Assay Detail
Binding
CHEMBL5387668
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His10-StrepII tagged human ROCK2 catalytic domain (1 to 553 residues) expressed in Sf9 insect cells by HTRF assay
92
Total Activities
90
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of unglycosylated indolocarbazoles as ROCK2 isoform-selective inhibitors for the treatment of breast cancer metastasis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 92 | 6.58 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5398049 | — | — | 1 | 8.52 |
| CHEMBL388978 | STAUROSPORINE | — | 2 | 8.40 |
| CHEMBL4294912 | — | — | 1 | 8.22 |
| CHEMBL5427567 | — | — | 1 | 8.15 |
| CHEMBL4763675 | — | — | 2 | 7.70 |
| CHEMBL190546 | — | — | 1 | 7.64 |
| CHEMBL4203245 | — | — | 1 | 7.46 |
| CHEMBL4277459 | — | — | 1 | 7.22 |
| CHEMBL4745670 | — | — | 1 | 7.12 |
| CHEMBL5396761 | — | — | 1 | 7.00 |
| CHEMBL5434756 | — | — | 1 | 6.96 |
| CHEMBL5407662 | — | — | 1 | 6.92 |
| CHEMBL4280872 | — | — | 1 | 6.92 |
| CHEMBL4796257 | — | — | 1 | 6.85 |
| CHEMBL4744662 | — | — | 1 | 6.85 |
| CHEMBL5402422 | — | — | 1 | 6.70 |
| CHEMBL4780192 | — | — | 1 | 6.68 |
| CHEMBL4291517 | — | — | 1 | 6.68 |
| CHEMBL4753473 | — | — | 1 | 6.60 |
| CHEMBL5396883 | — | — | 1 | 6.58 |
| CHEMBL5430350 | — | — | 1 | 6.58 |
| CHEMBL4745928 | — | — | 1 | 6.52 |
| CHEMBL4284275 | — | — | 1 | 6.50 |
| CHEMBL4745823 | — | — | 1 | 6.48 |
| CHEMBL4758448 | — | — | 1 | 6.47 |
| CHEMBL4754496 | — | — | 1 | 6.44 |
| CHEMBL5403816 | — | — | 1 | 6.44 |
| CHEMBL4794799 | — | — | 1 | 6.44 |
| CHEMBL4758636 | — | — | 1 | 6.43 |
| CHEMBL5399426 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5398049 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4294912 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5427567 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4763675 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL190546 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4203245 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4277459 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4745670 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL5396761 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5434756 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4280872 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5407662 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4796257 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4744662 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5402422 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4291517 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4780192 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4753473 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5430350 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5396883 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4745928 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4763675 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4284275 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4745823 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4758448 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4794799 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5403816 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4754496 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4758636 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL5399426 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4207068 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4783165 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL5405477 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL59004 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5411955 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4764299 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL64742 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL5423360 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL4762704 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4763267 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL4777775 | — | IC50 | = | 2070.0 | nM | 5.68 |
| CHEMBL4761909 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL4759925 | — | IC50 | = | 2240.0 | nM | 5.65 |
| CHEMBL4744480 | — | IC50 | = | 2720.0 | nM | 5.57 |
| CHEMBL4216395 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4763012 | — | IC50 | = | 2880.0 | nM | 5.54 |
| CHEMBL4759449 | — | IC50 | = | 4780.0 | nM | 5.32 |
| CHEMBL4762923 | — | IC50 | = | 8000.0 | nM | 5.10 |