# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA4767464 | Binding | Inhibition of recombinant human PAK4 kinase domain (300 to 591 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition rate using serine/threonine-20 peptide as substrate at 50 uM incubated for 60 mins in presence of ATP by FRET based Z'-LYTE assay | Homo sapiens | 14 | ALA4765244 | assay format | Scientific Literature | |
2. | ALA4767465 | Binding | Inhibition of recombinant human PAK4 kinase domain (300 to 591 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition rate using serine/threonine-20 peptide as substrate at 5 uM incubated for 60 mins in presence of ATP by FRET based Z'-LYTE assay | Homo sapiens | 14 | ALA4765244 | assay format | Scientific Literature | |
3. | ALA4767466 | Binding | Inhibition of recombinant human PAK4 kinase domain (300 to 591 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition rate using serine/threonine-20 peptide as substrate at 0.5 uM incubated for 60 mins in presence of ATP by FRET based Z'-LYTE assay | Homo sapiens | 14 | ALA4765244 | assay format | Scientific Literature | |
4. | ALA4767467 | Physicochemical | Chemical stability of the compound in pH 7.4 PBS buffer assessed as compound remaining measured after 2 hrs by HPLC analysis | 12 | ALA4765244 | small-molecule physicochemical format | Scientific Literature | ||
5. | ALA4767468 | Unassigned | Chemical stability of the compound in pH 1.2 simulated gastric fluid buffer assessed as compound remaining measured after 2 hrs by HPLC analysis | 12 | ALA4765244 | small-molecule physicochemical format | Scientific Literature | ||
6. | ALA4767469 | Unassigned | Chemical stability of the compound in pH 6.8 simulated intestinal fluid assessed as compound remaining measured after 2 hrs by HPLC analysis | 12 | ALA4765244 | small-molecule physicochemical format | Scientific Literature | ||
7. | ALA4767470 | ADME | Stability of the compound in human plasma assessed as compound remaining measured within 120 mins at 37 degC by HPLC analysis | Homo sapiens | 13 | ALA4765244 | cell-free format | Scientific Literature | |
8. | ALA4767471 | ADME | Prodrug conversion in human plasma assessed as release of active metabolite (R)-(6-chloro-4-(5-cyclopropyl-1H-pyrazol-3-ylamino)quinazolin-2-yl)(3-methylpiperazin-1-yl)methanone hydrochloride measured within 120 mins at 37 degC by HPLC analysis | Homo sapiens | 12 | ALA4765244 | cell-free format | Scientific Literature | |
9. | ALA4767472 | ADME | Stability of the compound in rat liver S9 fraction assessed as compound remaining measured after 60 mins at 37 degC by LC-MS/MS analysis | Rattus norvegicus | 13 | ALA4765244 | subcellular format | Scientific Literature | |
10. | ALA4767473 | ADME | Prodrug conversion in rat liver S9 fraction assessed as release of active metabolite (R)-(6-chloro-4-(5-cyclopropyl-1H-pyrazol-3-ylamino)quinazolin-2-yl)(3-methylpiperazin-1-yl)methanone hydrochloride measured after 60 mins at 37 degC by LC-MS/MS analysis | Rattus norvegicus | 12 | ALA4765244 | subcellular format | Scientific Literature | |
