| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA2038874 | B | Inhibition of Tel-fused FMS in mouse BA/F3 cells | Mus musculus | 6 | cell-based format | Scientific Literature | ||
| 2. | ALA961254 | B | Inhibition of Fms-mediated CSF1-stimulated mouse BMDM proliferation by bromodeoxyuridine incorporation assay | Mus musculus | 29 | single protein format | Scientific Literature | ||
| 3. | ALA2163157 | B | Inhibition of FMS-mediated proliferation in CSF1-stimulated bone marrow-derived mouse macrophages assessed as inhibition of incorporation of bromodeoxyuridine into the DNA after 30 hrs by ELISA | Mus musculus | 30 | single protein format | Scientific Literature | ||
| 4. | ALA2213417 | B | Inhibition of CSF1R in mouse M-NFS-60 cells assessed as inhibition of cell proliferation after 72 hrs by Celltiter-Blue assay | Mus musculus | 17 | cell-based format | Scientific Literature | ||
| 5. | ALA3088372 | B | Inhibition of FMS in mouse BMDM cells | Mus musculus | 57 | cell-based format | Scientific Literature | ||
| 6. | ALA3705109 | B | Fluorescence Polarization Competition Assay: A fluorescence polarization competition immunoassay was used to measure compound inhibition of CSF-1R phosphorylation of tyrosine on a synthetic CSF-1R555-568 peptide (SYEGNSYTFIDPTQ). The assay was performed in black 96-well microplates (Cat #42-000-0117, Molecular Devices, Sunnyvale, Calif.). To each well, 5 μL of compound (in 4% DMSO) were mixed with 2 μL of 3.5 nM CSF-1R, 25 mM MgCl2 in assay buffer (100 mM HEPES (hydroxyethylpiperazineethylsodiumsulfonate), pH 7.5, 1 mM DTT (dithiothreitol), 0.01% Tween-20), and 2 μL of 1540 μM peptide in assay buffer. The kinase reaction was initiated by adding 1 μL of 10 mM ATP in assay buffer. The final concentrations in the 10 uL reaction mixture were 100 mM HEPES, pH 7.5, 1 mM DTT, 0.01% Tween-20, 2% DMSO, 308 μM SYEGNSYTFIDPTQ, 1 mM ATP, 5 mM MgCl2, and 0.7 nM CSF-1R. | Mus musculus | 85 | single protein format | BindingDB Database | ||
| 7. | ALA3705295 | B | Fluorescence Polarization Competition Assay: An autophosphorylation, fluroescence polarization competition immunoassay was used to determine the potency for c-fms inhibition. | Mus musculus | 27 | single protein format | BindingDB Database | ||
| 8. | ALA3705422 | B | Fluorescence Polarization Competition Immunoassay: An autophosphorylation, fluorescence polarization competition immunoassay was used to determine the potency for c-fms inhibition exhibited by selected compounds of Formula I. The assay was performed in black 96-well microplates (LJL BioSystems). The assay buffer used was 100 mM 4-(2-hydroxyethyl)piperazine 1-ethanesulfonic acid (HEPES), pH 7.5, 1 mM 1,4-dithio-DL-threitol (DTT), 0.01% (v/v) Tween-20. Compounds were diluted in assay buffer containing 4% dimethylsulfoxide (DMSO) just prior to the assay. To each well, 5 μL of compound were added followed by the addition of 3 μL of a mix containing 33 nM c-fms (Johnson & Johnson PRD) and 16.7 mM MgCl2 (Sigma) in assay buffer. The kinase reaction was initiated by adding 2 μL of 5 mM ATP (Sigma) in assay buffer. The final concentrations in the assay were 10 nM c-fms, 1 mM ATP, 5 mM MgCl2, 2% DMSO. | Mus musculus | 2 | single protein format | BindingDB Database | ||
| 9. | ALA3888751 | B | Fluorescence Polarization Competition Immunoassay: An autophosphorylation, fluorescence polarization competition immunoassay was used to determine the potency for c-fms inhibition exhibited by selected compounds of Formula I. The assay was performed in black 96-well microplates (LJL BioSystems). The assay buffer used was 100 mM 4-(2-hydroxyethyl)piperazine 1-ethanesulfonic acid (HEPES), pH 7.5, 1 mM 1,4-dithio-DL-threitol (DTT), 0.01% (v/v) Tween-20. Compounds were diluted in assay buffer containing 4% dimethylsulfoxide (DMSO) just prior to the assay. To each well, 5 μL of compound were added followed by the addition of 3 μL of a mix containing 33 nM c-fms (Johnson & Johnson PRD) and 16.7 mM MgCl2 (Sigma) in assay buffer. The kinase reaction was initiated by adding 2 μL of 5 mM ATP (Sigma) in assay buffer. The final concentrations in the assay were 10 nM c-fms, 1 mM ATP, 5 mM MgCl2, 2% DMSO. Control reactions were ran in each plate: in positive and negative control wells, assay buffer (made 4% in DMSO) was substituted for the compound; in addition, positive control wells received 1.2 μL of 50 mM ethylenediaminetetraaceticacid (EDTA). The plates were incubated at room temperature for 45 min. At the end of the incubation, the reaction was quenched with 1.2 μL of 50 mM EDTA (EDTA was not added to the positive control wells at this point; see above). Following a 5-min incubation, each well received 10 μL of a 1:1:3 mixture of anti-phosphotyrosine antibody, 10×, PTK green tracer, 10× (vortexed), FP dilution buffer, respectively (all from PanVera, cat. #P2837). The plate was covered, incubated for 30 min at room temperature and the fluorescence polarization was read on the Analyst. The instrument settings were: 485 nm excitation filter; 530 nm emission filter; Z height: middle of well; G factor: 0.93. Under these conditions, the fluorescence polarization values for positive and negative controls were approximately 300 and 150, respectively, and were used to define the 100% and 0% inhibition of the c-fms reaction. | Mus musculus | 44 | single protein format | BindingDB Database | ||
