Assay Detail
Binding
CHEMBL4022065
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His6-tagged PARP5a catalytic domain (1091 to 1325 residues) expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay
16
Total Activities
8
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
Poly [ADP-ribose] polymerase tankyrase-1 (CHEMBL6164) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of potent inhibitors of the mono(ADP-ribosyl)transferase, PARP14.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.40 | 6.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4085694 | — | — | 2 | 6.24 |
| CHEMBL4068366 | — | — | 2 | 6.05 |
| CHEMBL4089522 | — | — | 2 | 5.57 |
| CHEMBL4104503 | — | — | 2 | 5.32 |
| CHEMBL4087082 | — | — | 2 | 5.22 |
| CHEMBL4074448 | — | — | 2 | 5.10 |
| CHEMBL4079213 | — | — | 2 | 5.03 |
| CHEMBL4097232 | — | — | 2 | 5.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4085694 | — | IC50 | = | 575.44 | nM | 6.24 |
| CHEMBL4068366 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4068366 | — | IC50 | = | 977.24 | nM | 6.01 |
| CHEMBL4085694 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4089522 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4089522 | — | IC50 | = | 2691.53 | nM | 5.57 |
| CHEMBL4104503 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4104503 | — | IC50 | = | 4786.3 | nM | 5.32 |
| CHEMBL4087082 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4087082 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL4074448 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL4074448 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4079213 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL4079213 | — | IC50 | = | 9332.54 | nM | 5.03 |
| CHEMBL4097232 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL4097232 | — | IC50 | = | 9772.37 | nM | 5.01 |