Assay Detail
Binding
CHEMBL861342
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]histamine from human H4 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 | 6.85 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL90019 | IMBUTAMINE | — | 1 | 8.00 |
| CHEMBL379027 | — | — | 1 | 7.70 |
| CHEMBL206346 | — | — | 1 | 7.40 |
| CHEMBL202744 | — | — | 1 | 7.40 |
| CHEMBL379447 | — | — | 1 | 7.40 |
| CHEMBL377954 | — | — | 1 | 7.30 |
| CHEMBL205731 | — | — | 1 | 7.30 |
| CHEMBL202728 | — | — | 1 | 7.30 |
| CHEMBL203263 | — | — | 1 | 7.20 |
| CHEMBL206303 | — | — | 1 | 7.20 |
| CHEMBL202638 | — | — | 1 | 7.20 |
| CHEMBL205559 | — | — | 1 | 7.10 |
| CHEMBL383324 | — | — | 1 | 7.00 |
| CHEMBL204843 | — | — | 1 | 7.00 |
| CHEMBL206451 | — | — | 1 | 6.90 |
| CHEMBL205834 | — | — | 1 | 6.90 |
| CHEMBL203390 | — | — | 1 | 6.80 |
| CHEMBL381074 | — | — | 1 | 6.80 |
| CHEMBL205732 | — | — | 1 | 6.70 |
| CHEMBL203441 | — | — | 1 | 6.70 |
| CHEMBL417096 | IMPENTAMINE | — | 1 | 6.60 |
| CHEMBL204413 | — | — | 1 | 6.50 |
| CHEMBL203389 | — | — | 1 | 6.50 |
| CHEMBL204615 | — | — | 1 | 6.50 |
| CHEMBL205583 | — | — | 1 | 6.40 |
| CHEMBL206548 | — | — | 1 | 6.30 |
| CHEMBL204360 | — | — | 1 | 6.30 |
| CHEMBL205868 | — | — | 1 | 6.30 |
| CHEMBL205511 | — | — | 1 | 6.20 |
| CHEMBL203228 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL90019 | IMBUTAMINE | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL379027 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL206346 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL202744 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL379447 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL377954 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL205731 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL202728 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL203263 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL206303 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL202638 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL205559 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL383324 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL204843 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL205834 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL206451 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL203390 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL381074 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL205732 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL203441 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL417096 | IMPENTAMINE | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL204413 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL203389 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL204615 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL205583 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL206548 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL204360 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL205868 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL205511 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL203228 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL377491 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL206000 | — | Ki | = | 794.33 | nM | 6.10 |