Assay Detail
Functional
CHEMBL1287096
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human 5HT2C receptor expressed in human SH-SY5Y cells by FLIPR assay
38
Total Activities
37
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SH-SY5Y |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 7.01 | 8.20 |
| pKi | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1276948 | — | — | 1 | 8.20 |
| CHEMBL1278116 | — | — | 1 | 8.10 |
| CHEMBL1278201 | — | — | 1 | 7.80 |
| CHEMBL1277769 | — | — | 1 | 7.80 |
| CHEMBL1278202 | — | — | 1 | 7.70 |
| CHEMBL1276859 | — | — | 1 | 7.70 |
| CHEMBL1277312 | — | — | 1 | 7.50 |
| CHEMBL1277584 | — | — | 1 | 7.50 |
| CHEMBL1277770 | — | — | 1 | 7.20 |
| CHEMBL1276947 | — | — | 1 | 7.20 |
| CHEMBL1278114 | — | — | 1 | 7.00 |
| CHEMBL1277679 | — | — | 1 | 6.90 |
| CHEMBL1277935 | — | — | 2 | 6.80 |
| CHEMBL1278020 | — | — | 1 | 6.80 |
| CHEMBL1277854 | — | — | 1 | 6.70 |
| CHEMBL534 | KETOTIFEN | 4.0 | 1 | 6.70 |
| CHEMBL1278113 | — | — | 1 | 6.70 |
| CHEMBL1277035 | — | — | 1 | 6.60 |
| CHEMBL1278112 | — | — | 1 | 6.50 |
| CHEMBL74355 | VOLINANSERIN | 3.0 | 1 | 6.50 |
| CHEMBL1277855 | — | — | 1 | 6.50 |
| CHEMBL1277678 | — | — | 1 | 6.00 |
| CHEMBL1277126 | — | — | 1 | 6.00 |
| CHEMBL1278019 | — | — | 1 | 5.80 |
| CHEMBL1277216 | — | — | 1 | - |
| CHEMBL1277491 | — | — | 1 | - |
| CHEMBL1277401 | — | — | 1 | - |
| CHEMBL1278115 | — | — | 1 | - |
| CHEMBL1277400 | — | — | 1 | - |
| CHEMBL1278021 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1276948 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL1278116 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL1277769 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL1278201 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL1278202 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL1276859 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL1277584 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL1277312 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL1277770 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL1276947 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL1278114 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1277679 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL1278020 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL1277935 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL534 | KETOTIFEN | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL1278113 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL1277854 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL1277035 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL1278112 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL74355 | VOLINANSERIN | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL1277855 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL1277678 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1277126 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1278019 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL1277585 | — | Ki | > | 2511.89 | nM | - |
| CHEMBL1277492 | — | pKi | - | — | - | |
| CHEMBL1276860 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL1277034 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL1277125 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL1277216 | — | pKi | - | — | - | |
| CHEMBL1277217 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL1278021 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL1277311 | — | pKi | - | — | - | |
| CHEMBL1278115 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL1277400 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL1277401 | — | pKi | - | — | - | |
| CHEMBL1277491 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL1277935 | — | Ki | > | 1995.26 | nM | - |