Assay Detail
Functional
CHEMBL1772153
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Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
17
Total Activities
17
Compounds Tested
2
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
Triamino pyrimidines and pyridines as histamine H(4) receptor modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 13 | 8.47 | 9.40 |
| pA2 | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1770980 | — | — | 1 | 9.40 |
| CHEMBL1770979 | — | — | 1 | 9.30 |
| CHEMBL1771000 | — | — | 1 | 8.90 |
| CHEMBL1770971 | — | — | 1 | 8.80 |
| CHEMBL1770969 | — | — | 1 | 8.80 |
| CHEMBL1770992 | — | — | 1 | 8.80 |
| CHEMBL505061 | — | — | 1 | 8.70 |
| CHEMBL1770995 | — | — | 1 | 8.10 |
| CHEMBL1770977 | — | — | 1 | 8.00 |
| CHEMBL1770990 | — | — | 1 | 7.90 |
| CHEMBL1770959 | — | — | 1 | 7.90 |
| CHEMBL1770972 | — | — | 1 | 7.80 |
| CHEMBL1770965 | — | — | 1 | 7.70 |
| CHEMBL1770997 | — | — | 1 | - |
| CHEMBL1770996 | — | — | 1 | - |
| CHEMBL1770994 | — | — | 1 | - |
| CHEMBL1770160 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1770980 | — | Kd | = | 0.3981 | nM | 9.40 |
| CHEMBL1770979 | — | Kd | = | 0.5012 | nM | 9.30 |
| CHEMBL1771000 | — | Kd | = | 1.259 | nM | 8.90 |
| CHEMBL1770971 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL1770969 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL1770992 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL505061 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL1770995 | — | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL1770977 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL1770990 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL1770959 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL1770972 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL1770965 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL1770997 | — | pA2 | - | — | - | |
| CHEMBL1770996 | — | pA2 | - | — | - | |
| CHEMBL1770994 | — | pA2 | - | — | - | |
| CHEMBL1770160 | — | pA2 | - | — | - |