Assay Detail
Binding
CHEMBL1805103
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Inhibition of human recombinant CDK5/p25
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Cyclin-dependent kinase 5/CDK5 activator 1 (CHEMBL1907600) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 5.61 | 6.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1802358 | — | — | 1 | 6.39 |
| CHEMBL1802849 | — | — | 1 | 6.22 |
| CHEMBL1803071 | — | — | 1 | 6.16 |
| CHEMBL1179821 | — | — | 1 | 6.04 |
| CHEMBL1803073 | — | — | 1 | 5.92 |
| CHEMBL1802851 | — | — | 1 | 5.89 |
| CHEMBL1802848 | — | — | 1 | 5.80 |
| CHEMBL1803070 | — | — | 1 | 5.80 |
| CHEMBL1802850 | — | — | 1 | 5.77 |
| CHEMBL1803085 | — | — | 1 | 5.77 |
| CHEMBL1802844 | — | — | 1 | 5.75 |
| CHEMBL1802847 | — | — | 1 | 5.70 |
| CHEMBL1803082 | — | — | 1 | 5.62 |
| CHEMBL1802843 | — | — | 1 | 5.52 |
| CHEMBL1802356 | — | — | 1 | 5.52 |
| CHEMBL1802846 | — | — | 1 | 5.51 |
| CHEMBL1802845 | — | — | 1 | 5.48 |
| CHEMBL1802855 | — | — | 1 | 5.40 |
| CHEMBL1803069 | — | — | 1 | 5.37 |
| CHEMBL1802853 | — | — | 1 | 5.35 |
| CHEMBL1803083 | — | — | 1 | 5.33 |
| CHEMBL1803072 | — | — | 1 | 5.24 |
| CHEMBL1803079 | — | — | 1 | 5.14 |
| CHEMBL1802842 | — | — | 1 | 4.80 |
| CHEMBL1802841 | — | — | 1 | 4.75 |
| CHEMBL1802852 | — | — | 1 | - |
| CHEMBL1802355 | — | — | 1 | - |
| CHEMBL485053 | LEUCETTAMINE B | — | 1 | - |
| CHEMBL1802357 | — | — | 1 | - |
| CHEMBL1803067 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1802358 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL1802849 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL1803071 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1179821 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL1803073 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1802851 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1802848 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1803070 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1802850 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1803085 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1802844 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1802847 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1803082 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1802843 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1802356 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1802846 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL1802845 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL1802855 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL1803069 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL1802853 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL1803083 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL1803072 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL1803079 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL1802842 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL1802841 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL1803068 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1802857 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1802856 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1803084 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1802854 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1803067 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1802357 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL485053 | LEUCETTAMINE B | IC50 | > | 10000.0 | nM | - |
| CHEMBL1802355 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1802852 | — | IC50 | > | 100000.0 | nM | - |