Assay Detail
Binding
CHEMBL694892
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Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in 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 |
|---|---|---|---|
| EC50 | 26 | 7.66 | 9.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18661 | IMMEPIP | — | 1 | 9.88 |
| CHEMBL153051 | — | — | 1 | 9.41 |
| CHEMBL268229 | — | — | 1 | 9.17 |
| CHEMBL153061 | — | — | 1 | 8.88 |
| CHEMBL440730 | — | — | 1 | 8.68 |
| CHEMBL152936 | — | — | 1 | 8.63 |
| CHEMBL417096 | IMPENTAMINE | — | 1 | 8.63 |
| CHEMBL356666 | — | — | 1 | 8.50 |
| CHEMBL13795 | VUF-5297 | — | 1 | 8.23 |
| CHEMBL90019 | IMBUTAMINE | — | 1 | 8.13 |
| CHEMBL78498 | — | — | 1 | 8.08 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 8.01 |
| CHEMBL150701 | — | — | 1 | 7.88 |
| CHEMBL153284 | — | — | 1 | 7.71 |
| CHEMBL554031 | — | — | 1 | 7.48 |
| CHEMBL91353 | HOMOHISTAMINE | — | 1 | 7.37 |
| CHEMBL151467 | — | — | 1 | 7.31 |
| CHEMBL13559 | VUF-5296 | — | 1 | 7.24 |
| CHEMBL152948 | — | — | 1 | 6.49 |
| CHEMBL153207 | — | — | 1 | 6.29 |
| CHEMBL154529 | — | — | 1 | 6.29 |
| CHEMBL150703 | — | — | 1 | 6.10 |
| CHEMBL150243 | — | — | 1 | 5.82 |
| CHEMBL358028 | — | — | 1 | 5.74 |
| CHEMBL345954 | — | — | 1 | 5.56 |
| CHEMBL150512 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18661 | IMMEPIP | EC50 | = | 0.1318 | nM | 9.88 |
| CHEMBL153051 | — | EC50 | = | 0.389 | nM | 9.41 |
| CHEMBL268229 | — | EC50 | = | 0.6761 | nM | 9.17 |
| CHEMBL153061 | — | EC50 | = | 1.318 | nM | 8.88 |
| CHEMBL440730 | — | EC50 | = | 2.089 | nM | 8.68 |
| CHEMBL152936 | — | EC50 | = | 2.344 | nM | 8.63 |
| CHEMBL417096 | IMPENTAMINE | EC50 | = | 2.344 | nM | 8.63 |
| CHEMBL356666 | — | EC50 | = | 3.162 | nM | 8.50 |
| CHEMBL13795 | VUF-5297 | EC50 | = | 5.888 | nM | 8.23 |
| CHEMBL90019 | IMBUTAMINE | EC50 | = | 7.413 | nM | 8.13 |
| CHEMBL78498 | — | EC50 | = | 8.318 | nM | 8.08 |
| CHEMBL90 | HISTAMINE | EC50 | = | 9.772 | nM | 8.01 |
| CHEMBL150701 | — | EC50 | = | 13.18 | nM | 7.88 |
| CHEMBL153284 | — | EC50 | = | 19.5 | nM | 7.71 |
| CHEMBL554031 | — | EC50 | = | 33.11 | nM | 7.48 |
| CHEMBL91353 | HOMOHISTAMINE | EC50 | = | 42.66 | nM | 7.37 |
| CHEMBL151467 | — | EC50 | = | 48.98 | nM | 7.31 |
| CHEMBL13559 | VUF-5296 | EC50 | = | 57.54 | nM | 7.24 |
| CHEMBL152948 | — | EC50 | = | 323.59 | nM | 6.49 |
| CHEMBL153207 | — | EC50 | = | 512.86 | nM | 6.29 |
| CHEMBL154529 | — | EC50 | = | 512.86 | nM | 6.29 |
| CHEMBL150703 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL150243 | — | EC50 | = | 1513.56 | nM | 5.82 |
| CHEMBL358028 | — | EC50 | = | 1819.7 | nM | 5.74 |
| CHEMBL345954 | — | EC50 | = | 2754.23 | nM | 5.56 |
| CHEMBL150512 | — | EC50 | < | 10000.0 | nM | - |