Assay Detail
Binding
CHEMBL714704
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Monophasic inhibitory concentration against melatonin receptor was measured on ovine pars tuberalis membrane.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Ovis aries |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis and structure-activity relationships of novel naphthalenic and bioisosteric related amidic derivatives as melatonin receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 7.10 | 10.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL320267 | — | — | 1 | 10.82 |
| CHEMBL10878 | AGOMELATINE | 4.0 | 1 | 10.12 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.80 |
| CHEMBL113441 | — | — | 1 | 9.01 |
| CHEMBL109235 | — | — | 1 | 8.92 |
| CHEMBL323332 | — | — | 1 | 8.77 |
| CHEMBL109086 | — | — | 1 | 8.72 |
| CHEMBL320253 | — | — | 1 | 8.41 |
| CHEMBL321612 | — | — | 1 | 8.40 |
| CHEMBL110980 | — | — | 1 | 8.26 |
| CHEMBL111718 | — | — | 1 | 8.23 |
| CHEMBL111063 | — | — | 1 | 7.59 |
| CHEMBL325593 | — | — | 1 | 7.50 |
| CHEMBL109361 | — | — | 1 | 7.33 |
| CHEMBL111558 | — | — | 1 | 7.00 |
| CHEMBL109595 | — | — | 1 | 6.91 |
| CHEMBL109784 | — | — | 1 | 6.61 |
| CHEMBL419024 | — | — | 1 | 6.51 |
| CHEMBL111464 | — | — | 1 | 6.50 |
| CHEMBL290646 | — | — | 1 | 6.36 |
| CHEMBL111062 | — | — | 1 | 5.88 |
| CHEMBL111673 | — | — | 1 | 5.73 |
| CHEMBL111674 | — | — | 1 | 5.73 |
| CHEMBL324078 | — | — | 1 | 5.61 |
| CHEMBL34348 | — | — | 1 | 5.60 |
| CHEMBL111748 | — | — | 1 | 5.58 |
| CHEMBL37341 | — | — | 1 | 5.57 |
| CHEMBL419566 | — | — | 1 | 5.52 |
| CHEMBL113692 | — | — | 1 | 5.28 |
| CHEMBL37721 | — | — | 1 | 5.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL320267 | — | IC50 | = | 0.0153 | nM | 10.82 |
| CHEMBL10878 | AGOMELATINE | IC50 | = | 0.0761 | nM | 10.12 |
| CHEMBL45 | MELATONIN | IC50 | = | 0.157 | nM | 9.80 |
| CHEMBL113441 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL109235 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL323332 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL109086 | — | IC50 | = | 1.89 | nM | 8.72 |
| CHEMBL320253 | — | IC50 | = | 3.87 | nM | 8.41 |
| CHEMBL321612 | — | IC50 | = | 4.01 | nM | 8.40 |
| CHEMBL110980 | — | IC50 | = | 5.45 | nM | 8.26 |
| CHEMBL111718 | — | IC50 | = | 5.82 | nM | 8.23 |
| CHEMBL111063 | — | IC50 | = | 25.8 | nM | 7.59 |
| CHEMBL325593 | — | IC50 | = | 31.4 | nM | 7.50 |
| CHEMBL109361 | — | IC50 | = | 46.9 | nM | 7.33 |
| CHEMBL111558 | — | IC50 | = | 98.9 | nM | 7.00 |
| CHEMBL109595 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL109784 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL419024 | — | IC50 | = | 307.0 | nM | 6.51 |
| CHEMBL111464 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL290646 | — | IC50 | = | 438.0 | nM | 6.36 |
| CHEMBL111062 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL111673 | — | IC50 | = | 1880.0 | nM | 5.73 |
| CHEMBL111674 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL324078 | — | IC50 | = | 2440.0 | nM | 5.61 |
| CHEMBL34348 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL111748 | — | IC50 | = | 2610.0 | nM | 5.58 |
| CHEMBL37341 | — | IC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL419566 | — | IC50 | = | 2990.0 | nM | 5.52 |
| CHEMBL113692 | — | IC50 | = | 5260.0 | nM | 5.28 |
| CHEMBL37721 | — | IC50 | = | 9790.0 | nM | 5.01 |
| CHEMBL290568 | — | IC50 | = | 9940.0 | nM | 5.00 |
| CHEMBL324467 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL288300 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL290493 | — | IC50 | = | 0.00345 | nM | - |
| CHEMBL322269 | — | IC50 | = | 0.00118 | nM | - |
| CHEMBL37549 | — | IC50 | = | 5e-05 | nM | - |
| CHEMBL322339 | — | IC50 | < | 0.001 | nM | - |