Assay Detail
Binding
CHEMBL838642
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Inhibitory constant for human cloned 5-HT4 receptor
24
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 | Expert |
Publication
Identification of a 5-HT4 receptor antagonist clinical candidate through side-chain modification.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 10.01 | 10.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL180835 | — | — | 1 | 10.80 |
| CHEMBL181202 | — | — | 1 | 10.60 |
| CHEMBL361118 | — | — | 1 | 10.60 |
| CHEMBL367354 | — | — | 1 | 10.50 |
| CHEMBL182999 | — | — | 1 | 10.50 |
| CHEMBL181126 | — | — | 1 | 10.50 |
| CHEMBL180680 | — | — | 1 | 10.30 |
| CHEMBL424790 | — | — | 1 | 10.30 |
| CHEMBL180201 | — | — | 1 | 10.20 |
| CHEMBL360449 | — | — | 1 | 10.10 |
| CHEMBL360245 | — | — | 1 | 10.00 |
| CHEMBL180830 | — | — | 1 | 10.00 |
| CHEMBL178669 | — | — | 1 | 9.90 |
| CHEMBL179833 | — | — | 1 | 9.90 |
| CHEMBL178285 | — | — | 1 | 9.90 |
| CHEMBL180697 | — | — | 1 | 9.80 |
| CHEMBL181415 | — | — | 1 | 9.80 |
| CHEMBL181928 | — | — | 1 | 9.70 |
| CHEMBL180632 | — | — | 1 | 9.60 |
| CHEMBL356359 | PIBOSEROD | 2.0 | 1 | 9.60 |
| CHEMBL360531 | — | — | 1 | 9.60 |
| CHEMBL179799 | — | — | 1 | 9.50 |
| CHEMBL362582 | — | — | 1 | 9.40 |
| CHEMBL182590 | — | — | 1 | 9.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL180835 | — | Ki | = | 0.01585 | nM | 10.80 |
| CHEMBL181202 | — | Ki | = | 0.02512 | nM | 10.60 |
| CHEMBL361118 | — | Ki | = | 0.02512 | nM | 10.60 |
| CHEMBL367354 | — | Ki | = | 0.03162 | nM | 10.50 |
| CHEMBL182999 | — | Ki | = | 0.03162 | nM | 10.50 |
| CHEMBL181126 | — | Ki | = | 0.03162 | nM | 10.50 |
| CHEMBL180680 | — | Ki | = | 0.05012 | nM | 10.30 |
| CHEMBL424790 | — | Ki | = | 0.05012 | nM | 10.30 |
| CHEMBL180201 | — | Ki | = | 0.0631 | nM | 10.20 |
| CHEMBL360449 | — | Ki | = | 0.07943 | nM | 10.10 |
| CHEMBL360245 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL180830 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL178669 | — | Ki | = | 0.1259 | nM | 9.90 |
| CHEMBL179833 | — | Ki | = | 0.1259 | nM | 9.90 |
| CHEMBL178285 | — | Ki | = | 0.1259 | nM | 9.90 |
| CHEMBL180697 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL181415 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL181928 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL180632 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL356359 | PIBOSEROD | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL360531 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL179799 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL362582 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL182590 | — | Ki | = | 0.7943 | nM | 9.10 |