Assay Detail
Binding
CHEMBL4022061
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His6-tagged PARP14 catalytic/WWE domain (1459 to 1801 residues) expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay
35
Total Activities
18
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
Protein mono-ADP-ribosyltransferase PARP14 (CHEMBL2176777) ↗| 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 | 35 | 6.01 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4068366 | — | — | 2 | 6.80 |
| CHEMBL4074448 | — | — | 2 | 6.57 |
| CHEMBL4104938 | — | — | 2 | 6.43 |
| CHEMBL4084742 | — | — | 2 | 6.39 |
| CHEMBL4079213 | — | — | 2 | 6.39 |
| CHEMBL4104503 | — | — | 2 | 6.35 |
| CHEMBL4080281 | — | — | 2 | 6.19 |
| CHEMBL4089522 | — | — | 2 | 6.16 |
| CHEMBL4085694 | — | — | 2 | 6.16 |
| CHEMBL4087082 | — | — | 2 | 6.05 |
| CHEMBL4103623 | — | — | 2 | 5.99 |
| CHEMBL4101019 | — | — | 2 | 5.97 |
| CHEMBL4101188 | — | — | 2 | 5.66 |
| CHEMBL4059706 | — | — | 2 | 5.55 |
| CHEMBL4081650 | — | — | 2 | 5.47 |
| CHEMBL4093441 | — | — | 2 | 5.46 |
| CHEMBL4097232 | — | — | 2 | 5.38 |
| CHEMBL4065025 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4068366 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4074448 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4074448 | — | IC50 | = | 275.42 | nM | 6.56 |
| CHEMBL4104938 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4104938 | — | IC50 | = | 371.54 | nM | 6.43 |
| CHEMBL4084742 | — | IC50 | = | 407.38 | nM | 6.39 |
| CHEMBL4079213 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4079213 | — | IC50 | = | 407.38 | nM | 6.39 |
| CHEMBL4104503 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4104503 | — | IC50 | = | 446.68 | nM | 6.35 |
| CHEMBL4068366 | — | IC50 | = | 616.6 | nM | 6.21 |
| CHEMBL4080281 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4080281 | — | IC50 | = | 676.08 | nM | 6.17 |
| CHEMBL4089522 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4085694 | — | IC50 | = | 691.83 | nM | 6.16 |
| CHEMBL4085694 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4089522 | — | IC50 | = | 707.95 | nM | 6.15 |
| CHEMBL4087082 | — | IC50 | = | 891.25 | nM | 6.05 |
| CHEMBL4087082 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4103623 | — | IC50 | = | 1023.29 | nM | 5.99 |
| CHEMBL4101019 | — | IC50 | = | 1071.52 | nM | 5.97 |
| CHEMBL4101019 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4103623 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4101188 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4101188 | — | IC50 | = | 2238.72 | nM | 5.65 |
| CHEMBL4084742 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4059706 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4059706 | — | IC50 | = | 2818.38 | nM | 5.55 |
| CHEMBL4081650 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4081650 | — | IC50 | = | 3388.44 | nM | 5.47 |
| CHEMBL4093441 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4093441 | — | IC50 | = | 3548.13 | nM | 5.45 |
| CHEMBL4097232 | — | IC50 | = | 4168.69 | nM | 5.38 |
| CHEMBL4097232 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4065025 | — | IC50 | > | 20000.0 | nM | - |