Assay Detail
Binding
CHEMBL4629986
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Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Late-Stage Lead Diversification Coupled with Quantitative Nuclear Magnetic Resonance Spectroscopy to Identify New Structure-Activity Relationship Vectors at Nanomole-Scale Synthesis: Application to Loratadine, a Human Histamine H1 Receptor Inverse Agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 26 | 6.83 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1172 | DESLORATADINE | 4.0 | 1 | 7.62 |
| CHEMBL4647038 | — | — | 1 | 7.55 |
| CHEMBL4647890 | — | — | 1 | 7.32 |
| CHEMBL4637657 | — | — | 1 | 7.29 |
| CHEMBL998 | LORATADINE | 4.0 | 1 | 6.72 |
| CHEMBL3357022 | — | — | 1 | 6.70 |
| CHEMBL4642460 | — | — | 1 | 6.69 |
| CHEMBL4638183 | — | — | 1 | 6.64 |
| CHEMBL4639563 | — | — | 1 | 6.59 |
| CHEMBL4633975 | — | — | 1 | 6.57 |
| CHEMBL4649344 | — | — | 1 | 6.37 |
| CHEMBL4645629 | — | — | 1 | 6.34 |
| CHEMBL4642056 | — | — | 1 | 6.34 |
| CHEMBL4633258 | — | — | 1 | - |
| CHEMBL4632720 | — | — | 1 | - |
| CHEMBL4632879 | — | — | 1 | - |
| CHEMBL4649329 | — | — | 1 | - |
| CHEMBL4648718 | — | — | 1 | - |
| CHEMBL4634809 | — | — | 1 | - |
| CHEMBL3357023 | — | — | 1 | - |
| CHEMBL4633111 | — | — | 1 | - |
| CHEMBL4634510 | — | — | 1 | - |
| CHEMBL4646840 | — | — | 1 | - |
| CHEMBL4641273 | — | — | 1 | - |
| CHEMBL4643460 | — | — | 1 | - |
| CHEMBL4649552 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1172 | DESLORATADINE | Kd | = | 24.0 | nM | 7.62 |
| CHEMBL4647038 | — | Kd | = | 28.0 | nM | 7.55 |
| CHEMBL4647890 | — | Kd | = | 48.0 | nM | 7.32 |
| CHEMBL4637657 | — | Kd | = | 51.0 | nM | 7.29 |
| CHEMBL998 | LORATADINE | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL3357022 | — | Kd | = | 199.0 | nM | 6.70 |
| CHEMBL4642460 | — | Kd | = | 206.0 | nM | 6.69 |
| CHEMBL4638183 | — | Kd | = | 227.0 | nM | 6.64 |
| CHEMBL4639563 | — | Kd | = | 257.0 | nM | 6.59 |
| CHEMBL4633975 | — | Kd | = | 271.0 | nM | 6.57 |
| CHEMBL4649344 | — | Kd | = | 423.0 | nM | 6.37 |
| CHEMBL4645629 | — | Kd | = | 454.0 | nM | 6.34 |
| CHEMBL4642056 | — | Kd | = | 454.0 | nM | 6.34 |
| CHEMBL4633258 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL4632720 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL4632879 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL4649329 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL4648718 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL4634809 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL3357023 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL4633111 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL4634510 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL4646840 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL4641273 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL4643460 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL4649552 | — | Kd | > | 1000.0 | nM | - |