Assay Detail
Binding
CHEMBL5733330
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cell-based Functional Assay: Measurement of [Ca2+]i using a FLIPR: CHO-OX1 or CHO-OX2 cells are seeded into black-walled clear-base 384-well plates (Costar) at a density of 20,000 cells per well in F12-K medium supplemented with 10% FBS and selection antibiotic (500 ug/ml G418 or 15 ug/ml Blasticidin) and cultured overnight. The cells are incubated with equal volume of calcium4 loading buffer (Molecular Devices, Inc.) containing 2.5 mM probenecid at 37° C. for 30 min, followed by putative OX1 or OX2 receptor antagonists (dose-range 0.1 nM-10 μM) for another 30 min.
1128
Total Activities
364
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Substituted prolines/piperidines as orexin receptor antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 376 | 7.65 | 9.00 |
| kon | 376 | - | - |
| k_off | 376 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5840325 | — | — | 3 | 9.00 |
| CHEMBL5837040 | — | — | 3 | 9.00 |
| CHEMBL5804937 | — | — | 3 | 9.00 |
| CHEMBL5872093 | — | — | 3 | 9.00 |
| CHEMBL5909020 | — | — | 3 | 9.00 |
| CHEMBL5896872 | — | — | 3 | 9.00 |
| CHEMBL5750962 | — | — | 3 | 9.00 |
| CHEMBL6003214 | — | — | 6 | 9.00 |
| CHEMBL5924693 | — | — | 3 | 9.00 |
| CHEMBL2031485 | — | — | 3 | 9.00 |
| CHEMBL6063902 | — | — | 3 | 9.00 |
| CHEMBL5933560 | — | — | 3 | 9.00 |
| CHEMBL5854442 | — | — | 3 | 9.00 |
| CHEMBL6057686 | — | — | 3 | 9.00 |
| CHEMBL5939278 | — | — | 3 | 9.00 |
| CHEMBL6041150 | — | — | 3 | 9.00 |
| CHEMBL5815031 | — | — | 3 | 9.00 |
| CHEMBL6019570 | — | — | 3 | 8.70 |
| CHEMBL5800593 | — | — | 3 | 8.70 |
| CHEMBL6016963 | — | — | 3 | 8.70 |
| CHEMBL5905716 | — | — | 3 | 8.70 |
| CHEMBL5904321 | — | — | 6 | 8.70 |
| CHEMBL5958744 | — | — | 6 | 8.70 |
| CHEMBL5999151 | — | — | 3 | 8.70 |
| CHEMBL6028684 | — | — | 3 | 8.70 |
| CHEMBL5994245 | — | — | 3 | 8.70 |
| CHEMBL5753451 | — | — | 3 | 8.70 |
| CHEMBL6057653 | — | — | 3 | 8.70 |
| CHEMBL5893649 | — | — | 6 | 8.70 |
| CHEMBL5976505 | — | — | 3 | 8.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6003214 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5854442 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5750962 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5837040 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5804937 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5939278 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5815031 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5896872 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2031485 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5909020 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL6063902 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL6003214 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5840325 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5872093 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL6041150 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5933560 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL6057686 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5924693 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5905716 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL6028684 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5904321 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL6019570 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5999151 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5958744 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5976505 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL6057653 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5753451 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5994245 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL6016963 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5800593 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5893649 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2031491 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5898351 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5782275 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5740980 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5888508 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL6016517 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5982728 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5884119 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5771582 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL6001089 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5795307 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2031490 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2031492 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5803615 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5918262 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5904321 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5829488 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL6003372 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5982728 | — | IC50 | = | 3.0 | nM | 8.52 |