| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA4386479 | F | Antiproliferative activity against human GISTT1 cells harboring heterozygous V560-Y578 deletion mutant assessed as reduction in cell viability by MTS assay | Homo sapiens | 16 | ALA4385613 | cell-based format | Scientific Literature | |
| 2. | ALA4386480 | F | Decrease in c-KIT phosphorylation in NOD-SCID mouse xenografted with human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant at 80 mg/kg, po measured after 8 hrs by immunoblotting analysis relative to control | Mus musculus | 1 | ALA4385613 | organism-based format | Scientific Literature | |
| 3. | ALA4386481 | F | Decrease in c-KIT phosphorylation in NOD-SCID mouse xenografted with human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant at 20 mg/kg, po measured after 8 hrs by immunoblotting analysis relative to control | Mus musculus | 1 | ALA4385613 | organism-based format | Scientific Literature | |
| 4. | ALA4386482 | F | Antitumor activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant xenografted in NOD-SCID mouse assessed as reduction in tumor size at 25, po administered for 2 weeks with 2 days rest after day 5 and measured thrice per week up to 14 days during compound dosing relative to control | Homo sapiens | 1 | ALA4385613 | organism-based format | Scientific Literature | |
| 5. | ALA4386483 | F | Antitumor activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant xenografted in NOD-SCID mouse assessed as tumor growth inhibition at 25 mg/kg, po administered for 2 weeks with 2 days rest after day 5 and measured thrice per week up to 21 days during compound dosing | Homo sapiens | 1 | ALA4385613 | organism-based format | Scientific Literature | |
| 6. | ALA4386484 | B | Inhibition of human c-KIT JM domain exon 11 V560G single mutant using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay | Homo sapiens | 1 | ALA4385613 | single protein format | Scientific Literature | |
| 7. | ALA4386485 | B | Inhibition of recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation measured after 150 mins in presence of ATP by ADP-glo based luminescence assay | Homo sapiens | 16 | ALA4385613 | cell-based format | Scientific Literature | |
| 8. | ALA4386486 | B | Inhibition of ATP-activated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 30 mins followed by ATP addition and measured after 30 mins by Kinase Glo based luminescence assay | Homo sapiens | 3 | ALA4385613 | cell-based format | Scientific Literature | |
| 9. | ALA4386487 | B | Inhibition of unactivated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 30 mins followed by ATP addition and measured after 120 mins by Kinase Glo based luminescence assay | Homo sapiens | 3 | ALA4385613 | cell-based format | Scientific Literature | |
| 10. | ALA4386488 | B | Inhibition of human c-KIT ATP binding domain exon 13 V654A single mutant using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay | Homo sapiens | 1 | ALA4385613 | single protein format | Scientific Literature | |
| 11. | ALA4386489 | B | Inhibition of human c-KIT ATP binding domain exon 13 V654A single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | Homo sapiens | 2 | ALA4385613 | single protein format | Scientific Literature | |
| 12. | ALA4386490 | B | Inhibition of human c-KIT JM domain exon 11 V560G single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | Homo sapiens | 2 | ALA4385613 | single protein format | Scientific Literature | |
| 13. | ALA4386491 | B | Inhibition of human c-KIT JM domain exon 11 V560G single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | Homo sapiens | 2 | ALA4385613 | single protein format | Scientific Literature | |
| 14. | ALA4386492 | B | Inhibition of human c-KIT ATP binding domain exon 13 V654A single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | Homo sapiens | 2 | ALA4385613 | single protein format | Scientific Literature | |
| 15. | ALA4386493 | B | Inhibition of human c-KIT ATP binding domain exon 13 K642E single mutant using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay | Homo sapiens | 1 | ALA4385613 | single protein format | Scientific Literature | |
| 16. | ALA4386494 | B | Inhibition of human c-KIT ATP binding domain exon 13 K642E single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | Homo sapiens | 2 | ALA4385613 | single protein format | Scientific Literature | |
| 17. | ALA4386495 | B | Inhibition of human c-KIT ATP binding domain exon 13 K642E single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | Homo sapiens | 2 | ALA4385613 | single protein format | Scientific Literature | |
| 18. | ALA4386496 | B | Inhibition of human c-KIT ATP binding domain exon 14 T670I single mutant using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay | Homo sapiens | 1 | ALA4385613 | single protein format | Scientific Literature | |
| 19. | ALA4386497 | B | Inhibition of human c-KIT ATP binding domain exon 14 T670I single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | Homo sapiens | 2 | ALA4385613 | single protein format | Scientific Literature | |
| 20. | ALA4386498 | B | Inhibition of human c-KIT ATP binding domain exon 14 T670I single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | Homo sapiens | 2 | ALA4385613 | single protein format | Scientific Literature |
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