Assay Detail
Binding
CHEMBL697541
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Binding affinity towards rat cortical H3 receptor
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 48 | 7.73 | 9.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL278462 | CIPRALISANT | 2.0 | 1 | 9.71 |
| CHEMBL280590 | — | — | 1 | 8.99 |
| CHEMBL27979 | A-349,821 | — | 1 | 8.78 |
| CHEMBL283313 | — | — | 1 | 8.69 |
| CHEMBL433031 | — | — | 1 | 8.55 |
| CHEMBL25519 | — | — | 1 | 8.55 |
| CHEMBL24863 | — | — | 1 | 8.53 |
| CHEMBL25205 | — | — | 1 | 8.44 |
| CHEMBL25342 | — | — | 1 | 8.42 |
| CHEMBL27933 | — | — | 1 | 8.38 |
| CHEMBL27501 | — | — | 1 | 8.29 |
| CHEMBL26880 | — | — | 1 | 8.18 |
| CHEMBL279463 | — | — | 1 | 8.14 |
| CHEMBL25685 | — | — | 1 | 8.08 |
| CHEMBL27209 | — | — | 1 | 8.06 |
| CHEMBL27697 | — | — | 1 | 8.05 |
| CHEMBL281640 | — | — | 1 | 8.04 |
| CHEMBL27444 | — | — | 1 | 7.99 |
| CHEMBL27665 | — | — | 1 | 7.89 |
| CHEMBL282903 | — | — | 1 | 7.86 |
| CHEMBL24468 | — | — | 1 | 7.79 |
| CHEMBL436340 | — | — | 1 | 7.76 |
| CHEMBL2113223 | — | — | 1 | 7.73 |
| CHEMBL27115 | — | — | 1 | 7.68 |
| CHEMBL27835 | — | — | 1 | 7.67 |
| CHEMBL25501 | — | — | 1 | 7.59 |
| CHEMBL2113222 | — | — | 1 | 7.56 |
| CHEMBL280895 | — | — | 1 | 7.55 |
| CHEMBL282685 | — | — | 1 | 7.54 |
| CHEMBL2113224 | — | — | 1 | 7.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL278462 | CIPRALISANT | Ki | = | 0.195 | nM | 9.71 |
| CHEMBL280590 | — | Ki | = | 1.023 | nM | 8.99 |
| CHEMBL27979 | A-349,821 | Ki | = | 1.66 | nM | 8.78 |
| CHEMBL283313 | — | Ki | = | 2.042 | nM | 8.69 |
| CHEMBL433031 | — | Ki | = | 2.818 | nM | 8.55 |
| CHEMBL25519 | — | Ki | = | 2.818 | nM | 8.55 |
| CHEMBL24863 | — | Ki | = | 2.951 | nM | 8.53 |
| CHEMBL25205 | — | Ki | = | 3.631 | nM | 8.44 |
| CHEMBL25342 | — | Ki | = | 3.802 | nM | 8.42 |
| CHEMBL27933 | — | Ki | = | 4.169 | nM | 8.38 |
| CHEMBL27501 | — | Ki | = | 5.129 | nM | 8.29 |
| CHEMBL26880 | — | Ki | = | 6.607 | nM | 8.18 |
| CHEMBL279463 | — | Ki | = | 7.244 | nM | 8.14 |
| CHEMBL25685 | — | Ki | = | 8.318 | nM | 8.08 |
| CHEMBL27209 | — | Ki | = | 8.71 | nM | 8.06 |
| CHEMBL27697 | — | Ki | = | 8.913 | nM | 8.05 |
| CHEMBL281640 | — | Ki | = | 9.12 | nM | 8.04 |
| CHEMBL27444 | — | Ki | = | 10.23 | nM | 7.99 |
| CHEMBL27665 | — | Ki | = | 12.88 | nM | 7.89 |
| CHEMBL282903 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL24468 | — | Ki | = | 16.22 | nM | 7.79 |
| CHEMBL436340 | — | Ki | = | 17.38 | nM | 7.76 |
| CHEMBL2113223 | — | Ki | = | 18.62 | nM | 7.73 |
| CHEMBL27115 | — | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL27835 | — | Ki | = | 21.38 | nM | 7.67 |
| CHEMBL25501 | — | Ki | = | 25.7 | nM | 7.59 |
| CHEMBL2113222 | — | Ki | = | 27.54 | nM | 7.56 |
| CHEMBL280895 | — | Ki | = | 28.18 | nM | 7.55 |
| CHEMBL282685 | — | Ki | = | 28.84 | nM | 7.54 |
| CHEMBL2113224 | — | Ki | = | 29.51 | nM | 7.53 |
| CHEMBL24865 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL24198 | — | Ki | = | 32.36 | nM | 7.49 |
| CHEMBL27339 | — | Ki | = | 33.11 | nM | 7.48 |
| CHEMBL25688 | — | Ki | = | 41.69 | nM | 7.38 |
| CHEMBL282062 | — | Ki | = | 42.66 | nM | 7.37 |
| CHEMBL24921 | — | Ki | = | 42.66 | nM | 7.37 |
| CHEMBL24847 | — | Ki | = | 52.48 | nM | 7.28 |
| CHEMBL282016 | — | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL27545 | — | Ki | = | 70.79 | nM | 7.15 |
| CHEMBL24352 | — | Ki | = | 97.72 | nM | 7.01 |
| CHEMBL28271 | — | Ki | = | 112.2 | nM | 6.95 |
| CHEMBL25126 | — | Ki | = | 114.82 | nM | 6.94 |
| CHEMBL24126 | — | Ki | = | 128.82 | nM | 6.89 |
| CHEMBL27343 | — | Ki | = | 134.9 | nM | 6.87 |
| CHEMBL281287 | — | Ki | = | 177.83 | nM | 6.75 |
| CHEMBL25290 | — | Ki | = | 218.78 | nM | 6.66 |
| CHEMBL284320 | — | Ki | = | 407.38 | nM | 6.39 |
| CHEMBL283451 | — | Ki | = | 478.63 | nM | 6.32 |