Assay Detail
Binding
CHEMBL5553852
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length N-terminal GST-tagged human CDK9 (1 to 372 residues) /His-tagged Cyclin T1 (1 to 726 residues) expressed in baculovirus expression system preincubated for 30 mins followed by ATP and ULight-histone H3 peptide/ULight-eIF4E binding protein addition and measured after 2 hrs by LANCE Ultra TR-FRET assay
3
Total Activities
3
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 |
Publication
A Comprehensive <i>In Vitro</i> Characterization of a New Class of Indole-Based Compounds Developed as Selective Haspin Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 5.12 | 5.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5178368 | — | — | 1 | 5.68 |
| CHEMBL5564324 | — | — | 1 | 5.01 |
| CHEMBL5575835 | — | — | 1 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5178368 | — | IC50 | = | 2078.0 | nM | 5.68 |
| CHEMBL5564324 | — | IC50 | = | 9828.0 | nM | 5.01 |
| CHEMBL5575835 | — | IC50 | = | 21690.0 | nM | 4.66 |