11. | ALA4767474 | ADME | Clearance in Wistar rat assessed as (R)-(6-chloro-4-(5-cyclopropyl-1H-pyrazol-3-ylamino)quinazolin-2-yl)(3-methylpiperazin-1-yl)methanone hydrochloride at 2.5 mg/kg, iv measured upto 24 hrs by LC/MS/MS analysis | Rattus norvegicus | 1 | ALA4765244 | organism-based format | Scientific Literature | |
12. | ALA4767475 | ADME | Initial plasma concentration in Wistar rat assessed as (R)-(6-chloro-4-(5-cyclopropyl-1H-pyrazol-3-ylamino)quinazolin-2-yl)(3-methylpiperazin-1-yl)methanone hydrochloride at 2.5 mg/kg, iv measured upto 24 hrs by LC/MS/MS analysis | Rattus norvegicus | 1 | ALA4765244 | organism-based format | Scientific Literature | |
13. | ALA4767486 | ADME | AUC in Wistar rat assessed as (R)-(6-chloro-4-(5-cyclopropyl-1H-pyrazol-3-ylamino)quinazolin-2-yl)(3-methylpiperazin-1-yl)methanone hydrochloride at 13.5 mg/kg, po measured upto 24 hrs by LC/MS/MS analysis | Rattus norvegicus | 1 | ALA4765244 | organism-based format | Scientific Literature | |
14. | ALA4767487 | ADME | AUC (0 to infinity) in Wistar rat assessed as (R)-(6-chloro-4-(5-cyclopropyl-1H-pyrazol-3-ylamino)quinazolin-2-yl)(3-methylpiperazin-1-yl)methanone hydrochloride at 13.5 mg/kg, po measured upto 24 hrs by LC/MS/MS analysis | Rattus norvegicus | 1 | ALA4765244 | organism-based format | Scientific Literature | |
15. | ALA4767488 | ADME | Half life in Wistar rat assessed as (R)-(6-chloro-4-(5-cyclopropyl-1H-pyrazol-3-ylamino)quinazolin-2-yl)(3-methylpiperazin-1-yl)methanone hydrochloride at 13.5 mg/kg, po measured upto 24 hrs by LC/MS/MS analysis | Rattus norvegicus | 1 | ALA4765244 | organism-based format | Scientific Literature | |
16. | ALA4767489 | ADME | Tmax in Wistar rat assessed as (R)-(6-chloro-4-(5-cyclopropyl-1H-pyrazol-3-ylamino)quinazolin-2-yl)(3-methylpiperazin-1-yl)methanone hydrochloride at 13.5 mg/kg, po measured upto 24 hrs by LC/MS/MS analysis | Rattus norvegicus | 1 | ALA4765244 | organism-based format | Scientific Literature | |
17. | ALA4767490 | ADME | Cmax in Wistar rat assessed as (R)-(6-chloro-4-(5-cyclopropyl-1H-pyrazol-3-ylamino)quinazolin-2-yl)(3-methylpiperazin-1-yl)methanone hydrochloride at 13.5 mg/kg, po measured upto 24 hrs by LC/MS/MS analysis | Rattus norvegicus | 1 | ALA4765244 | organism-based format | Scientific Literature | |
18. | ALA4767502 | ADME | Oral bioavailability in Wistar rat assessed as (R)-(6-chloro-4-(5-cyclopropyl-1H-pyrazol-3-ylamino)quinazolin-2-yl)(3-methylpiperazin-1-yl)methanone hydrochloride at 13.5 mg/kg measured upto 24 hrs by LC/MS/MS analysis | Rattus norvegicus | 1 | ALA4765244 | organism-based format | Scientific Literature | |
19. | ALA4767503 | ADME | Volume of distribution in Wistar rat assessed as (R)-(6-chloro-4-(5-cyclopropyl-1H-pyrazol-3-ylamino)quinazolin-2-yl)(3-methylpiperazin-1-yl)methanone hydrochloride at 2.5 mg/kg, iv measured upto 24 hrs by LC/MS/MS analysis | Rattus norvegicus | 1 | ALA4765244 | organism-based format | Scientific Literature | |
20. | ALA4767504 | ADME | Half life in Wistar rat assessed as (R)-(6-chloro-4-(5-cyclopropyl-1H-pyrazol-3-ylamino)quinazolin-2-yl)(3-methylpiperazin-1-yl)methanone hydrochloride at 2.5 mg/kg, iv measured upto 24 hrs by LC/MS/MS analysis | Rattus norvegicus | 1 | ALA4765244 | organism-based format | Scientific Literature |