Assay Detail
Binding
CHEMBL643231
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Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A 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 | 6.18 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL327931 | — | — | 1 | 6.96 |
| CHEMBL279436 | — | — | 3 | 6.82 |
| CHEMBL91022 | — | — | 1 | 6.56 |
| CHEMBL91550 | — | — | 1 | 6.45 |
| CHEMBL284103 | — | — | 1 | 6.40 |
| CHEMBL91956 | — | — | 1 | 6.35 |
| CHEMBL312871 | — | — | 1 | 6.30 |
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 6.26 |
| CHEMBL89685 | — | — | 1 | 6.22 |
| CHEMBL313160 | — | — | 1 | 6.20 |
| CHEMBL327775 | — | — | 1 | 6.20 |
| CHEMBL284470 | — | — | 1 | 6.19 |
| CHEMBL313953 | — | — | 1 | 6.17 |
| CHEMBL88448 | — | — | 1 | 6.17 |
| CHEMBL89243 | — | — | 1 | 6.12 |
| CHEMBL327712 | — | — | 1 | 6.04 |
| CHEMBL88388 | — | — | 1 | 6.02 |
| CHEMBL315392 | — | — | 1 | 6.02 |
| CHEMBL91415 | — | — | 1 | 5.95 |
| CHEMBL313251 | — | — | 1 | 5.93 |
| CHEMBL5483012 | — | — | 1 | 5.92 |
| CHEMBL315914 | — | — | 1 | 5.89 |
| CHEMBL92322 | — | — | 1 | 5.80 |
| CHEMBL88628 | — | — | 1 | 5.68 |
| CHEMBL314960 | — | — | 1 | 5.67 |
| CHEMBL315538 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL327931 | — | Ki | = | 109.65 | nM | 6.96 |
| CHEMBL279436 | — | Ki | = | 151.36 | nM | 6.82 |
| CHEMBL91022 | — | Ki | = | 275.42 | nM | 6.56 |
| CHEMBL279436 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL91550 | — | Ki | = | 354.81 | nM | 6.45 |
| CHEMBL279436 | — | Ki | = | 371.54 | nM | 6.43 |
| CHEMBL284103 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL91956 | — | Ki | = | 446.68 | nM | 6.35 |
| CHEMBL312871 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL611 | TERAZOSIN | Ki | = | 549.54 | nM | 6.26 |
| CHEMBL89685 | — | Ki | = | 602.56 | nM | 6.22 |
| CHEMBL313160 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL327775 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL284470 | — | Ki | = | 645.65 | nM | 6.19 |
| CHEMBL88448 | — | Ki | = | 676.08 | nM | 6.17 |
| CHEMBL313953 | — | Ki | = | 676.08 | nM | 6.17 |
| CHEMBL89243 | — | Ki | = | 758.58 | nM | 6.12 |
| CHEMBL327712 | — | Ki | = | 912.01 | nM | 6.04 |
| CHEMBL88388 | — | Ki | = | 954.99 | nM | 6.02 |
| CHEMBL315392 | — | Ki | = | 954.99 | nM | 6.02 |
| CHEMBL91415 | — | Ki | = | 1122.02 | nM | 5.95 |
| CHEMBL313251 | — | Ki | = | 1174.9 | nM | 5.93 |
| CHEMBL5483012 | — | Ki | = | 1202.26 | nM | 5.92 |
| CHEMBL315914 | — | Ki | = | 1288.25 | nM | 5.89 |
| CHEMBL92322 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL88628 | — | Ki | = | 2089.3 | nM | 5.68 |
| CHEMBL314960 | — | Ki | = | 2137.96 | nM | 5.67 |
| CHEMBL315538 | — | Ki | = | 2187.76 | nM | 5.66 |