEMBL2368260 | — | — | 1 | 5.42 |
| CHEMBL159536 | — | — | 1 | 5.41 |
| CHEMBL2368258 | — | — | 1 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL128 | SUMATRIPTAN | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL1185 | ZOLMITRIPTAN | IC50 | = | 6.166 | nM | 8.21 |
| CHEMBL2368254 | — | IC50 | = | 9.55 | nM | 8.02 |
| CHEMBL159332 | — | IC50 | = | 14.45 | nM | 7.84 |
| CHEMBL2110299 | — | IC50 | = | 18.2 | nM | 7.74 |
| CHEMBL2368256 | — | IC50 | = | 32.36 | nM | 7.49 |
| CHEMBL158638 | — | IC50 | = | 44.67 | nM | 7.35 |
| CHEMBL2368253 | — | IC50 | = | 97.72 | nM | 7.01 |
| CHEMBL2368257 | — | IC50 | = | 97.72 | nM | 7.01 |
| CHEMBL2110300 | — | IC50 | = | 112.2 | nM | 6.95 |
| CHEMBL3084967 | — | IC50 | = | 141.25 | nM | 6.85 |
| CHEMBL2110300 | — | IC50 | = | 162.18 | nM | 6.79 |
| CHEMBL2368261 | — | IC50 | = | 204.17 | nM | 6.69 |
| CHEMBL2368257 | — | IC50 | = | 204.17 | nM | 6.69 |
| CHEMBL350277 | — | IC50 | = | 263.03 | nM | 6.58 |
| CHEMBL2368259 | — | IC50 | = | 275.42 | nM | 6.56 |
| CHEMBL159470 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL2110300 | — | IC50 | = | 562.34 | nM | 6.25 |
| CHEMBL350637 | — | IC50 | = | 831.76 | nM | 6.08 |
| CHEMBL2368255 | — | IC50 | = | 1122.02 | nM | 5.95 |
| CHEMBL2368262 | — | IC50 | = | 1202.26 | nM | 5.92 |
| CHEMBL348811 | — | IC50 | = | 1348.96 | nM | 5.87 |
| CHEMBL161694 | — | IC50 | = | 1513.56 | nM | 5.82 |
| CHEMBL2368260 | — | IC50 | = | 3801.89 | nM | 5.42 |
| CHEMBL159536 | — | IC50 | = | 3890.45 | nM | 5.41 |
| CHEMBL2368258 | — | IC50 | = | 6309.57 | nM | 5.20 |