Assay Detail
Binding
CHEMBL5112349
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Inhibition of recombinant LIMK2 (347 to 659 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 180 mins by RapidFire Mass Spectrometry kinase assay
21
Total Activities
21
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
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.29 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL570116 | — | — | 1 | 8.74 |
| CHEMBL5169387 | — | — | 1 | 8.26 |
| CHEMBL5202859 | — | — | 1 | 8.20 |
| CHEMBL3355509 | — | — | 1 | 8.14 |
| CHEMBL3356433 | LX-7101 | 1.0 | 1 | 7.97 |
| CHEMBL3355507 | — | — | 1 | 7.90 |
| CHEMBL3609326 | — | — | 1 | 7.87 |
| CHEMBL4790618 | — | — | 1 | 7.84 |
| CHEMBL3182065 | — | — | 1 | 7.52 |
| CHEMBL2141887 | — | — | 1 | 7.48 |
| CHEMBL5186508 | — | — | 1 | 7.40 |
| CHEMBL2070615 | — | — | 1 | 6.87 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 6.65 |
| CHEMBL3355491 | — | — | 1 | 6.57 |
| CHEMBL3410036 | — | — | 1 | 5.72 |
| CHEMBL1774055 | — | — | 1 | 5.71 |
| CHEMBL363160 | PHA-680632 | — | 1 | 5.10 |
| CHEMBL2107823 | GANDOTINIB | 2.0 | 1 | - |
| CHEMBL3185148 | — | — | 1 | - |
| CHEMBL3990456 | — | — | 1 | - |
| CHEMBL4303259 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL570116 | — | IC50 | = | 1.82 | nM | 8.74 |
| CHEMBL5169387 | — | IC50 | = | 5.495 | nM | 8.26 |
| CHEMBL5202859 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL3355509 | — | IC50 | = | 7.244 | nM | 8.14 |
| CHEMBL3356433 | LX-7101 | IC50 | = | 10.72 | nM | 7.97 |
| CHEMBL3355507 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL3609326 | — | IC50 | = | 13.49 | nM | 7.87 |
| CHEMBL4790618 | — | IC50 | = | 14.45 | nM | 7.84 |
| CHEMBL3182065 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL2141887 | — | IC50 | = | 33.11 | nM | 7.48 |
| CHEMBL5186508 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL2070615 | — | IC50 | = | 134.9 | nM | 6.87 |
| CHEMBL5416410 | DASATINIB | IC50 | = | 223.87 | nM | 6.65 |
| CHEMBL3355491 | — | IC50 | = | 269.15 | nM | 6.57 |
| CHEMBL3410036 | — | IC50 | = | 1905.46 | nM | 5.72 |
| CHEMBL1774055 | — | IC50 | = | 1949.84 | nM | 5.71 |
| CHEMBL363160 | PHA-680632 | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL2107823 | GANDOTINIB | IC50 | > | 10000.0 | nM | - |
| CHEMBL3185148 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3990456 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4303259 | — | IC50 | > | 10000.0 | nM | - |