Assay Detail
Binding
CHEMBL3705445
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Biochemical Assay: Affinity evaluation of the tested compounds and their selectivity with respect to the different PARP isoforms of interest was assessed in a displacement assay.The identification of compounds capable of binding several PARP proteins is carried out through a screening method including the steps ofa) providing a reaction mixture containing:the PARP protein isoform under investigation,a compound of formula (IP): wherein R10 is hydrogen or methyl, B is (CH2)nNH group, n is 2 to 6; m is 0 or 1 and X− is a counterion, and serial dilutions of the test compound;b) comparing the polarization signal generated in the absence of the test compound with the one generated in the presence of different concentrations of the test compound, andc) evaluating the ability of the test compound to displace the compound of formula (IP) as defined above indicated from a decreased fluorescence polarization level. The polarization signal can be measured, e.g., by a plate reader such as the Saphire2 (Tecan).
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
3-oxo-2,3-dihydro-1H-isoindole-4-carboxamides as PARP inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 6.28 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3606021 | — | — | 1 | 8.00 |
| CHEMBL3605985 | — | — | 1 | 7.40 |
| CHEMBL3606024 | — | — | 1 | 7.10 |
| CHEMBL3699004 | — | — | 1 | 7.10 |
| CHEMBL3605984 | — | — | 1 | 7.10 |
| CHEMBL3698978 | — | — | 1 | 7.05 |
| CHEMBL3606016 | — | — | 1 | 7.00 |
| CHEMBL3605998 | — | — | 1 | 6.96 |
| CHEMBL3698977 | — | — | 1 | 6.85 |
| CHEMBL3698976 | — | — | 1 | 6.80 |
| CHEMBL3699003 | — | — | 1 | 6.80 |
| CHEMBL3606015 | — | — | 1 | 6.72 |
| CHEMBL3698987 | — | — | 1 | 6.70 |
| CHEMBL3698994 | — | — | 1 | 6.64 |
| CHEMBL3698995 | — | — | 1 | 6.58 |
| CHEMBL3698996 | — | — | 1 | 6.58 |
| CHEMBL3698989 | — | — | 1 | 6.52 |
| CHEMBL3698993 | — | — | 1 | 6.52 |
| CHEMBL3698988 | — | — | 1 | 6.50 |
| CHEMBL3606018 | — | — | 1 | 6.48 |
| CHEMBL3698997 | — | — | 1 | 6.48 |
| CHEMBL3699002 | — | — | 1 | 6.44 |
| CHEMBL3698990 | — | — | 1 | 6.42 |
| CHEMBL3698975 | — | — | 1 | 6.41 |
| CHEMBL3698974 | — | — | 1 | 6.40 |
| CHEMBL3605995 | — | — | 1 | 6.39 |
| CHEMBL3699001 | — | — | 1 | 6.30 |
| CHEMBL3606023 | — | — | 1 | 6.30 |
| CHEMBL3606019 | — | — | 1 | 6.28 |
| CHEMBL3698998 | — | — | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3606021 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3605985 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3699004 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3605984 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3606024 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3698978 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3606016 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3605998 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3698977 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3698976 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3699003 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3606015 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3698987 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3698994 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3698996 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3698995 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3698989 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3698993 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3698988 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3606018 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3698997 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3699002 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3698990 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3698975 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL3698974 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3605995 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3699001 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3606023 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3606019 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3698998 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL3698992 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3698991 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3605996 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3606014 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL3698980 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3699000 | — | IC50 | = | 2660.0 | nM | 5.58 |
| CHEMBL3606003 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3698981 | — | IC50 | = | 3950.0 | nM | 5.40 |
| CHEMBL3606000 | — | IC50 | = | 4420.0 | nM | 5.36 |
| CHEMBL3698979 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL3698999 | — | IC50 | = | 5310.0 | nM | 5.28 |
| CHEMBL3698985 | — | IC50 | = | 5770.0 | nM | 5.24 |
| CHEMBL3606001 | — | IC50 | = | 5990.0 | nM | 5.22 |
| CHEMBL3606005 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL3698986 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL3605997 | — | IC50 | = | 9890.0 | nM | 5.00 |