Assay Detail
Functional
CHEMBL695771
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist potency against human histamine H3 receptor expressed in CHO cells was determined by GTPgamma-S-assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 8.19 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1204309 | — | — | 1 | 9.42 |
| CHEMBL1202893 | — | — | 1 | 9.37 |
| CHEMBL2447986 | — | — | 1 | 9.27 |
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 9.24 |
| CHEMBL1202892 | — | — | 1 | 9.13 |
| CHEMBL2447955 | — | — | 1 | 9.07 |
| CHEMBL1202896 | — | — | 1 | 9.02 |
| CHEMBL2447983 | — | — | 1 | 8.92 |
| CHEMBL2447956 | — | — | 1 | 8.92 |
| CHEMBL2447995 | — | — | 1 | 8.92 |
| CHEMBL1202903 | — | — | 1 | 8.85 |
| CHEMBL1202904 | — | — | 1 | 8.82 |
| CHEMBL1202901 | — | — | 1 | 8.64 |
| CHEMBL1202900 | — | — | 1 | 8.59 |
| CHEMBL1202894 | — | — | 1 | 8.57 |
| CHEMBL268229 | — | — | 1 | 8.57 |
| CHEMBL1202899 | — | — | 1 | 8.54 |
| CHEMBL2447989 | — | — | 1 | 8.44 |
| CHEMBL2447992 | — | — | 1 | 8.36 |
| CHEMBL2447991 | — | — | 1 | 8.08 |
| CHEMBL1202902 | — | — | 1 | 8.07 |
| CHEMBL2447993 | — | — | 1 | 8.04 |
| CHEMBL2447988 | — | — | 1 | 7.88 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 7.85 |
| CHEMBL1202897 | — | — | 1 | 7.62 |
| CHEMBL2447994 | — | — | 1 | 7.47 |
| CHEMBL2447985 | — | — | 1 | 7.05 |
| CHEMBL1202895 | — | — | 1 | 7.03 |
| CHEMBL14638 | CIPROXIFAN | — | 1 | 7.03 |
| CHEMBL1202898 | — | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1204309 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL1202893 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL2447986 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL1202892 | — | Ki | = | 0.74 | nM | 9.13 |
| CHEMBL2447955 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL1202896 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL2447983 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2447956 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2447995 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL1202903 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL1202904 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1202901 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL1202900 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL268229 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL1202894 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL1202899 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL2447989 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL2447992 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL2447991 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL1202902 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL2447993 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL2447988 | — | Ki | = | 13.3 | nM | 7.88 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1202897 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL2447994 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL2447985 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL1202895 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL14638 | CIPROXIFAN | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL1202898 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL2447990 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL2447987 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL2447984 | — | Ki | = | 1100.0 | nM | 5.96 |