Assay Detail
Binding
CHEMBL696446
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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 H4 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 | 6.24 | 7.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 7.26 |
| CHEMBL18661 | IMMEPIP | — | 1 | 7.25 |
| CHEMBL90019 | IMBUTAMINE | — | 1 | 7.05 |
| CHEMBL91353 | HOMOHISTAMINE | — | 1 | 6.67 |
| CHEMBL440730 | — | — | 1 | 6.38 |
| CHEMBL153061 | — | — | 1 | 6.13 |
| CHEMBL153051 | — | — | 1 | 5.99 |
| CHEMBL153284 | — | — | 1 | 5.96 |
| CHEMBL268229 | — | — | 1 | 5.95 |
| CHEMBL153207 | — | — | 1 | 5.69 |
| CHEMBL151467 | — | — | 1 | 5.40 |
| CHEMBL13795 | VUF-5297 | — | 1 | 5.15 |
| CHEMBL152936 | — | — | 1 | - |
| CHEMBL150701 | — | — | 1 | - |
| CHEMBL13559 | VUF-5296 | — | 1 | - |
| CHEMBL154529 | — | — | 1 | - |
| CHEMBL152948 | — | — | 1 | - |
| CHEMBL356666 | — | — | 1 | - |
| CHEMBL345954 | — | — | 1 | - |
| CHEMBL417096 | IMPENTAMINE | — | 1 | - |
| CHEMBL150703 | — | — | 1 | - |
| CHEMBL150243 | — | — | 1 | - |
| CHEMBL358028 | — | — | 1 | - |
| CHEMBL150512 | — | — | 1 | - |
| CHEMBL554031 | — | — | 1 | - |
| CHEMBL78498 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL90 | HISTAMINE | EC50 | = | 54.95 | nM | 7.26 |
| CHEMBL18661 | IMMEPIP | EC50 | = | 56.23 | nM | 7.25 |
| CHEMBL90019 | IMBUTAMINE | EC50 | = | 89.13 | nM | 7.05 |
| CHEMBL91353 | HOMOHISTAMINE | EC50 | = | 213.8 | nM | 6.67 |
| CHEMBL440730 | — | EC50 | = | 416.87 | nM | 6.38 |
| CHEMBL153061 | — | EC50 | = | 741.31 | nM | 6.13 |
| CHEMBL153051 | — | EC50 | = | 1023.29 | nM | 5.99 |
| CHEMBL153284 | — | EC50 | = | 1096.48 | nM | 5.96 |
| CHEMBL268229 | — | EC50 | = | 1122.02 | nM | 5.95 |
| CHEMBL153207 | — | EC50 | = | 2041.74 | nM | 5.69 |
| CHEMBL151467 | — | EC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL13795 | VUF-5297 | EC50 | = | 7079.46 | nM | 5.15 |
| CHEMBL152936 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL150701 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL13559 | VUF-5296 | EC50 | < | 10000.0 | nM | - |
| CHEMBL154529 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL152948 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL356666 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL345954 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL417096 | IMPENTAMINE | EC50 | < | 10000.0 | nM | - |
| CHEMBL150703 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL150243 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL358028 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL150512 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL554031 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL78498 | — | EC50 | < | 10000.0 | nM | - |