Assay Detail
Binding
CHEMBL3888937
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation Assay: The Notch-CBF1 (C-promoter binding factor I) cell based transactivation assay is based on the ability of the released Notch intracellular domain fragments (NICDs) to function as transcription factors in conjunction with CBF1 and other nuclear factors. Luciferase assays were used to measure the antagonism of Notch-CBF1 transcriptional activity. HeLa cervical cancer cells are transiently co-transfected with pCDNA3.1/Hygro plasmids containing truncated Notch 1, Notch 2, Notch 3, or Notch 4 receptors and a PGL3 luciferase reporter vector containing 4 copies of CBF1 binding site. The cells were then tested for Notch-CBF1 activity in the absence or presence of test compounds. HeLa cells, maintained in DMEM (high glucose with HEPES), 1× glutamine/penicillin/streptomycin and 10% Fetal Bovine serum, were transiently transfected in a T175 Flask (4.5×106 cells/flask) using the Monster Transfection Kit (Minis #MIR2906) according to manufacturers specifications.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HeLa |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Recombining binding protein suppressor of hairless (CHEMBL4105709) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Fluoroalkyl and fluorocycloalkyl 1,4-benzodiazepinone compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 8.14 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4111071 | — | — | 1 | 8.85 |
| CHEMBL4112855 | — | — | 1 | 8.68 |
| CHEMBL4114579 | — | — | 1 | 8.66 |
| CHEMBL4111904 | — | — | 1 | 8.62 |
| CHEMBL3921166 | — | — | 1 | 8.62 |
| CHEMBL4114126 | — | — | 1 | 8.62 |
| CHEMBL3896414 | — | — | 1 | 8.49 |
| CHEMBL4107767 | — | — | 1 | 8.49 |
| CHEMBL4107070 | — | — | 1 | 8.42 |
| CHEMBL4112577 | — | — | 1 | 8.40 |
| CHEMBL4106629 | — | — | 1 | 8.37 |
| CHEMBL4109925 | — | — | 1 | 8.36 |
| CHEMBL3935675 | — | — | 1 | 8.27 |
| CHEMBL4115546 | — | — | 1 | 8.22 |
| CHEMBL4112450 | — | — | 1 | 8.14 |
| CHEMBL4108092 | — | — | 1 | 8.05 |
| CHEMBL4108896 | — | — | 1 | 8.03 |
| CHEMBL4111709 | — | — | 1 | 7.97 |
| CHEMBL3958560 | — | — | 1 | 7.96 |
| CHEMBL3957276 | — | — | 1 | 7.90 |
| CHEMBL3974604 | — | — | 1 | 7.87 |
| CHEMBL3890931 | — | — | 1 | 7.86 |
| CHEMBL3975558 | — | — | 1 | 7.81 |
| CHEMBL3956533 | — | — | 1 | 7.78 |
| CHEMBL4113103 | — | — | 1 | 7.72 |
| CHEMBL4107530 | — | — | 1 | 7.70 |
| CHEMBL4112536 | — | — | 1 | 7.67 |
| CHEMBL429441 | — | — | 1 | 7.32 |
| CHEMBL3945182 | — | — | 1 | 7.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4111071 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4112855 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4114579 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4111904 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3921166 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4114126 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3896414 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4107767 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4107070 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4112577 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4106629 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4109925 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL3935675 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4115546 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4112450 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4108092 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL4108896 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4111709 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL3958560 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3957276 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL3974604 | — | IC50 | = | 13.5 | nM | 7.87 |
| CHEMBL3890931 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL3975558 | — | IC50 | = | 15.4 | nM | 7.81 |
| CHEMBL3956533 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL4113103 | — | IC50 | = | 18.9 | nM | 7.72 |
| CHEMBL4107530 | — | IC50 | = | 20.1 | nM | 7.70 |
| CHEMBL4112536 | — | IC50 | = | 21.2 | nM | 7.67 |
| CHEMBL429441 | — | IC50 | = | 48.3 | nM | 7.32 |
| CHEMBL3945182 | — | IC50 | = | 74.5 | nM | 7.13 |