Assay Detail
Functional
CHEMBL3789140
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of N'-(arylsulfonyl)pyrazoline-1-carboxamidines by exploiting a novel interaction site in the 5-HT6 antagonistic binding pocket.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 32 | 8.06 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3785512 | — | — | 1 | 10.30 |
| CHEMBL3785100 | — | — | 1 | 9.50 |
| CHEMBL3786752 | — | — | 1 | 9.10 |
| CHEMBL3785453 | — | — | 1 | 9.00 |
| CHEMBL3787525 | — | — | 1 | 8.80 |
| CHEMBL3785231 | — | — | 1 | 8.60 |
| CHEMBL3787201 | — | — | 1 | 8.50 |
| CHEMBL3786973 | — | — | 1 | 8.40 |
| CHEMBL3785626 | — | — | 1 | 8.40 |
| CHEMBL3786693 | — | — | 1 | 8.30 |
| CHEMBL3787508 | — | — | 1 | 8.30 |
| CHEMBL1834226 | — | — | 1 | 8.30 |
| CHEMBL3785259 | — | — | 1 | 8.10 |
| CHEMBL3785431 | — | — | 1 | 8.00 |
| CHEMBL3787014 | — | — | 1 | 8.00 |
| CHEMBL3786087 | — | — | 1 | 7.90 |
| CHEMBL1834345 | — | — | 1 | 7.80 |
| CHEMBL1834225 | — | — | 1 | 7.80 |
| CHEMBL1834234 | — | — | 1 | 7.70 |
| CHEMBL3785864 | — | — | 1 | 7.60 |
| CHEMBL1834352 | — | — | 1 | 7.20 |
| CHEMBL3786703 | — | — | 1 | 7.20 |
| CHEMBL3787246 | — | — | 1 | 7.10 |
| CHEMBL3786563 | — | — | 1 | 7.00 |
| CHEMBL3785278 | — | — | 1 | 6.90 |
| CHEMBL3787388 | — | — | 1 | 5.80 |
| CHEMBL3785894 | — | — | 1 | - |
| CHEMBL3786951 | — | — | 1 | - |
| CHEMBL3786432 | — | — | 1 | - |
| CHEMBL3785105 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3785512 | — | Kd | = | 0.05012 | nM | 10.30 |
| CHEMBL3785100 | — | Kd | = | 0.3162 | nM | 9.50 |
| CHEMBL3786752 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL3785453 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL3787525 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL3785231 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL3787201 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL3786973 | — | Kd | = | 3.981 | nM | 8.40 |
| CHEMBL3785626 | — | Kd | = | 3.981 | nM | 8.40 |
| CHEMBL3786693 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL3787508 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL1834226 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL3785259 | — | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL3785431 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL3787014 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL3786087 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL1834345 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL1834225 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL1834234 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL3785864 | — | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL1834352 | — | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL3786703 | — | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL3787246 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL3786563 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL3785278 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL3787388 | — | Kd | = | 1584.89 | nM | 5.80 |
| CHEMBL3785894 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL3786951 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL3786432 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL3785105 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL3786071 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL3785853 | — | Kd | > | 1000.0 | nM | - |