Assay Detail
Binding
CHEMBL3607347
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Binding affinity to full length recombinant human PARP-2 by fluorescence polarization displacement assay
41
Total Activities
41
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 |
Publication
Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 41 | 5.93 | 7.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3605990 | — | — | 1 | 7.48 |
| CHEMBL3605992 | — | — | 1 | 7.12 |
| CHEMBL3605967 | — | — | 1 | 6.90 |
| CHEMBL3605972 | — | — | 1 | 6.75 |
| CHEMBL3605993 | — | — | 1 | 6.58 |
| CHEMBL3605973 | — | — | 1 | 6.54 |
| CHEMBL3605991 | — | — | 1 | 6.47 |
| CHEMBL3605982 | — | — | 1 | 6.38 |
| CHEMBL1329044 | — | — | 1 | 6.38 |
| CHEMBL3605994 | — | — | 1 | 6.36 |
| CHEMBL3605970 | — | — | 1 | 6.24 |
| CHEMBL3606012 | — | — | 1 | 6.23 |
| CHEMBL3605981 | — | — | 1 | 6.17 |
| CHEMBL3606013 | — | — | 1 | 6.01 |
| CHEMBL3605984 | — | — | 1 | 5.95 |
| CHEMBL3606009 | — | — | 1 | 5.84 |
| CHEMBL3606011 | — | — | 1 | 5.77 |
| CHEMBL3606000 | — | — | 1 | 5.64 |
| CHEMBL3606001 | — | — | 1 | 5.62 |
| CHEMBL3606015 | — | — | 1 | 5.60 |
| CHEMBL3605985 | — | — | 1 | 5.58 |
| CHEMBL3606016 | — | — | 1 | 5.52 |
| CHEMBL3605978 | — | — | 1 | 5.47 |
| CHEMBL3606004 | — | — | 1 | 5.44 |
| CHEMBL3606010 | — | — | 1 | 5.43 |
| CHEMBL3606018 | — | — | 1 | 5.41 |
| CHEMBL3605983 | — | — | 1 | 5.24 |
| CHEMBL3605976 | — | — | 1 | 5.23 |
| CHEMBL3606007 | — | — | 1 | 5.17 |
| CHEMBL3605999 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3605990 | — | Kd | = | 33.0 | nM | 7.48 |
| CHEMBL3605992 | — | Kd | = | 75.0 | nM | 7.12 |
| CHEMBL3605967 | — | Kd | = | 125.0 | nM | 6.90 |
| CHEMBL3605972 | — | Kd | = | 178.0 | nM | 6.75 |
| CHEMBL3605993 | — | Kd | = | 264.0 | nM | 6.58 |
| CHEMBL3605973 | — | Kd | = | 286.0 | nM | 6.54 |
| CHEMBL3605991 | — | Kd | = | 340.0 | nM | 6.47 |
| CHEMBL3605982 | — | Kd | = | 420.0 | nM | 6.38 |
| CHEMBL1329044 | — | Kd | = | 422.0 | nM | 6.38 |
| CHEMBL3605994 | — | Kd | = | 441.0 | nM | 6.36 |
| CHEMBL3605970 | — | Kd | = | 575.0 | nM | 6.24 |
| CHEMBL3606012 | — | Kd | = | 583.0 | nM | 6.23 |
| CHEMBL3605981 | — | Kd | = | 670.0 | nM | 6.17 |
| CHEMBL3606013 | — | Kd | = | 983.0 | nM | 6.01 |
| CHEMBL3605984 | — | Kd | = | 1112.0 | nM | 5.95 |
| CHEMBL3606009 | — | Kd | = | 1435.0 | nM | 5.84 |
| CHEMBL3606011 | — | Kd | = | 1698.0 | nM | 5.77 |
| CHEMBL3606000 | — | Kd | = | 2289.0 | nM | 5.64 |
| CHEMBL3606001 | — | Kd | = | 2425.0 | nM | 5.62 |
| CHEMBL3606015 | — | Kd | = | 2510.0 | nM | 5.60 |
| CHEMBL3605985 | — | Kd | = | 2600.0 | nM | 5.58 |
| CHEMBL3606016 | — | Kd | = | 3017.0 | nM | 5.52 |
| CHEMBL3605978 | — | Kd | = | 3360.0 | nM | 5.47 |
| CHEMBL3606004 | — | Kd | = | 3627.0 | nM | 5.44 |
| CHEMBL3606010 | — | Kd | = | 3700.0 | nM | 5.43 |
| CHEMBL3606018 | — | Kd | = | 3937.0 | nM | 5.41 |
| CHEMBL3605983 | — | Kd | = | 5776.0 | nM | 5.24 |
| CHEMBL3605976 | — | Kd | = | 5870.0 | nM | 5.23 |
| CHEMBL3606007 | — | Kd | = | 6804.0 | nM | 5.17 |
| CHEMBL3605999 | — | Kd | = | 6916.0 | nM | 5.16 |
| CHEMBL3605997 | — | Kd | = | 8714.0 | nM | 5.06 |
| CHEMBL3605998 | — | Kd | = | 8991.0 | nM | 5.05 |
| CHEMBL3606003 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL3606005 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL3606006 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL3606008 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL3605996 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL3605974 | — | Kd | < | 30.0 | nM | - |
| CHEMBL3605986 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL3606017 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL3606014 | — | Kd | > | 10000.0 | nM | - |