Assay Detail
Binding
CHEMBL3801620
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 7-methoxy-[3H]-prazosin from human alpha1D adrenergic receptor expressed in CHO-K1 cell membranes incubated for 60 mins by liquid scintillation counting analysis
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Active α1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 7.71 | 9.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3798124 | — | — | 1 | 9.18 |
| CHEMBL3800606 | — | — | 1 | 9.07 |
| CHEMBL3799553 | — | — | 1 | 8.96 |
| CHEMBL3799292 | (R)-9s | — | 1 | 8.80 |
| CHEMBL3800305 | — | — | 1 | 8.59 |
| CHEMBL3800470 | — | — | 1 | 8.47 |
| CHEMBL3799912 | — | — | 1 | 8.43 |
| CHEMBL3800506 | — | — | 1 | 8.32 |
| CHEMBL3799420 | — | — | 1 | 8.12 |
| CHEMBL3799166 | — | — | 1 | 8.07 |
| CHEMBL3799089 | — | — | 1 | 8.06 |
| CHEMBL3799869 | — | — | 1 | 8.03 |
| CHEMBL3798655 | — | — | 1 | 8.00 |
| CHEMBL3799115 | — | — | 1 | 7.96 |
| CHEMBL3800449 | — | — | 1 | 7.82 |
| CHEMBL3800219 | — | — | 1 | 7.80 |
| CHEMBL3797369 | — | — | 1 | 7.64 |
| CHEMBL3799486 | — | — | 1 | 7.58 |
| CHEMBL3797529 | — | — | 1 | 7.52 |
| CHEMBL3799219 | — | — | 1 | 7.41 |
| CHEMBL3799783 | — | — | 1 | 7.28 |
| CHEMBL3799155 | — | — | 1 | 7.27 |
| CHEMBL3798527 | — | — | 1 | 7.19 |
| CHEMBL3797887 | (S)-9s | — | 1 | 6.89 |
| CHEMBL3798506 | — | — | 1 | 6.80 |
| CHEMBL3797500 | — | — | 1 | 6.80 |
| CHEMBL3799335 | — | — | 1 | 6.60 |
| CHEMBL3800485 | — | — | 1 | 6.38 |
| CHEMBL3797685 | — | — | 1 | 6.09 |
| CHEMBL3799440 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3798124 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL3800606 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL3799553 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3799292 | (R)-9s | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL3800305 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL3800470 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL3799912 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL3800506 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL3799420 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL3799166 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL3799089 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL3799869 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL3798655 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3799115 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3800449 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3800219 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL3797369 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL3799486 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL3797529 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL3799219 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL3799783 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL3799155 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL3798527 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL3797887 | (S)-9s | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL3798506 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL3797500 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL3799335 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL3800485 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL3797685 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL3799440 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL3797464 | — | Ki | > | 940.0 | nM | - |
| CHEMBL3798057 | — | Ki | > | 940.0 | nM | - |
| CHEMBL3797886 | — | Ki | > | 940.0 | nM | - |
| CHEMBL3797382 | — | Ki | > | 940.0 | nM | - |