Assay Detail
Binding
CHEMBL3705637
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinase Inhibition Assay: Inhibition of ROCK2 activity was determined using the IMAP Screening Express Kit (Molecular Devices product number #8073). ROCK2 kinase (UpstateChemicon #14-451) and Flourescein tagged substrate peptide Fl-AKRRRLSSLRA (Molecular Devices product number R7184).
166
Total Activities
165
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Cytoskeletal active rho kinase inhibitor compounds, composition and use
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 166 | 6.27 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3689393 | — | — | 1 | 7.82 |
| CHEMBL3689439 | — | — | 1 | 7.59 |
| CHEMBL3689429 | — | — | 1 | 7.53 |
| CHEMBL3689421 | — | — | 1 | 7.52 |
| CHEMBL3689422 | — | — | 1 | 7.52 |
| CHEMBL3689489 | — | — | 1 | 7.52 |
| CHEMBL3689400 | — | — | 1 | 7.50 |
| CHEMBL3689442 | — | — | 1 | 7.46 |
| CHEMBL3689440 | — | — | 1 | 7.37 |
| CHEMBL3689399 | — | — | 1 | 7.32 |
| CHEMBL3689431 | — | — | 1 | 7.31 |
| CHEMBL3689417 | — | — | 1 | 7.28 |
| CHEMBL3689389 | — | — | 1 | 7.24 |
| CHEMBL3689412 | — | — | 1 | 7.23 |
| CHEMBL3689462 | — | — | 1 | 7.23 |
| CHEMBL3689392 | — | — | 1 | 7.20 |
| CHEMBL3689418 | — | — | 1 | 7.20 |
| CHEMBL3689352 | — | — | 1 | 7.18 |
| CHEMBL3689376 | — | — | 1 | 7.16 |
| CHEMBL3689379 | — | — | 1 | 7.16 |
| CHEMBL3689441 | — | — | 1 | 7.16 |
| CHEMBL3689445 | — | — | 1 | 7.16 |
| CHEMBL3689414 | — | — | 1 | 7.14 |
| CHEMBL3689415 | — | — | 1 | 7.13 |
| CHEMBL3689470 | — | — | 1 | 7.13 |
| CHEMBL3689375 | — | — | 1 | 7.06 |
| CHEMBL3689401 | — | — | 1 | 7.06 |
| CHEMBL3689495 | — | — | 1 | 7.06 |
| CHEMBL3689433 | — | — | 1 | 7.00 |
| CHEMBL3689465 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3689393 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL3689439 | — | IC50 | = | 25.8 | nM | 7.59 |
| CHEMBL3689429 | — | IC50 | = | 29.4 | nM | 7.53 |
| CHEMBL3689489 | — | IC50 | = | 29.9 | nM | 7.52 |
| CHEMBL3689421 | — | IC50 | = | 30.1 | nM | 7.52 |
| CHEMBL3689422 | — | IC50 | = | 30.4 | nM | 7.52 |
| CHEMBL3689400 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3689442 | — | IC50 | = | 34.3 | nM | 7.46 |
| CHEMBL3689440 | — | IC50 | = | 42.9 | nM | 7.37 |
| CHEMBL3689399 | — | IC50 | = | 47.5 | nM | 7.32 |
| CHEMBL3689431 | — | IC50 | = | 49.4 | nM | 7.31 |
| CHEMBL3689417 | — | IC50 | = | 53.1 | nM | 7.28 |
| CHEMBL3689389 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3689412 | — | IC50 | = | 58.5 | nM | 7.23 |
| CHEMBL3689462 | — | IC50 | = | 59.2 | nM | 7.23 |
| CHEMBL3689418 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3689392 | — | IC50 | = | 62.6 | nM | 7.20 |
| CHEMBL3689352 | — | IC50 | = | 65.8 | nM | 7.18 |
| CHEMBL3689445 | — | IC50 | = | 69.2 | nM | 7.16 |
| CHEMBL3689441 | — | IC50 | = | 68.5 | nM | 7.16 |
| CHEMBL3689376 | — | IC50 | = | 69.1 | nM | 7.16 |
| CHEMBL3689379 | — | IC50 | = | 69.5 | nM | 7.16 |
| CHEMBL3689414 | — | IC50 | = | 71.6 | nM | 7.14 |
| CHEMBL3689415 | — | IC50 | = | 74.5 | nM | 7.13 |
| CHEMBL3689470 | — | IC50 | = | 73.9 | nM | 7.13 |
| CHEMBL3689495 | — | IC50 | = | 87.1 | nM | 7.06 |
| CHEMBL3689375 | — | IC50 | = | 86.9 | nM | 7.06 |
| CHEMBL3689401 | — | IC50 | = | 87.2 | nM | 7.06 |
| CHEMBL3689503 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL3689465 | — | IC50 | = | 98.8 | nM | 7.00 |
| CHEMBL3689433 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL3689419 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL3689443 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL3689368 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL3689416 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL3689413 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL3689458 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL3689502 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL3689491 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3689395 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL3689360 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL3689461 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL3689383 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL3689382 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL3689446 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL3689388 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL3689403 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL3689500 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3689420 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL3689405 | — | IC50 | = | 165.0 | nM | 6.78 |