Assay Detail
Binding
CHEMBL3705161
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Homogenous Time-Resolved Fluorescence (HTRF) Assay: MARK3 activity was assayed in vitro using a Cdc25C biotinylated peptide substrate (Cell Signalling Technologies). The phosphopeptide product was quantitated using a Homogenous Time-Resolved Fluorescence (HTRF) assay system (Park et al., 1999, Anal. Biochem. 269:94-104).
5
Total Activities
5
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
Imidazo[1,2-a]pyridines and imidazo[1,2-b]pyridazines as mark inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.56 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3648448 | — | — | 1 | 9.30 |
| CHEMBL3648449 | — | — | 1 | 7.82 |
| CHEMBL3648447 | — | — | 1 | 7.70 |
| CHEMBL3648450 | — | — | 1 | 6.85 |
| CHEMBL3648446 | — | — | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3648448 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3648449 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3648447 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3648450 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3648446 | — | IC50 | = | 720.0 | nM | 6.14 |