# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA4305534 | Binding | Inhibition of recombinant N-terminal His-tagged human FER (SH2 domain to C-terminal) expressed in Escherichia coli assessed as decrease in FL-Peptide22 substrate phosphorylation incubated for 90 mins | Homo sapiens | 21 | ALA4304751 | assay format | Scientific Literature | |
2. | ALA4305535 | Binding | Inhibition of myc/His-tagged ETV6-FER (452 to 821 residues) (unknown origin) expressed in BA/F3 cells assessed as decrease in cell viability after 3 days by luminescence based CellTiter-Glo assay | Homo sapiens | 8 | ALA4304751 | cell-based format | Scientific Literature | |
3. | ALA4305536 | ADME | Growth inhibition of mouse mock transfected BA/F3 cells assessed as decrease in cell viability after 3 days by luminescence based CellTiter-Glo assay | Mus musculus | 6 | ALA4304751 | cell-based format | Scientific Literature | |
4. | ALA4305537 | ADME | Metabolic stability in mouse liver microsomes assessed as parent compound remaining at 1 uM after 30 mins relative to control | Mus musculus | 2 | ALA4304751 | microsome format | Scientific Literature | |
5. | ALA4305538 | Physicochemical | Solubility in buffer at pH 6.8 | 2 | ALA4304751 | small-molecule physicochemical format | Scientific Literature | ||
6. | ALA4305539 | ADME | Protein binding in BALB/c mouse serum at 10 ug/mL incubated for 4 hrs under shaking condition by LC/MS/MS analysis | Mus musculus | 2 | ALA4304751 | cell-free format | Scientific Literature | |
7. | ALA4305540 | ADME | Effective permeability of compound at 5 uM after 24 hrs at pH 7.4 by LC/MS/MS based PAMPA assay | 2 | ALA4304751 | assay format | Scientific Literature | ||
8. | ALA4305541 | ADME | Total plasma clearance in BALB/cAnNCrlCrlj mouse at 1 mg/kg, iv after 24 hrs | Mus musculus | 2 | ALA4304751 | organism-based format | Scientific Literature | |
9. | ALA4305542 | ADME | AUC in BALB/cAnNCrlCrlj mouse at 10 mg/kg, po administered via gavage after 24 hrs | Mus musculus | 2 | ALA4304751 | organism-based format | Scientific Literature | |
10. | ALA4305543 | ADME | Cmax in BALB/cAnNCrlCrlj mouse at 10 mg/kg, po administered via gavage after 24 hrs | Mus musculus | 2 | ALA4304751 | organism-based format | Scientific Literature | |
11. | ALA4305544 | ADME | Oral bioavailability in BALB/cAnNCrlCrlj mouse at 10 mg/kg administered via gavage after 24 hrs | Mus musculus | 2 | ALA4304751 | organism-based format | Scientific Literature | |
12. | ALA4305545 | Functional | Antitumor activity against mouse BA/F3 cells expressing myc/His-tagged ETV6-FER kinase domain (452 to 821 residues) allografted in BALB/cAJcl nu/nu mouse assessed as decrease in tumor volume administered orally once per day for 4 days starting from 6 days after tumor cell implantation and measured during compound dosing | Mus musculus | 1 | ALA4304751 | cell-based format | Scientific Literature | |
13. | ALA4305546 | Toxicity | Toxicity in BALB/cAJcl nu/nu mouse allografted with mouse BA/F3 cells expressing myc/His-tagged ETV6-FER kinase domain (452 to 821 residues) assessed as change in body weight loss at 12.5 to 100 mg/kg, po administered once per day for 4 days starting from 6 days after tumor cell implantation and measured during compound dosing | Mus musculus | 1 | ALA4304751 | organism-based format | Scientific Literature | |
14. | ALA4305547 | ADME | Unbound plasma concentration in BALB/cAnNCrlCrlj mouse at 10 mg/kg, po administered via gavage after 24 hrs by non-compartmental analysis | Mus musculus | 1 | ALA4304751 | organism-based format | Scientific Literature | |
15. | ALA4305548 | Binding | Inhibition of recombinant N-terminal GST-fusion protein tagged human ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system assessed as decrease in fluorescence labelled Srctide phosphorylation at 200 nM by off-chip mobility shift assay relative to control | Homo sapiens | 1 | ALA4304751 | assay format | Scientific Literature | |
16. | ALA4305549 | Binding | Inhibition of recombinant N-terminal GST-fusion protein tagged human FLT3 cytoplasmic domain (564 to 993 residues) expressed in baculovirus expression system assessed as decrease in fluorescence labelled Srctide phosphorylation at 200 nM by off-chip mobility shift assay relative to control | Homo sapiens | 1 | ALA4304751 | assay format | Scientific Literature | |
17. | ALA4305550 | Binding | Inhibition of recombinant N-terminal GST-fusion protein tagged human FMS cytoplasmic domain (538 to 972 residues) expressed in baculovirus expression system assessed as decrease in fluorescence labelled Srctide phosphorylation at 200 nM by off-chip mobility shift assay relative to control | Homo sapiens | 1 | ALA4304751 | assay format | Scientific Literature | |
18. | ALA4305551 | Binding | Inhibition of recombinant N-terminal GST-fusion protein tagged human KIT cytoplasmic domain (544 to 976 residues) expressed in baculovirus expression system assessed as decrease in fluorescence labelled Srctide phosphorylation at 200 nM by off-chip mobility shift assay relative to control | Homo sapiens | 1 | ALA4304751 | assay format | Scientific Literature | |
19. | ALA4305552 | Binding | Inhibition of recombinant N-terminal GST-fusion protein tagged human full length PYK2 (1 to 967 residues) expressed in baculovirus expression system assessed as decrease in fluorescence labelled Blk/Lyntide phosphorylation at 200 nM by off-chip mobility shift assay relative to control | Homo sapiens | 1 | ALA4304751 | assay format | Scientific Literature | |
20. | ALA4305553 | Binding | Inhibition of recombinant N-terminal GST-fusion protein tagged human ROS1 cytoplasmic domain (1883 to 2347 residues) expressed in baculovirus expression system assessed as decrease in fluorescence labelled IRS1 phosphorylation at 200 nM by off-chip mobility shift assay relative to control | Homo sapiens | 1 | ALA4304751 | assay format | Scientific Literature |