Assay Detail
Binding
CHEMBL2033943
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Inhibition of biotin-labelled Bcl-xL using [FAM]-IWIAQELRRIGDEFNAYY-NH2 as substrate after 60 mins by FRET analysis
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Pyrazole and pyrimidine phenylacylsulfonamides as dual Bcl-2/Bcl-xL antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.27 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2030856 | — | — | 1 | 8.22 |
| CHEMBL2030860 | — | — | 1 | 8.15 |
| CHEMBL2030857 | — | — | 1 | 8.15 |
| CHEMBL2030859 | — | — | 1 | 8.10 |
| CHEMBL2031009 | — | — | 1 | 8.05 |
| CHEMBL2030847 | — | — | 1 | 7.96 |
| CHEMBL2030855 | — | — | 1 | 7.89 |
| CHEMBL2030861 | — | — | 1 | 7.89 |
| CHEMBL2031008 | — | — | 1 | 7.85 |
| CHEMBL2030864 | — | — | 1 | 7.82 |
| CHEMBL2030858 | — | — | 1 | 7.82 |
| CHEMBL2030853 | — | — | 1 | 7.75 |
| CHEMBL2030854 | — | — | 1 | 7.58 |
| CHEMBL2030846 | — | — | 1 | 7.52 |
| CHEMBL2030852 | — | — | 1 | 7.46 |
| CHEMBL2030851 | — | — | 1 | 7.46 |
| CHEMBL2030845 | — | — | 1 | 7.38 |
| CHEMBL2030848 | — | — | 1 | 7.32 |
| CHEMBL2030850 | — | — | 1 | 7.26 |
| CHEMBL2030863 | — | — | 1 | 6.92 |
| CHEMBL2031006 | — | — | 1 | 6.92 |
| CHEMBL2031004 | — | — | 1 | 6.89 |
| CHEMBL2030862 | — | — | 1 | 6.85 |
| CHEMBL2031003 | — | — | 1 | 6.80 |
| CHEMBL2031005 | — | — | 1 | 6.64 |
| CHEMBL2031007 | — | — | 1 | 6.60 |
| CHEMBL2030849 | — | — | 1 | 6.33 |
| CHEMBL2030866 | — | — | 1 | 6.32 |
| CHEMBL2030865 | — | — | 1 | 6.30 |
| CHEMBL2030844 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2030856 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2030860 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2030857 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2030859 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2031009 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2030847 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2030855 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2030861 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2031008 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2030864 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2030858 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2030853 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2030854 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2030846 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2030851 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2030852 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2030845 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2030848 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL2030850 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL2030863 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2031006 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2031004 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2030862 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2031003 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2031005 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2031007 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2030849 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL2030866 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL2030865 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2030844 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL2031002 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL2031001 | — | IC50 | = | 970.0 | nM | 6.01 |