# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA1273510 | Binding | Binding affinity Bcl-xL at 200 uM by one-dimensional 1H nuclear magnetic resonance spectroscopy | 17 | ALA1269007 | single protein format | Scientific Literature | ||
2. | ALA1273511 | Functional | Cytotoxicity against human PC3 cells expressing high level of Bcl-xL after 72 hrs by ATP-LITE assay | Homo sapiens | 17 | ALA1269007 | cell-based format | Scientific Literature | |
3. | ALA1273512 | Functional | Cytotoxicity against human H460 cells expressing high level of Bcl-2 after 72 hrs by ATP-LITE assay | Homo sapiens | 17 | ALA1269007 | cell-based format | Scientific Literature | |
4. | ALA1273513 | Functional | Cytotoxicity against human H1299 cells expressing high level of Mcl-1 after 72 hrs by ATP-LITE assay | Homo sapiens | 17 | ALA1269007 | cell-based format | Scientific Literature | |
5. | ALA1273514 | Functional | Cytotoxicity against human BP3 cells expressing high level of Bfl-1 and Mcl-1 after 72 hrs by annexin V-FITC and propidium iodide staining | Homo sapiens | 17 | ALA1269007 | cell-based format | Scientific Literature | |
6. | ALA1273515 | Functional | Cytotoxicity against human RS4:11 cells expressing high level of Bcl-2 and Bcl-xL after 72 hrs by annexin V-FITC and propidium iodide staining | Homo sapiens | 17 | ALA1269007 | cell-based format | Scientific Literature | |
7. | ALA1273516 | Binding | Displacement of F-BakBH3 from Bcl-xL after 30 mins by fluorescence polarization assay | 12 | ALA1269007 | single protein format | Scientific Literature | ||
8. | ALA1273517 | Binding | Displacement of F-BakBH3 from Bcl-2 after 30 mins by fluorescence polarization assay | 12 | ALA1269007 | single protein format | Scientific Literature | ||
9. | ALA1273518 | Binding | Displacement of F-BakBH3 from Bfl-1 after 30 mins by fluorescence polarization assay | 12 | ALA1269007 | single protein format | Scientific Literature | ||
10. | ALA1273519 | Binding | Displacement of F-BakBH3 from Mcl-1 after 30 mins by fluorescence polarization assay | 12 | ALA1269007 | single protein format | Scientific Literature | ||
11. | ALA1273520 | Binding | Binding affinity Bcl-xL by isothermal titration calorimetry assay | 12 | ALA1269007 | single protein format | Scientific Literature | ||
12. | ALA1273521 | ADME | Metabolic stability of the compound in rat plasma after 40 mins | Rattus norvegicus | 8 | ALA1269007 | cell-free format | Scientific Literature | |
13. | ALA1273522 | ADME | Metabolic stability of the compound in rat microsomes after 40 mins | Rattus norvegicus | 8 | ALA1269007 | microsome format | Scientific Literature | |
14. | ALA1273523 | ADME | Permeability of the compound by PAMPA | 8 | ALA1269007 | assay format | Scientific Literature | ||
15. | ALA1273526 | Functional | Reduction of spleen weight in ip dosed human Bcl2 expressing B6 transgenic BALB/c mouse administered as single dose after 24 hrs | Mus musculus | 17 | ALA1269007 | organism-based format | Scientific Literature | |
16. | ALA1273530 | Toxicity | Toxicity in human Bcl2 expressing B6 transgenic BALB/c mouse assessed as mortality at 60 umol/kg, ip administered as single dose after 24 hrs | Mus musculus | 3 | ALA1269007 | organism-based format | Scientific Literature | |
17. | ALA1273531 | Toxicity | Toxicity in human Bcl2 expressing B6 transgenic BALB/c mouse assessed as mortality at 30 umol/kg, ip administered as single dose after 24 hrs | Mus musculus | 3 | ALA1269007 | organism-based format | Scientific Literature | |
18. | ALA3705614 | Binding | Fluorescence Polarization Assay: A Bak BH3 peptide (F-BakBH3) (GQVGRQLAIIGDDINR (SEQ ID NO:1)) was labeled at the N-terminus with fluorescein isothiocyanate (FITC) (Molecular Probes) and purified by HPLC. For competitive binding assays, 100 nM GST-BCL-XL DTM protein was preincubated with the tested compound at varying concentrations in 47.5 uL PBS (pH=7.4) in 96-well black plates at room temperature for 10 min, then 2.5 uL of 100 nM FITC-labeled Bak BH3 peptide was added to produce a final volume of 50 uL. The wild-type and mutant Bak BH3 peptides were included in each assay plate as positive and negative controls, respectively. After 30 min incubation at room temperature, the polarization values in millipolarization units were measured at excitation/emission wavelengths of 480/535 nm with a multilabel plate reader (PerkinElmer). IC50 was determined by fitting the experimental data to a sigmoidal dose-response nonlinear regression model. | Homo sapiens | 12 | ALA3638406 | single protein format | BindingDB Database | |
19. | ALA3707868 | Binding | Fluorescence Polarization Assay: A Bak BH3 peptide (F-BakBH3) (GQVGRQLAIIGDDINR (SEQ ID NO:1)) was labeled at the N-terminus with fluorescein isothiocyanate (FITC) (Molecular Probes) and purified by HPLC. For competitive binding assays, 100 nM GST-BCL-XL DTM protein was preincubated with the tested compound at varying concentrations in 47.5 uL PBS (pH=7.4) in 96-well black plates at room temperature for 10 min, then 2.5 uL of 100 nM FITC-labeled Bak BH3 peptide was added to produce a final volume of 50 uL. The wild-type and mutant Bak BH3 peptides were included in each assay plate as positive and negative controls, respectively. After 30 min incubation at room temperature, the polarization values in millipolarization units were measured at excitation/emission wavelengths of 480/535 nm with a multilabel plate reader (PerkinElmer). IC50 was determined by fitting the experimental data to a sigmoidal dose-response nonlinear regression model. | Homo sapiens | 12 | ALA3638406 | single protein format | BindingDB Database | |
20. | ALA3707894 | Binding | Fluorescence Polarization Assay: A Bak BH3 peptide (F-BakBH3) (GQVGRQLAIIGDDINR (SEQ ID NO:1)) was labeled at the N-terminus with fluorescein isothiocyanate (FITC) (Molecular Probes) and purified by HPLC. For competitive binding assays, 100 nM GST-BCL-XL DTM protein was preincubated with the tested compound at varying concentrations in 47.5 uL PBS (pH=7.4) in 96-well black plates at room temperature for 10 min, then 2.5 uL of 100 nM FITC-labeled Bak BH3 peptide was added to produce a final volume of 50 uL. The wild-type and mutant Bak BH3 peptides were included in each assay plate as positive and negative controls, respectively. After 30 min incubation at room temperature, the polarization values in millipolarization units were measured at excitation/emission wavelengths of 480/535 nm with a multilabel plate reader (PerkinElmer). IC50 was determined by fitting the experimental data to a sigmoidal dose-response nonlinear regression model. | Homo sapiens | 12 | ALA3638406 | single protein format | BindingDB Database |
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