Assay Detail
Binding
CHEMBL692580
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Inhibitory activity measured by [3H]- N alpha- methyl-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H3 receptor
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | SK-N-MC |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.50 | 9.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18661 | IMMEPIP | — | 1 | 9.32 |
| CHEMBL153051 | — | — | 1 | 8.85 |
| CHEMBL153061 | — | — | 1 | 8.44 |
| CHEMBL152936 | — | — | 1 | 8.40 |
| CHEMBL90019 | IMBUTAMINE | — | 1 | 8.39 |
| CHEMBL268229 | — | — | 1 | 8.36 |
| CHEMBL78498 | — | — | 1 | 8.35 |
| CHEMBL417096 | IMPENTAMINE | — | 1 | 8.29 |
| CHEMBL440730 | — | — | 1 | 8.28 |
| CHEMBL356666 | — | — | 1 | 8.23 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 8.03 |
| CHEMBL13795 | VUF-5297 | — | 1 | 8.03 |
| CHEMBL554031 | — | — | 1 | 8.00 |
| CHEMBL150701 | — | — | 1 | 7.70 |
| CHEMBL153284 | — | — | 1 | 7.45 |
| CHEMBL91353 | HOMOHISTAMINE | — | 1 | 7.31 |
| CHEMBL13559 | VUF-5296 | — | 1 | 7.17 |
| CHEMBL151467 | — | — | 1 | 7.17 |
| CHEMBL154529 | — | — | 1 | 7.08 |
| CHEMBL152948 | — | — | 1 | 7.03 |
| CHEMBL153207 | — | — | 1 | 6.74 |
| CHEMBL358028 | — | — | 1 | 6.06 |
| CHEMBL150703 | — | — | 1 | 5.94 |
| CHEMBL150512 | — | — | 1 | 5.55 |
| CHEMBL345954 | — | — | 1 | 5.41 |
| CHEMBL150243 | — | — | 1 | 5.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18661 | IMMEPIP | Ki | = | 0.4786 | nM | 9.32 |
| CHEMBL153051 | — | Ki | = | 1.413 | nM | 8.85 |
| CHEMBL153061 | — | Ki | = | 3.631 | nM | 8.44 |
| CHEMBL152936 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL90019 | IMBUTAMINE | Ki | = | 4.074 | nM | 8.39 |
| CHEMBL268229 | — | Ki | = | 4.365 | nM | 8.36 |
| CHEMBL78498 | — | Ki | = | 4.467 | nM | 8.35 |
| CHEMBL417096 | IMPENTAMINE | Ki | = | 5.129 | nM | 8.29 |
| CHEMBL440730 | — | Ki | = | 5.248 | nM | 8.28 |
| CHEMBL356666 | — | Ki | = | 5.888 | nM | 8.23 |
| CHEMBL90 | HISTAMINE | Ki | = | 9.333 | nM | 8.03 |
| CHEMBL13795 | VUF-5297 | Ki | = | 9.333 | nM | 8.03 |
| CHEMBL554031 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL150701 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL153284 | — | Ki | = | 35.48 | nM | 7.45 |
| CHEMBL91353 | HOMOHISTAMINE | Ki | = | 48.98 | nM | 7.31 |
| CHEMBL13559 | VUF-5296 | Ki | = | 67.61 | nM | 7.17 |
| CHEMBL151467 | — | Ki | = | 67.61 | nM | 7.17 |
| CHEMBL154529 | — | Ki | = | 83.18 | nM | 7.08 |
| CHEMBL152948 | — | Ki | = | 93.33 | nM | 7.03 |
| CHEMBL153207 | — | Ki | = | 181.97 | nM | 6.74 |
| CHEMBL358028 | — | Ki | = | 870.96 | nM | 6.06 |
| CHEMBL150703 | — | Ki | = | 1148.15 | nM | 5.94 |
| CHEMBL150512 | — | Ki | = | 2818.38 | nM | 5.55 |
| CHEMBL345954 | — | Ki | = | 3890.45 | nM | 5.41 |
| CHEMBL150243 | — | Ki | = | 4265.8 | nM | 5.37 |