Assay Detail
Functional
CHEMBL1287093
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
38
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 | 38 | 7.31 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL534 | KETOTIFEN | 4.0 | 1 | 9.80 |
| CHEMBL1278116 | — | — | 1 | 8.40 |
| CHEMBL1276948 | — | — | 1 | 8.20 |
| CHEMBL1278114 | — | — | 1 | 8.00 |
| CHEMBL1278202 | — | — | 1 | 7.90 |
| CHEMBL1278201 | — | — | 1 | 7.80 |
| CHEMBL1278020 | — | — | 1 | 7.80 |
| CHEMBL1277584 | — | — | 1 | 7.70 |
| CHEMBL1277935 | — | — | 2 | 7.70 |
| CHEMBL1277585 | — | — | 1 | 7.60 |
| CHEMBL1278115 | — | — | 1 | 7.60 |
| CHEMBL1276947 | — | — | 1 | 7.50 |
| CHEMBL1276859 | — | — | 1 | 7.50 |
| CHEMBL1277854 | — | — | 1 | 7.40 |
| CHEMBL1277678 | — | — | 1 | 7.40 |
| CHEMBL1277855 | — | — | 1 | 7.40 |
| CHEMBL1276860 | — | — | 1 | 7.40 |
| CHEMBL1277126 | — | — | 1 | 7.30 |
| CHEMBL1277770 | — | — | 1 | 7.30 |
| CHEMBL1277312 | — | — | 1 | 7.30 |
| CHEMBL1277679 | — | — | 1 | 7.30 |
| CHEMBL1277769 | — | — | 1 | 7.30 |
| CHEMBL1278112 | — | — | 1 | 7.20 |
| CHEMBL1277216 | — | — | 1 | 7.10 |
| CHEMBL1277400 | — | — | 1 | 7.10 |
| CHEMBL1278113 | — | — | 1 | 7.00 |
| CHEMBL1277125 | — | — | 1 | 7.00 |
| CHEMBL1277311 | — | — | 1 | 6.90 |
| CHEMBL1278021 | — | — | 1 | 6.80 |
| CHEMBL1277217 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL534 | KETOTIFEN | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL1278116 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL1276948 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL1278114 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1278202 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL1278020 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL1278201 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL1277935 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL1277584 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL1277935 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL1277585 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL1278115 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL1276947 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL1276859 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL1277678 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL1276860 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL1277854 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL1277855 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL1277769 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL1277312 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL1277126 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL1277770 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL1277679 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL1278112 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL1277216 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL1277400 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL1278113 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1277125 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1277311 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL1277217 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL1278021 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL1277492 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL1277035 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL1277491 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL1277034 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL1278019 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL1277401 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL74355 | VOLINANSERIN | Ki | = | 1000.0 | nM | 6.00 |