# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA4414022 | Binding | Inhibition of SHP2 in human KYSE520 cells assessed as reduction in ERK phosphorylation after 2 hrs by SureFire p-ERK assay | Homo sapiens | 15 | ALA4411331 | cell-based format | Scientific Literature | |
2. | ALA4414023 | Binding | Inhibition of human 6His-tagged SHP2 (1 to 525 residues) expressed in Escherichia coli BL21 Star (DE3) using DiFMUP as surrogate substrate as preincubated for 30 to 60 mins followed by substrate addition and measured after 30 mins bpV-based fluorescence assay | Homo sapiens | 16 | ALA4411331 | assay format | Scientific Literature | |
3. | ALA4414024 | Functional | Antiproliferative activity against human KYSE520 cells added 24 hrs after cell plating and measured on day 5 by Celltiter-Glo assay | Homo sapiens | 15 | ALA4411331 | cell-based format | Scientific Literature | |
4. | ALA4414026 | Binding | Inhibition of human ERG | Homo sapiens | 11 | ALA4411331 | single protein format | Scientific Literature | |
5. | ALA4414027 | ADME | Apparent permeability across apical to basolateral side in human Caco2 cells | Homo sapiens | 3 | ALA4411331 | cell-based format | Scientific Literature | |
6. | ALA4414028 | ADME | Intrinsic clearance in rat liver microsomes | Rattus norvegicus | 3 | ALA4411331 | microsome format | Scientific Literature | |
7. | ALA4414029 | ADME | Half life in rat liver microsomes | Rattus norvegicus | 3 | ALA4411331 | microsome format | Scientific Literature | |
8. | ALA4414030 | ADME | Dose normalized AUC in rat at 1 mg/kg, po | Rattus norvegicus | 2 | ALA4411331 | organism-based format | Scientific Literature | |
9. | ALA4414031 | ADME | Oral bioavailability in rat at 1 mg/kg | Rattus norvegicus | 2 | ALA4411331 | organism-based format | Scientific Literature | |
10. | ALA4414037 | ADME | Intrinsic clearance in mouse liver microsomes | Mus musculus | 1 | ALA4411331 | microsome format | Scientific Literature | |
11. | ALA4414038 | ADME | Half life in mouse liver microsomes | Mus musculus | 1 | ALA4411331 | microsome format | Scientific Literature | |
12. | ALA4414039 | Physicochemical | Aqueous solubility of the compound in 6.8 pH buffer | 2 | ALA4411331 | small-molecule physicochemical format | Scientific Literature | ||
13. | ALA4414040 | ADME | Efflux ratio of apparent permeability in human Caco2 cells | Homo sapiens | 1 | ALA4411331 | cell-based format | Scientific Literature | |
14. | ALA4414041 | Functional | Antiproliferative activity against human Detroit 562 cells after 24 hrs by Celltiter-Glo assay | Homo sapiens | 4 | ALA4411331 | cell-based format | Scientific Literature | |
15. | ALA4414042 | ADME | Drug uptake in human Detroit 562 cells xenografted NU/NU mouse at 20 to 80 mg/kg, po BID | Mus musculus | 1 | ALA4411331 | organism-based format | Scientific Literature | |
16. | ALA4414043 | Functional | In vivo inhibition of SHP2 in human Detroit 562 cells xenografted in NU/NU mouse assessed as reduction in DUSP6 mRNA levels at 20 to 80 mg/kg, po administered BID and measured after 3 hrs by qPCR analysis | Mus musculus | 1 | ALA4411331 | organism-based format | Scientific Literature | |
17. | ALA4414044 | Functional | Antitumor activity against human Detroit 562 cells xenografted in NU/NU mouse assessed as reduction in tumor volume at 20 to 80 mg/kg, po administered BID and measured after 21 days | Homo sapiens | 1 | ALA4411331 | organism-based format | Scientific Literature | |
18. | ALA4414045 | Functional | Antitumor activity against human Detroit 562 cells xenografted in NU/NU mouse assessed as tumor stasis at 40 mg/kg, po administered BID and measured after 21 days relative to control | Homo sapiens | 1 | ALA4411331 | organism-based format | Scientific Literature | |
19. | ALA4414046 | Functional | Antitumor activity against human Detroit 562 cells xenografted in NU/NU mouse assessed as tumor regression at 80 mg/kg, po administered BID and measured after 14 days post dose relative to control | Homo sapiens | 1 | ALA4411331 | organism-based format | Scientific Literature | |
20. | ALA4414050 | ADME | Clearance in rat | Rattus norvegicus | 1 | ALA4411331 | assay format | Scientific Literature |