Assay Detail
Binding
CHEMBL886090
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Binding affinity at human SERT
27
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 |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 27 | 7.58 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL245919 | — | — | 2 | 8.57 |
| CHEMBL245920 | — | — | 3 | 8.52 |
| CHEMBL245921 | — | — | 1 | 8.40 |
| CHEMBL2447963 | — | — | 1 | 8.14 |
| CHEMBL198298 | — | — | 1 | 8.08 |
| CHEMBL246125 | — | — | 1 | 8.06 |
| CHEMBL391193 | — | — | 1 | 8.05 |
| CHEMBL394321 | — | — | 1 | 8.00 |
| CHEMBL245715 | — | — | 1 | 7.96 |
| CHEMBL248375 | — | — | 1 | 7.85 |
| CHEMBL245716 | — | — | 1 | 7.80 |
| CHEMBL245516 | — | — | 1 | 7.80 |
| CHEMBL438490 | — | — | 1 | 7.58 |
| CHEMBL245515 | — | — | 1 | 7.54 |
| CHEMBL393071 | — | — | 1 | 7.38 |
| CHEMBL394322 | — | — | 1 | 7.34 |
| CHEMBL245714 | — | — | 1 | 7.22 |
| CHEMBL245514 | — | — | 1 | 7.21 |
| CHEMBL246126 | — | — | 1 | 6.80 |
| CHEMBL245308 | — | — | 1 | 6.77 |
| CHEMBL248376 | — | — | 1 | 6.70 |
| CHEMBL245309 | — | — | 1 | 6.61 |
| CHEMBL248377 | — | — | 1 | 6.55 |
| CHEMBL245307 | — | — | 1 | 5.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL245919 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL245920 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL245921 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL245920 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL2447963 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL198298 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL246125 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL391193 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL245920 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL394321 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL245715 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL248375 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL245716 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL245516 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL245919 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL438490 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL245515 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL393071 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL394322 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL245714 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL245514 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL246126 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL245308 | — | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL248376 | — | Ki | = | 199.0 | nM | 6.70 |
| CHEMBL245309 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL248377 | — | Ki | = | 281.0 | nM | 6.55 |
| CHEMBL245307 | — | Ki | = | 1480.0 | nM | 5.83 |