Assay Detail
Functional
CHEMBL860283
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
29
Total Activities
29
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SK-N-MC |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 28 | 7.54 | 8.20 |
| pA2 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129436 | — | — | 1 | 8.20 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 8.10 |
| CHEMBL340740 | — | — | 1 | 8.10 |
| CHEMBL129540 | — | — | 1 | 8.10 |
| CHEMBL338937 | — | — | 1 | 8.00 |
| CHEMBL364400 | — | — | 1 | 7.90 |
| CHEMBL128613 | — | — | 1 | 7.80 |
| CHEMBL120591 | — | — | 1 | 7.80 |
| CHEMBL268525 | — | — | 1 | 7.70 |
| CHEMBL185951 | — | — | 1 | 7.70 |
| CHEMBL199062 | — | — | 1 | 7.70 |
| CHEMBL129444 | — | — | 1 | 7.70 |
| CHEMBL128088 | — | — | 1 | 7.70 |
| CHEMBL436381 | — | — | 1 | 7.70 |
| CHEMBL383384 | — | — | 1 | 7.60 |
| CHEMBL129026 | — | — | 1 | 7.50 |
| CHEMBL199231 | — | — | 1 | 7.50 |
| CHEMBL129199 | — | — | 1 | 7.40 |
| CHEMBL187285 | — | — | 1 | 7.30 |
| CHEMBL370135 | — | — | 1 | 7.30 |
| CHEMBL333220 | — | — | 1 | 7.30 |
| CHEMBL382276 | — | — | 1 | 7.20 |
| CHEMBL338972 | — | — | 1 | 7.10 |
| CHEMBL338051 | — | — | 1 | 7.10 |
| CHEMBL128958 | — | — | 1 | 7.10 |
| CHEMBL120854 | — | — | 1 | 6.90 |
| CHEMBL128252 | — | — | 1 | 6.90 |
| CHEMBL128505 | — | — | 1 | 6.80 |
| CHEMBL129488 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129436 | — | Kd | = | 6.31 | nM | 8.20 |
| CHEMBL129198 | JNJ-7777120 | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL340740 | — | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL129540 | — | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL338937 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL364400 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL128613 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL120591 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL268525 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL185951 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL199062 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL129444 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL128088 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL436381 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL383384 | — | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL129026 | — | Kd | = | 31.62 | nM | 7.50 |
| CHEMBL199231 | — | Kd | = | 31.62 | nM | 7.50 |
| CHEMBL129199 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL187285 | — | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL370135 | — | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL333220 | — | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL382276 | — | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL338972 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL338051 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL128958 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL120854 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL128252 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL128505 | — | Kd | = | 158.49 | nM | 6.80 |
| CHEMBL129488 | — | pA2 | = | 7.9 | nM | - |