Assay Detail
Binding
CHEMBL649248
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Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 | 6.43 | 7.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL327931 | — | — | 1 | 7.32 |
| CHEMBL91022 | — | — | 1 | 7.09 |
| CHEMBL327712 | — | — | 1 | 6.80 |
| CHEMBL279436 | — | — | 3 | 6.78 |
| CHEMBL91550 | — | — | 1 | 6.72 |
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 6.65 |
| CHEMBL88448 | — | — | 1 | 6.61 |
| CHEMBL91956 | — | — | 1 | 6.61 |
| CHEMBL284470 | — | — | 1 | 6.55 |
| CHEMBL284103 | — | — | 1 | 6.49 |
| CHEMBL5483012 | — | — | 1 | 6.43 |
| CHEMBL89685 | — | — | 1 | 6.43 |
| CHEMBL313160 | — | — | 1 | 6.40 |
| CHEMBL88388 | — | — | 1 | 6.39 |
| CHEMBL315914 | — | — | 1 | 6.38 |
| CHEMBL313953 | — | — | 1 | 6.37 |
| CHEMBL327775 | — | — | 1 | 6.32 |
| CHEMBL91415 | — | — | 1 | 6.24 |
| CHEMBL92322 | — | — | 1 | 6.20 |
| CHEMBL312871 | — | — | 1 | 6.14 |
| CHEMBL313251 | — | — | 1 | 6.11 |
| CHEMBL315392 | — | — | 1 | 6.09 |
| CHEMBL89243 | — | — | 1 | 6.06 |
| CHEMBL314960 | — | — | 1 | 6.00 |
| CHEMBL88628 | — | — | 1 | 5.99 |
| CHEMBL315538 | — | — | 1 | 5.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL327931 | — | Ki | = | 47.86 | nM | 7.32 |
| CHEMBL91022 | — | Ki | = | 81.28 | nM | 7.09 |
| CHEMBL327712 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL279436 | — | Ki | = | 165.96 | nM | 6.78 |
| CHEMBL91550 | — | Ki | = | 190.55 | nM | 6.72 |
| CHEMBL611 | TERAZOSIN | Ki | = | 223.87 | nM | 6.65 |
| CHEMBL88448 | — | Ki | = | 245.47 | nM | 6.61 |
| CHEMBL91956 | — | Ki | = | 245.47 | nM | 6.61 |
| CHEMBL284470 | — | Ki | = | 281.84 | nM | 6.55 |
| CHEMBL279436 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL279436 | — | Ki | = | 323.59 | nM | 6.49 |
| CHEMBL284103 | — | Ki | = | 323.59 | nM | 6.49 |
| CHEMBL5483012 | — | Ki | = | 371.54 | nM | 6.43 |
| CHEMBL89685 | — | Ki | = | 371.54 | nM | 6.43 |
| CHEMBL313160 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL88388 | — | Ki | = | 407.38 | nM | 6.39 |
| CHEMBL315914 | — | Ki | = | 416.87 | nM | 6.38 |
| CHEMBL313953 | — | Ki | = | 426.58 | nM | 6.37 |
| CHEMBL327775 | — | Ki | = | 478.63 | nM | 6.32 |
| CHEMBL91415 | — | Ki | = | 575.44 | nM | 6.24 |
| CHEMBL92322 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL312871 | — | Ki | = | 724.44 | nM | 6.14 |
| CHEMBL313251 | — | Ki | = | 776.25 | nM | 6.11 |
| CHEMBL315392 | — | Ki | = | 812.83 | nM | 6.09 |
| CHEMBL89243 | — | Ki | = | 870.96 | nM | 6.06 |
| CHEMBL314960 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL88628 | — | Ki | = | 1023.29 | nM | 5.99 |
| CHEMBL315538 | — | Ki | = | 1148.15 | nM | 5.94 |