Assay Detail
Binding
CHEMBL4479676
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length recombinant human GST-tagged MARK3 expressed in baculovirus expression system using biotinylated-Cdc25C peptide substrate measured after 2 hrs by HTRF assay
27
Total Activities
27
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 |
Target
MAP/microtubule affinity-regulating kinase 3 (CHEMBL5600) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.93 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4569508 | — | — | 1 | 9.00 |
| CHEMBL4532781 | — | — | 1 | 9.00 |
| CHEMBL4550486 | — | — | 1 | 8.89 |
| CHEMBL4528550 | — | — | 1 | 8.70 |
| CHEMBL4552799 | — | — | 1 | 8.62 |
| CHEMBL4562217 | — | — | 1 | 8.52 |
| CHEMBL4552628 | — | — | 1 | 8.30 |
| CHEMBL4593028 | — | — | 1 | 8.30 |
| CHEMBL4550702 | — | — | 1 | 8.22 |
| CHEMBL4579339 | — | — | 1 | 8.05 |
| CHEMBL4571737 | — | — | 1 | 8.05 |
| CHEMBL4543195 | — | — | 1 | 8.00 |
| CHEMBL4569165 | — | — | 1 | 8.00 |
| CHEMBL4547786 | — | — | 1 | 7.89 |
| CHEMBL4557345 | — | — | 1 | 7.82 |
| CHEMBL4578265 | — | — | 1 | 7.82 |
| CHEMBL4589674 | — | — | 1 | 7.66 |
| CHEMBL4544609 | — | — | 1 | 7.62 |
| CHEMBL4526375 | — | — | 1 | 7.42 |
| CHEMBL4588200 | — | — | 1 | 7.37 |
| CHEMBL4550262 | — | — | 1 | 7.16 |
| CHEMBL4541288 | — | — | 1 | 7.13 |
| CHEMBL4514812 | — | — | 1 | 7.00 |
| CHEMBL4556844 | — | — | 1 | 6.89 |
| CHEMBL4561857 | — | — | 1 | 6.89 |
| CHEMBL4568087 | — | — | 1 | - |
| CHEMBL4565845 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4569508 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4532781 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4550486 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4528550 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4552799 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4562217 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4552628 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4593028 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4550702 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4579339 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4571737 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4543195 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4569165 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4547786 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4557345 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4578265 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4589674 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4544609 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4526375 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4588200 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4550262 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4541288 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4514812 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4556844 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4561857 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4568087 | — | IC50 | <= | 0.5 | nM | - |
| CHEMBL4565845 | — | IC50 | < | 0.25 | nM | - |