Assay Detail
Binding
CHEMBL696458
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Inhibition of rat kidney Histamine N-Methyltransferase (HMT) activity determined by the formation of N-methyl-histamine
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.95 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14740 | — | — | 1 | 7.80 |
| CHEMBL277061 | — | — | 1 | 7.68 |
| CHEMBL274041 | — | — | 1 | 7.51 |
| CHEMBL14657 | — | — | 1 | 7.47 |
| CHEMBL275617 | — | — | 1 | 7.35 |
| CHEMBL15056 | — | — | 1 | 7.32 |
| CHEMBL14868 | — | — | 1 | 7.32 |
| CHEMBL277113 | — | — | 1 | 7.31 |
| CHEMBL15153 | — | — | 1 | 7.29 |
| CHEMBL15098 | — | — | 1 | 7.28 |
| CHEMBL14524 | — | — | 1 | 7.19 |
| CHEMBL14753 | — | — | 1 | 7.19 |
| CHEMBL14484 | — | — | 1 | 7.14 |
| CHEMBL14573 | — | — | 1 | 7.08 |
| CHEMBL14754 | — | — | 1 | 7.02 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 6.96 |
| CHEMBL277988 | — | — | 1 | 6.96 |
| CHEMBL14860 | — | — | 1 | 6.92 |
| CHEMBL276938 | — | — | 1 | 6.92 |
| CHEMBL15101 | — | — | 1 | 6.92 |
| CHEMBL14816 | — | — | 1 | 6.85 |
| CHEMBL14849 | — | — | 1 | 6.80 |
| CHEMBL14665 | — | — | 1 | 6.75 |
| CHEMBL14498 | — | — | 1 | 6.70 |
| CHEMBL280011 | — | — | 1 | 6.68 |
| CHEMBL276305 | — | — | 1 | 6.66 |
| CHEMBL15289 | — | — | 1 | 6.64 |
| CHEMBL14283 | — | — | 1 | 6.64 |
| CHEMBL14364 | — | — | 1 | 6.51 |
| CHEMBL14595 | — | — | 1 | 6.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14740 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL277061 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL274041 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL14657 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL275617 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL15056 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL14868 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL277113 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL15153 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL15098 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL14524 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL14753 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL14484 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL14573 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL14754 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL95 | TACRINE | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL277988 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL14860 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL15101 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL276938 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL14816 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL14849 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL14665 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL14498 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL280011 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL276305 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL15289 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL14283 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL14364 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL14595 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL14656 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL14587 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL275874 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL14781 | — | IC50 | = | 1400.0 | nM | 5.85 |