Assay Detail
Binding
CHEMBL2024960
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Displacement of fluorescent-ARC-1063 from recombinant bovine PKAc by luminescence intensity assay
16
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Conjugates of 5-isoquinolinesulfonylamides and oligo-D-arginine possess high affinity and selectivity towards Rho kinase (ROCK).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 8 | 8.50 | 10.25 |
| IC50 | 8 | 5.20 | 6.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1077375 | — | — | 2 | 10.25 |
| CHEMBL279185 | — | — | 2 | 9.60 |
| CHEMBL525385 | — | — | 2 | 9.59 |
| CHEMBL2023843 | — | — | 2 | 8.48 |
| CHEMBL297394 | — | — | 2 | 8.35 |
| CHEMBL104264 | — | — | 2 | 7.77 |
| CHEMBL2023842 | — | — | 2 | 7.60 |
| CHEMBL38380 | FASUDIL | 3.0 | 2 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1077375 | — | Kd | = | 0.056 | nM | 10.25 |
| CHEMBL279185 | — | Kd | = | 0.25 | nM | 9.60 |
| CHEMBL525385 | — | Kd | = | 0.26 | nM | 9.59 |
| CHEMBL2023843 | — | Kd | = | 3.3 | nM | 8.48 |
| CHEMBL297394 | — | Kd | = | 4.5 | nM | 8.35 |
| CHEMBL104264 | — | Kd | = | 17.0 | nM | 7.77 |
| CHEMBL2023842 | — | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL1077375 | — | IC50 | = | 165.96 | nM | 6.78 |
| CHEMBL38380 | FASUDIL | Kd | = | 420.0 | nM | 6.38 |
| CHEMBL525385 | — | IC50 | = | 758.58 | nM | 6.12 |
| CHEMBL279185 | — | IC50 | = | 758.58 | nM | 6.12 |
| CHEMBL2023843 | — | IC50 | = | 9772.37 | nM | 5.01 |
| CHEMBL297394 | — | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL104264 | — | IC50 | = | 50118.72 | nM | 4.30 |
| CHEMBL38380 | FASUDIL | IC50 | = | 54954.09 | nM | 4.26 |
| CHEMBL2023842 | — | IC50 | = | 75857.76 | nM | 4.12 |