| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA2150378 | B | Inhibition of NICD-mediated HES1 protein expression in human H4 cells at 10 uM after 24 hrs by Western blot analysis | Homo sapiens | 1 | ALA2146445 | cell-based format | Scientific Literature | |
| 2. | ALA3225624 | B | Binding affinity to human Notch-1 (amino acid residues A19 to Q526) at 0.125 to 2 uM by surface plasmon resonance assay | Homo sapiens | 1 | ALA3217476 | single protein format | Scientific Literature | |
| 3. | ALA3398717 | A | Inhibition of NOTCH-1 signaling (unknown origin) expressed in CHO cells at 5 to 50 uM after 24 hrs by dual luciferase reporter gene assay | Homo sapiens | 2 | ALA3397016 | cell-based format | Scientific Literature | |
| 4. | ALA3398718 | A | Inhibition of NOTCH-1 signaling (unknown origin) expressed in CHO cells at 0.5 uM after 24 hrs by dual luciferase reporter gene assay | Homo sapiens | 1 | ALA3397016 | cell-based format | Scientific Literature | |
| 5. | ALA3412050 | B | Inhibition of Notch1 intracellular domain fragment transfected in human HeLa cells co-transfected with CBF1-PGL3 luciferase reporter vector by transactivation assay | Homo sapiens | 20 | ALA3407492 | cell-based format | Scientific Literature | |
| 6. | ALA3888075 | B | Biological Assay: The pharmacological properties of the compounds of this invention may be confirmed by a number of biological assays. | 35 | ALA3886564 | single protein format | BindingDB Database | ||
| 7. | ALA3888076 | B | 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. | 4 | ALA3886564 | cell-based format | BindingDB Database | ||
| 8. | ALA3888936 | B | 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 | ALA3886893 | cell-based format | BindingDB Database | ||
| 9. | ALA4132673 | B | Inhibition of recombinant mouse N-terminal FLAG-tagged Notch1 (1704 to 2531 residues) expressed in human LS174T cells assessed as reduction in doxycycline-induced NICD expression after 12 hrs by Bright-Glo luciferase reporter gene assay | Homo sapiens | 8 | ALA4130386 | cell-based format | Scientific Literature | |
| 10. | ALA4132674 | B | Inhibition of doxycycline-induced recombinant mouse N-terminal FLAG-tagged Notch1 (1704 to 2531 residues) activation expressed in human LS174T cells assessed as reduction in Hes1 level at 0.1 to 1 uM after 12 hrs by Western blot analysis | Homo sapiens | 2 | ALA4130386 | cell-based format | Scientific Literature | |
| 11. | ALA4132675 | B | Inhibition of doxycycline-induced recombinant mouse N-terminal FLAG-tagged Notch1 (1704 to 2531 residues) activation expressed in human LS174T cells assessed as reduction in Hes5 level at 0.1 to 1 uM after 12 hrs by Western blot analysis | Homo sapiens | 2 | ALA4130386 | cell-based format | Scientific Literature | |
| 12. | ALA4256564 | B | Inhibition of Notch1 in human HPBALL cells assessed as reduction in NICD expression at 0.5 uM after 12 hrs in presence of proteasome inhibitor MG132 by Western blot analysis | Homo sapiens | 1 | ALA4251745 | cell-based format | Scientific Literature | |
| 13. | ALA4256566 | B | Inhibition of Notch1 in human HPBALL cells assessed as reduction in HES1 expression after 72 hrs by Western blot analysis | Homo sapiens | 1 | ALA4251745 | cell-based format | Scientific Literature | |
| 14. | ALA4256567 | B | Inhibition of Notch1 in human HPBALL cells assessed as reduction in NICD expression at 0.5 uM after 12 hrs by Western blot analysis | Homo sapiens | 1 | ALA4251745 | cell-based format | Scientific Literature | |
| 15. | ALA4256568 | B | Inhibition of Notch1 in human HPBALL cells assessed as reduction in NICD expression after 72 hrs by Western blot analysis | Homo sapiens | 1 | ALA4251745 | cell-based format | Scientific Literature | |
| 16. | ALA4267500 | B | Inhibition of Notch1 deltaE mutant (unknown origin) expressed in HEK293 cells after 16 hrs by resazurin dye-based luciferase reporter gene assay | Homo sapiens | 24 | ALA4265915 | cell-based format | Scientific Literature | |
| 17. | ALA4267501 | B | Potency index, ratio of FLI-06 IC50 to compound IC50 for inhibition of Notch1 deltaE mutant (unknown origin) | Homo sapiens | 1 | ALA4265915 | single protein format | Scientific Literature | |
| 18. | ALA4340228 | B | Inhibition of NOTCH1 signalling in human KOPTK1 cells harboring activating Notch1 gene mutations assessed as reduction in N1Val protein expression at 2.5 uM incubated for 36 hrs by Western blot analysis | Homo sapiens | 6 | ALA4339229 | cell-based format | Scientific Literature | |
| 19. | ALA4340229 | B | Inhibition of NOTCH1 signalling in human KOPTK1 cells harboring activating Notch1 gene mutations assessed as reduction in DELTEX1 mRNA expression at 2.5 uM incubated for 36 hrs by RT-PCR analysis | Homo sapiens | 6 | ALA4339229 | cell-based format | Scientific Literature | |
| 20. | ALA4619104 | A | Inhibition of human Notch1 expressed in HEK293 cells coexpressing luciferase reporter measured after 20 hrs by chemiluminescence assay | Homo sapiens | 2 | ALA4616706 | cell-based format | Scientific Literature |
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