Assay Detail
Functional
CHEMBL691452
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonism of the human histamine H1 receptor
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and sar of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/tachykinin NK1 receptor antagonist activity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.32 | 6.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL330430 | — | — | 1 | 6.91 |
| CHEMBL330367 | — | — | 1 | 6.80 |
| CHEMBL317524 | — | — | 1 | 6.69 |
| CHEMBL431458 | — | — | 1 | 6.63 |
| CHEMBL327497 | — | — | 1 | 6.62 |
| CHEMBL330719 | — | — | 1 | 6.54 |
| CHEMBL95127 | — | — | 1 | 6.53 |
| CHEMBL93556 | — | — | 1 | 6.51 |
| CHEMBL96442 | — | — | 1 | 6.44 |
| CHEMBL322194 | — | — | 1 | 6.42 |
| CHEMBL330172 | — | — | 1 | 6.38 |
| CHEMBL431850 | — | — | 1 | 6.36 |
| CHEMBL264007 | — | — | 1 | 6.36 |
| CHEMBL329450 | — | — | 1 | 6.35 |
| CHEMBL94834 | — | — | 1 | 6.33 |
| CHEMBL330499 | — | — | 1 | 6.30 |
| CHEMBL410270 | — | — | 1 | 6.30 |
| CHEMBL17157 | TERFENADINE | 4.0 | 1 | 6.25 |
| CHEMBL316705 | — | — | 1 | 6.00 |
| CHEMBL328511 | — | — | 1 | 5.92 |
| CHEMBL537027 | — | — | 1 | 5.47 |
| CHEMBL542908 | — | — | 1 | 5.03 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | - |
| CHEMBL16192 | CP-96345 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL330430 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL330367 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL317524 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL431458 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL327497 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL330719 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL95127 | — | IC50 | = | 293.0 | nM | 6.53 |
| CHEMBL93556 | — | IC50 | = | 309.0 | nM | 6.51 |
| CHEMBL96442 | — | IC50 | = | 366.0 | nM | 6.44 |
| CHEMBL322194 | — | IC50 | = | 381.0 | nM | 6.42 |
| CHEMBL330172 | — | IC50 | = | 416.0 | nM | 6.38 |
| CHEMBL431850 | — | IC50 | = | 437.0 | nM | 6.36 |
| CHEMBL264007 | — | IC50 | = | 436.0 | nM | 6.36 |
| CHEMBL329450 | — | IC50 | = | 446.0 | nM | 6.35 |
| CHEMBL94834 | — | IC50 | = | 473.0 | nM | 6.33 |
| CHEMBL330499 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL410270 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL17157 | TERFENADINE | IC50 | = | 563.0 | nM | 6.25 |
| CHEMBL316705 | — | IC50 | = | 994.0 | nM | 6.00 |
| CHEMBL328511 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL537027 | — | IC50 | = | 3420.0 | nM | 5.47 |
| CHEMBL542908 | — | IC50 | = | 9447.0 | nM | 5.03 |
| CHEMBL90 | HISTAMINE | IC50 | ~ | 1000.0 | nM | - |
| CHEMBL16192 | CP-96345 | IC50 | ~ | 10000.0 | nM | - |