Assay Detail
Binding
CHEMBL698299
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Displacement of [3H]clonidine from imidazoline receptor I-1 of bovine chromaffin cell membranes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and biological evaluation of pyrrolinic isosteres of rilmenidine. Discovery of cis-/trans-dicyclopropylmethyl-(4,5-dimethyl-4,5-dihydro-3H-pyrrol-2-yl)-amine (LNP 509), an I1 imidazoline receptor selective ligand with hypotensive activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 6.41 | 7.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL289480 | RILMENIDINE | 4.0 | 1 | 7.13 |
| CHEMBL40399 | — | — | 1 | 6.77 |
| CHEMBL288951 | — | — | 1 | 6.29 |
| CHEMBL288139 | — | — | 1 | 6.27 |
| CHEMBL442156 | — | — | 1 | 6.19 |
| CHEMBL40337 | — | — | 1 | 5.80 |
| CHEMBL40393 | — | — | 1 | - |
| CHEMBL40287 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL289480 | RILMENIDINE | Ki | = | 74.13 | nM | 7.13 |
| CHEMBL40399 | — | Ki | = | 169.82 | nM | 6.77 |
| CHEMBL288951 | — | Ki | = | 512.86 | nM | 6.29 |
| CHEMBL288139 | — | Ki | = | 537.03 | nM | 6.27 |
| CHEMBL442156 | — | Ki | = | 645.65 | nM | 6.19 |
| CHEMBL40337 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL40393 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL40287 | — | Ki | < | 10000.0 | nM | - |