Assay Detail
Functional
CHEMBL3396059
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Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
12
Total Activities
12
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 | Autocuration |
Publication
Diaminopyrimidines, diaminopyridines and diaminopyridazines as histamine H4 receptor modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 12 | 8.47 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3393547 | — | — | 1 | 10.10 |
| CHEMBL3393526 | — | — | 1 | 9.20 |
| CHEMBL3393532 | — | — | 1 | 9.00 |
| CHEMBL3393535 | — | — | 1 | 9.00 |
| CHEMBL3354816 | — | — | 1 | 8.50 |
| CHEMBL3393548 | — | — | 1 | 8.10 |
| CHEMBL3393557 | — | — | 1 | 8.10 |
| CHEMBL3393553 | — | — | 1 | 8.00 |
| CHEMBL3393556 | — | — | 1 | 8.00 |
| CHEMBL3393550 | — | — | 1 | 7.80 |
| CHEMBL3393533 | — | — | 1 | 7.40 |
| CHEMBL3393534 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3393547 | — | Kd | = | 0.07943 | nM | 10.10 |
| CHEMBL3393526 | — | Kd | = | 0.631 | nM | 9.20 |
| CHEMBL3393532 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL3393535 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL3354816 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL3393548 | — | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL3393557 | — | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL3393553 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL3393556 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL3393550 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL3393533 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL3393534 | — | Kd | = | 0.00631 | nM | - |