Assay Detail
Functional
CHEMBL886657
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Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SK-N-MC |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 16 | 8.27 | 9.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL247268 | — | — | 1 | 9.18 |
| CHEMBL247062 | — | — | 1 | 9.14 |
| CHEMBL247063 | — | — | 1 | 8.98 |
| CHEMBL247076 | — | — | 1 | 8.98 |
| CHEMBL247670 | — | — | 1 | 8.45 |
| CHEMBL241712 | — | — | 1 | 8.45 |
| CHEMBL246873 | — | — | 1 | 8.41 |
| CHEMBL241706 | — | — | 1 | 8.23 |
| CHEMBL392429 | — | — | 1 | 8.01 |
| CHEMBL394732 | — | — | 1 | 7.95 |
| CHEMBL247472 | — | — | 1 | 7.93 |
| CHEMBL247265 | — | — | 1 | 7.85 |
| CHEMBL247094 | — | — | 1 | 7.78 |
| CHEMBL247683 | — | — | 1 | 7.74 |
| CHEMBL247061 | — | — | 1 | 7.67 |
| CHEMBL241705 | — | — | 1 | 7.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL247268 | — | Kd | = | 0.6607 | nM | 9.18 |
| CHEMBL247062 | — | Kd | = | 0.7244 | nM | 9.14 |
| CHEMBL247063 | — | Kd | = | 1.047 | nM | 8.98 |
| CHEMBL247076 | — | Kd | = | 1.047 | nM | 8.98 |
| CHEMBL247670 | — | Kd | = | 3.548 | nM | 8.45 |
| CHEMBL241712 | — | Kd | = | 3.548 | nM | 8.45 |
| CHEMBL246873 | — | Kd | = | 3.89 | nM | 8.41 |
| CHEMBL241706 | — | Kd | = | 5.888 | nM | 8.23 |
| CHEMBL392429 | — | Kd | = | 9.772 | nM | 8.01 |
| CHEMBL394732 | — | Kd | = | 11.22 | nM | 7.95 |
| CHEMBL247472 | — | Kd | = | 11.75 | nM | 7.93 |
| CHEMBL247265 | — | Kd | = | 14.13 | nM | 7.85 |
| CHEMBL247094 | — | Kd | = | 16.6 | nM | 7.78 |
| CHEMBL247683 | — | Kd | = | 18.2 | nM | 7.74 |
| CHEMBL247061 | — | Kd | = | 21.38 | nM | 7.67 |
| CHEMBL241705 | — | Kd | = | 25.7 | nM | 7.59 |