Assay Detail
Binding
CHEMBL886091
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Binding affinity at human histamine H3 receptor
28
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and biological evaluation of diamine-based histamine H3 antagonists with serotonin reuptake inhibitor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 8.77 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL246126 | — | — | 1 | 9.70 |
| CHEMBL438490 | — | — | 2 | 9.22 |
| CHEMBL245307 | — | — | 1 | 9.15 |
| CHEMBL245516 | — | — | 1 | 9.15 |
| CHEMBL245715 | — | — | 1 | 9.15 |
| CHEMBL245308 | — | — | 1 | 9.10 |
| CHEMBL245309 | — | — | 1 | 9.10 |
| CHEMBL245920 | — | — | 3 | 9.05 |
| CHEMBL245919 | — | — | 2 | 9.05 |
| CHEMBL246125 | — | — | 1 | 9.05 |
| CHEMBL394321 | — | — | 1 | 9.05 |
| CHEMBL394322 | — | — | 1 | 9.00 |
| CHEMBL248377 | — | — | 1 | 9.00 |
| CHEMBL245714 | — | — | 1 | 9.00 |
| CHEMBL245921 | — | — | 1 | 9.00 |
| CHEMBL245515 | — | — | 1 | 8.89 |
| CHEMBL391193 | — | — | 1 | 8.77 |
| CHEMBL245716 | — | — | 1 | 8.77 |
| CHEMBL393071 | — | — | 1 | 8.64 |
| CHEMBL248375 | — | — | 1 | 8.57 |
| CHEMBL248376 | — | — | 1 | 8.48 |
| CHEMBL2447963 | — | — | 1 | 8.37 |
| CHEMBL245514 | — | — | 1 | 8.30 |
| CHEMBL198298 | — | — | 1 | 5.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL246126 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL438490 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL438490 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL245307 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL245516 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL245715 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL245308 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL245309 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL246125 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL245920 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL394321 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL245919 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL245919 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL248377 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL245921 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL245714 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL394322 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL245515 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL245716 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL391193 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL393071 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL248375 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL248376 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL245920 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2447963 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL245514 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL245920 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL198298 | — | Ki | = | 6633.0 | nM | 5.18 |