Assay Detail
Binding
CHEMBL861819
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]N-alpha-methylhistamine from human H3 receptor expressed in SK-N-MC cells
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SK-N-MC |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
A chemical switch for the modulation of the functional activity of higher homologues of histamine on the human histamine H3 receptor: effect of various substitutions at the primary amino function.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 7.85 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL205834 | — | — | 1 | 8.80 |
| CHEMBL203263 | — | — | 1 | 8.60 |
| CHEMBL377954 | — | — | 1 | 8.50 |
| CHEMBL206000 | — | — | 1 | 8.50 |
| CHEMBL205559 | — | — | 1 | 8.50 |
| CHEMBL90019 | IMBUTAMINE | — | 1 | 8.40 |
| CHEMBL202744 | — | — | 1 | 8.40 |
| CHEMBL203441 | — | — | 1 | 8.40 |
| CHEMBL417096 | IMPENTAMINE | — | 1 | 8.30 |
| CHEMBL381074 | — | — | 1 | 8.30 |
| CHEMBL206303 | — | — | 1 | 8.20 |
| CHEMBL203389 | — | — | 1 | 8.10 |
| CHEMBL205731 | — | — | 1 | 8.10 |
| CHEMBL204413 | — | — | 1 | 8.10 |
| CHEMBL206346 | — | — | 1 | 8.00 |
| CHEMBL206451 | — | — | 1 | 7.90 |
| CHEMBL379027 | — | — | 1 | 7.80 |
| CHEMBL203390 | — | — | 1 | 7.80 |
| CHEMBL206548 | — | — | 1 | 7.80 |
| CHEMBL205583 | — | — | 1 | 7.70 |
| CHEMBL204843 | — | — | 1 | 7.60 |
| CHEMBL383324 | — | — | 1 | 7.50 |
| CHEMBL203228 | — | — | 1 | 7.50 |
| CHEMBL202638 | — | — | 1 | 7.40 |
| CHEMBL205868 | — | — | 1 | 7.40 |
| CHEMBL204360 | — | — | 1 | 7.40 |
| CHEMBL379447 | — | — | 1 | 7.40 |
| CHEMBL202728 | — | — | 1 | 7.40 |
| CHEMBL205511 | — | — | 1 | 7.20 |
| CHEMBL205732 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL205834 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL203263 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL377954 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL206000 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL205559 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL90019 | IMBUTAMINE | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL202744 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL203441 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL381074 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL417096 | IMPENTAMINE | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL206303 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL203389 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL205731 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL204413 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL206346 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL206451 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL379027 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL206548 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL203390 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL205583 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL204843 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL383324 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL203228 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL202638 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL205868 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL204360 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL379447 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL202728 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL205511 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL205732 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL204615 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL377491 | — | Ki | = | 630.96 | nM | 6.20 |