Assay Detail
Binding
CHEMBL1647664
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Inhibition of ROCK-1 by Immobilized metal ion affinity-based fluorescence polarization assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Fragment-based discovery of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 5.87 | 6.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1643573 | — | — | 1 | 6.62 |
| CHEMBL1643574 | — | — | 1 | 6.62 |
| CHEMBL1643356 | — | — | 1 | 6.37 |
| CHEMBL1643365 | — | — | 1 | 6.24 |
| CHEMBL1643357 | — | — | 1 | 6.23 |
| CHEMBL1233300 | HYDROXYFASUDIL | — | 1 | 6.12 |
| CHEMBL1643358 | — | — | 1 | 6.11 |
| CHEMBL1643359 | — | — | 1 | 6.09 |
| CHEMBL559147 | Y-27632 | — | 1 | 6.06 |
| CHEMBL1643360 | — | — | 1 | 6.00 |
| CHEMBL1643361 | — | — | 1 | 5.89 |
| CHEMBL1643362 | — | — | 1 | 5.83 |
| CHEMBL1643363 | — | — | 1 | 5.77 |
| CHEMBL1643364 | — | — | 1 | 5.73 |
| CHEMBL1643571 | — | — | 1 | 5.71 |
| CHEMBL1643368 | — | — | 1 | 5.67 |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | 5.50 |
| CHEMBL1643366 | — | — | 1 | 5.46 |
| CHEMBL1643572 | — | — | 1 | 5.44 |
| CHEMBL1643575 | — | — | 1 | 5.37 |
| CHEMBL1643367 | — | — | 1 | 5.17 |
| CHEMBL1643355 | — | — | 1 | 5.11 |
| CHEMBL1643576 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1643573 | — | IC50 | = | 239.88 | nM | 6.62 |
| CHEMBL1643574 | — | IC50 | = | 239.88 | nM | 6.62 |
| CHEMBL1643356 | — | IC50 | = | 426.58 | nM | 6.37 |
| CHEMBL1643365 | — | IC50 | = | 575.44 | nM | 6.24 |
| CHEMBL1643357 | — | IC50 | = | 588.84 | nM | 6.23 |
| CHEMBL1233300 | HYDROXYFASUDIL | IC50 | = | 758.58 | nM | 6.12 |
| CHEMBL1643358 | — | IC50 | = | 776.25 | nM | 6.11 |
| CHEMBL1643359 | — | IC50 | = | 812.83 | nM | 6.09 |
| CHEMBL559147 | Y-27632 | IC50 | = | 870.96 | nM | 6.06 |
| CHEMBL1643360 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1643361 | — | IC50 | = | 1288.25 | nM | 5.89 |
| CHEMBL1643362 | — | IC50 | = | 1479.11 | nM | 5.83 |
| CHEMBL1643363 | — | IC50 | = | 1698.24 | nM | 5.77 |
| CHEMBL1643364 | — | IC50 | = | 1862.09 | nM | 5.73 |
| CHEMBL1643571 | — | IC50 | = | 1949.84 | nM | 5.71 |
| CHEMBL1643368 | — | IC50 | = | 2137.96 | nM | 5.67 |
| CHEMBL38380 | FASUDIL | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL1643366 | — | IC50 | = | 3467.37 | nM | 5.46 |
| CHEMBL1643572 | — | IC50 | = | 3630.78 | nM | 5.44 |
| CHEMBL1643575 | — | IC50 | = | 4265.8 | nM | 5.37 |
| CHEMBL1643367 | — | IC50 | = | 6760.83 | nM | 5.17 |
| CHEMBL1643355 | — | IC50 | = | 7762.47 | nM | 5.11 |
| CHEMBL1643576 | — | IC50 | > | 100000.0 | nM | - |