Assay Detail
Binding
CHEMBL645109
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Binding affinity determined by displacement of [3H]rauwolscine from alpha-2B adrenergic receptor
28
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 6.31 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 7.51 |
| CHEMBL327931 | — | — | 1 | 7.04 |
| CHEMBL313251 | — | — | 1 | 6.70 |
| CHEMBL312871 | — | — | 1 | 6.69 |
| CHEMBL91022 | — | — | 1 | 6.66 |
| CHEMBL91550 | — | — | 1 | 6.59 |
| CHEMBL279436 | — | — | 3 | 6.55 |
| CHEMBL284470 | — | — | 1 | 6.43 |
| CHEMBL88388 | — | — | 1 | 6.42 |
| CHEMBL313953 | — | — | 1 | 6.42 |
| CHEMBL89685 | — | — | 1 | 6.36 |
| CHEMBL88448 | — | — | 1 | 6.31 |
| CHEMBL91956 | — | — | 1 | 6.29 |
| CHEMBL88628 | — | — | 1 | 6.24 |
| CHEMBL313160 | — | — | 1 | 6.24 |
| CHEMBL5483012 | — | — | 1 | 6.10 |
| CHEMBL327775 | — | — | 1 | 6.08 |
| CHEMBL91415 | — | — | 1 | 6.06 |
| CHEMBL92322 | — | — | 1 | 6.05 |
| CHEMBL315914 | — | — | 1 | 6.04 |
| CHEMBL284103 | — | — | 1 | 6.03 |
| CHEMBL327712 | — | — | 1 | 5.90 |
| CHEMBL89243 | — | — | 1 | 5.90 |
| CHEMBL315538 | — | — | 1 | 5.82 |
| CHEMBL315392 | — | — | 1 | 5.74 |
| CHEMBL314960 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL611 | TERAZOSIN | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL327931 | — | Ki | = | 91.2 | nM | 7.04 |
| CHEMBL313251 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL312871 | — | Ki | = | 204.17 | nM | 6.69 |
| CHEMBL91022 | — | Ki | = | 218.78 | nM | 6.66 |
| CHEMBL91550 | — | Ki | = | 257.04 | nM | 6.59 |
| CHEMBL279436 | — | Ki | = | 281.84 | nM | 6.55 |
| CHEMBL284470 | — | Ki | = | 371.54 | nM | 6.43 |
| CHEMBL88388 | — | Ki | = | 380.19 | nM | 6.42 |
| CHEMBL313953 | — | Ki | = | 380.19 | nM | 6.42 |
| CHEMBL279436 | — | Ki | = | 407.38 | nM | 6.39 |
| CHEMBL279436 | — | Ki | = | 416.87 | nM | 6.38 |
| CHEMBL89685 | — | Ki | = | 436.52 | nM | 6.36 |
| CHEMBL88448 | — | Ki | = | 489.78 | nM | 6.31 |
| CHEMBL91956 | — | Ki | = | 512.86 | nM | 6.29 |
| CHEMBL88628 | — | Ki | = | 575.44 | nM | 6.24 |
| CHEMBL313160 | — | Ki | = | 575.44 | nM | 6.24 |
| CHEMBL5483012 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL327775 | — | Ki | = | 831.76 | nM | 6.08 |
| CHEMBL91415 | — | Ki | = | 870.96 | nM | 6.06 |
| CHEMBL92322 | — | Ki | = | 891.25 | nM | 6.05 |
| CHEMBL315914 | — | Ki | = | 912.01 | nM | 6.04 |
| CHEMBL284103 | — | Ki | = | 933.25 | nM | 6.03 |
| CHEMBL327712 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL89243 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL315538 | — | Ki | = | 1513.56 | nM | 5.82 |
| CHEMBL315392 | — | Ki | = | 1819.7 | nM | 5.74 |
| CHEMBL314960 | — | Ki | = | 2290.87 | nM | 5.64 |