| 10. | ALA3888766 | B | Fluorescence Polarization Competition Immunoassay: An autophosphorylation, fluorescence polarization competition immunoassay was used to determine the potency for c-fms inhibition exhibited by selected compounds of Formula I. The assay was performed in black 96-well microplates (LJL BioSystems). The assay buffer used was 100 mM 4-(2-hydroxyethyl)piperazine 1-ethanesulfonic acid (HEPES), pH 7.5, 1 mM 1,4-dithio-DL-threitol (DTT), 0.01% (v/v) Tween-20. Compounds were diluted in assay buffer containing 4% dimethylsulfoxide (DMSO) just prior to the assay. To each well, 5 μL of compound were added followed by the addition of 3 μL of a mix containing 33 nM c-fms (Johnson & Johnson PRD) and 16.7 mM MgCl2 (Sigma) in assay buffer. The kinase reaction was initiated by adding 2 μL of 5 mM ATP (Sigma) in assay buffer. The final concentrations in the assay were 10 nM c-fms, 1 mM ATP, 5 mM MgCl2, 2% DMSO. Control reactions were ran in each plate: in positive and negative control wells, assay buffer (made 4% in DMSO) was substituted for the compound; in addition, positive control wells received 1.2 μL of 50 mM ethylenediaminetetraaceticacid (EDTA). The plates were incubated at room temperature for 45 min. At the end of the incubation, the reaction was quenched with 1.2 μL of 50 mM EDTA (EDTA was not added to the positive control wells at this point; see above). Following a 5-min incubation, each well received 10 μL of a 1:1:3 mixture of anti-phosphotyrosine antibody, 10×, PTK green tracer, 10× (vortexed), FP dilution buffer, respectively (all from PanVera, cat. # P2837). The plate was covered, incubated for 30 min at room temperature and the fluorescence polarization was read on the Analyst. The instrument settings were: 485 nm excitation filter; 530 nm emission filter; Z height: middle of well; G factor: 0.93. Under these conditions, the fluorescence polarization values for positive and negative controls were approximately 300 and 150, respectively, and were used to define the 100% and 0% inhibition of the c-fms reaction. | Mus musculus | 10 | single protein format | BindingDB Database | ||
| 11. | ALA4038041 | B | Inhibition of CSF1R phosphorylation in mouse RAW264.7 cells preincubated for 6 hrs followed by CSF1 stimulation for 20 mins by Western blot analysis | Mus musculus | 1 | cell-based format | Scientific Literature | ||
| 12. | ALA4038042 | B | Inhibition of CSF1R in mouse RAW264.7 cells assessed as suppression of AKT phosphorylation preincubated for 6 hrs followed by CSF1 stimulation for 20 mins by Western blot analysis | Mus musculus | 1 | cell-based format | Scientific Literature | ||
| 13. | ALA4038043 | B | Inhibition of CSF1R phosphorylation in mouse RAW264.7 cells at 80 nM preincubated for 6 hrs followed by CSF1 stimulation for 20 mins by Western blot analysis relative to control | Mus musculus | 1 | cell-based format | Scientific Literature | ||
| 14. | ALA4038044 | B | Inhibition of CSF1R phosphorylation in mouse RAW264.7 cells assessed as reduction in AKT phosphorylation at 80 nM preincubated for 6 hrs followed by CSF1 stimulation for 20 mins by Western blot analysis relative to control | Mus musculus | 1 | cell-based format | Scientific Literature | ||
| 15. | ALA4256961 | B | Inhibition of c-fms in mouse bone marrow macrophages assessed as reduction in recombinant mouse CSF-1-driven cell proliferation by measuring bromodeoxyuridine incorporation incubated for 30 hrs by ELISA | Mus musculus | 74 | single protein format | Patent Bioactivity Data | ||
| 16. | ALA4256964 | B | Inhibition of c-FMS in mouse BMDM assessed as reduction in CSF-1 stimulated cell proliferation by measuring BrDU incorporation treated for 30 hrs followed by BrDU addition during last 6 hrs of incubation by ELISA | Mus musculus | 2 | single protein format | Patent Bioactivity Data | ||
| 17. | ALA4325647 | B | Inhibition of CSF1R in CSF1-stimulated mouse RAW264.7 cells assessed as reduction in CSF1R phosphorylation preincubated for 6 hrs followed by CSF1 stimulation and measured after 20 mins by Western blot analysis | Mus musculus | 1 | cell-based format | Scientific Literature | ||
| 18. | ALA4325648 | B | Inhibition of CSF1R in CSF1-stimulated mouse RAW264.7 cells assessed as reduction in AKT phosphorylation preincubated for 6 hrs followed by CSF1 stimulation and measured after 20 mins by Western blot analysis | Mus musculus | 1 | cell-based format | Scientific Literature | ||
| 19. | ALA4361187 | B | Inhibition of CSF1R in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | Mus musculus | 1 | assay format | Scientific Literature | ||
| 20. | ALA4424849 | B | Inhibition of CSF1R in CSF1-induced DBA/1J mouse BMMC assessed as reduction in LPS-induced IL6 production preincubated for overnight followed by LPS-stimulation and measured after 6 hrs by ELISA | Mus musculus | 21 | single protein format | Scientific Literature |
The page will load shortly, Thanks for your patience!