Assay Detail
Binding
CHEMBL3585197
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ROCK1 (6 to 553 amino acids) (unknown origin) using Lys-Lys-Arg-Asn-Arg-Thr-Leu-Ser-Val as substrate preincubated for 15 mins followed by ATP addition by pyruvate kinase/lactate dehydrogenase coupled assay
38
Total Activities
38
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
Design, Synthesis, and Structure-Activity Relationships of Pyridine-Based Rho Kinase (ROCK) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 38 | 7.00 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3581126 | — | — | 1 | 8.15 |
| CHEMBL3581132 | — | — | 1 | 8.00 |
| CHEMBL3580669 | — | — | 1 | 8.00 |
| CHEMBL3581129 | — | — | 1 | 7.77 |
| CHEMBL3581146 | — | — | 1 | 7.75 |
| CHEMBL3581149 | — | — | 1 | 7.66 |
| CHEMBL3581128 | — | — | 1 | 7.58 |
| CHEMBL3581123 | — | — | 1 | 7.55 |
| CHEMBL3581150 | — | — | 1 | 7.52 |
| CHEMBL3581147 | — | — | 1 | 7.36 |
| CHEMBL3581148 | — | — | 1 | 7.35 |
| CHEMBL3581133 | — | — | 1 | 7.21 |
| CHEMBL3581124 | — | — | 1 | 7.16 |
| CHEMBL3581119 | — | — | 1 | 7.09 |
| CHEMBL3581135 | — | — | 1 | 7.05 |
| CHEMBL3581121 | — | — | 1 | 7.00 |
| CHEMBL3581125 | — | — | 1 | 7.00 |
| CHEMBL3581144 | — | — | 1 | 6.96 |
| CHEMBL3581138 | — | — | 1 | 6.92 |
| CHEMBL3581118 | — | — | 1 | 6.92 |
| CHEMBL3581145 | — | — | 1 | 6.92 |
| CHEMBL3581117 | — | — | 1 | 6.89 |
| CHEMBL3581134 | — | — | 1 | 6.85 |
| CHEMBL3581140 | — | — | 1 | 6.77 |
| CHEMBL3581116 | — | — | 1 | 6.77 |
| CHEMBL3581139 | — | — | 1 | 6.68 |
| CHEMBL3581127 | — | — | 1 | 6.46 |
| CHEMBL3581131 | — | — | 1 | 6.31 |
| CHEMBL3581130 | — | — | 1 | 6.28 |
| CHEMBL1427910 | — | — | 1 | 6.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3581126 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL3581132 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3580669 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3581129 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3581146 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL3581149 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL3581128 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL3581123 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL3581150 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL3581147 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL3581148 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL3581133 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL3581124 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL3581119 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL3581135 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL3581121 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3581125 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3581144 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL3581145 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL3581118 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL3581138 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL3581117 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL3581134 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL3581140 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL3581116 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL3581139 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL3581127 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL3581131 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL3581130 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL1427910 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL3581141 | — | Ki | = | 770.0 | nM | 6.11 |
| CHEMBL3581122 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL3581115 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL3581136 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL3581120 | — | Ki | > | 2500.0 | nM | - |
| CHEMBL3581143 | — | Ki | > | 2500.0 | nM | - |
| CHEMBL3581142 | — | Ki | > | 2500.0 | nM | - |
| CHEMBL3581137 | — | Ki | > | 2500.0 | nM | - |