| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA3541965 | ADME | Activity of human recombinant N-terminal His-SUMO fused wild type CDA expressed in Escherichia coli BL21(DE3) cells assessed as intrinsic clearance for 2',2'-difluorodeoxyuridine formation by liquid chromatography-tandem mass spectrometry | Homo sapiens | 1 | ALA3525898 | cell-based format | Scientific Literature | |
| 2. | ALA3541966 | ADME | Activity of human recombinant N-terminal His-SUMO fused CDA Ala70Thr mutant expressed in Escherichia coli BL21(DE3) cells assessed as 2',2'-difluorodeoxyuridine formation by liquid chromatography-tandem mass spectrometry | Homo sapiens | 1 | ALA3525898 | cell-based format | Scientific Literature | |
| 3. | ALA3541967 | ADME | Activity of human recombinant N-terminal His-SUMO fused CDA Lys27Gln mutant expressed in Escherichia coli BL21(DE3) cells assessed as 2',2'-difluorodeoxyuridine formation by liquid chromatography-tandem mass spectrometry | Homo sapiens | 1 | ALA3525898 | cell-based format | Scientific Literature | |
| 4. | ALA3541968 | ADME | Activity of human recombinant N-terminal His-SUMO fused wild type CDA expressed in Escherichia coli BL21(DE3) cells assessed as 2',2'-difluorodeoxyuridine formation by liquid chromatography-tandem mass spectrometry | Homo sapiens | 1 | ALA3525898 | cell-based format | Scientific Literature | |
| 5. | ALA3541969 | ADME | Activity of human recombinant N-terminal His-SUMO fused CDA Ala70Thr mutant expressed in Escherichia coli BL21(DE3) cells assessed as intrinsic clearance for arabinofuranosyl uridine formation by liquid chromatography-tandem mass spectrometry | Homo sapiens | 1 | ALA3525898 | cell-based format | Scientific Literature | |
| 6. | ALA3541970 | ADME | Activity of human recombinant N-terminal His-SUMO fused CDA Lys27Gln mutant expressed in Escherichia coli BL21(DE3) cells assessed as intrinsic clearance for arabinofuranosyl uridine formation by liquid chromatography-tandem mass spectrometry | Homo sapiens | 1 | ALA3525898 | cell-based format | Scientific Literature | |
| 7. | ALA3541971 | ADME | Activity of human recombinant N-terminal His-SUMO fused wild type CDA expressed in Escherichia coli BL21(DE3) cells assessed as intrinsic clearance for arabinofuranosyl uridine formation by liquid chromatography-tandem mass spectrometry | Homo sapiens | 1 | ALA3525898 | cell-based format | Scientific Literature | |
| 8. | ALA3541972 | ADME | Activity of human recombinant N-terminal His-SUMO fused CDA Ala70Thr mutant expressed in Escherichia coli BL21(DE3) cells assessed as arabinofuranosyl uridine formation by liquid chromatography-tandem mass spectrometry | Homo sapiens | 1 | ALA3525898 | cell-based format | Scientific Literature | |
| 9. | ALA3541973 | ADME | Activity of human recombinant N-terminal His-SUMO fused CDA Lys27Gln mutant expressed in Escherichia coli BL21(DE3) cells assessed as arabinofuranosyl uridine formation by liquid chromatography-tandem mass spectrometry | Homo sapiens | 1 | ALA3525898 | cell-based format | Scientific Literature | |
| 10. | ALA3541974 | ADME | Activity of human recombinant N-terminal His-SUMO fused wild type CDA expressed in Escherichia coli BL21(DE3) cells assessed as arabinofuranosyl uridine formation by liquid chromatography-tandem mass spectrometry | Homo sapiens | 1 | ALA3525898 | cell-based format | Scientific Literature | |
| 11. | ALA3538245 | ADME | Activity of human recombinant N-terminal His-SUMO fused CDA Ala70Thr mutant expressed in Escherichia coli BL21(DE3) cells assessed as intrinsic clearance for 2',2'-difluorodeoxyuridine formation by liquid chromatography-tandem mass spectrometry | Homo sapiens | 1 | ALA3525898 | cell-based format | Scientific Literature | |
| 12. | ALA3538246 | ADME | Activity of human recombinant N-terminal His-SUMO fused CDA Lys27Gln mutant expressed in Escherichia coli BL21(DE3) cells assessed as intrinsic clearance for 2',2'-difluorodeoxyuridine formation by liquid chromatography-tandem mass spectrometry | Homo sapiens | 1 | ALA3525898 | cell-based format | Scientific Literature | |
| 13. | ALA3705845 | Binding | Enzyme Assay: The procedure to determine CDA enzymatic activity is based on published methodologies (for example, Cacciamani, T. et al., Arch. Biochem. Biophys. 1991, 290, 285-92; Cohen R. et al., J. Biol. Chem., 1971, 246, 7566-8; Vincenzetti S. et al., Protein Expr. Purif. 1996, 8, 247-53). The assay follows the change in absorbance at 286 nm of the CDA-catalyzed deamination of cytidine to form uridine. The reaction is carried out in potassium phosphate buffer (pH 7.4, 20 mM, containing 1mM DTT) in a total volume of 200 μl in a 96-well plate format. The final reaction mixture contains cytidine (50 μM) and purified human recombinant CDA. Purified enzyme is diluted so as to produce an absorbance change of approximately 2 milli-absorbance units/minute. Base line measurements of absorbance change over time are made before CDA addition to insure no change of absorbance in the absence of CDA. After CDA addition, absorbance change is monitored for 20-30 minutes. | Homo sapiens | 9 | ALA3639118 | single protein format | BindingDB Database | |
| 14. | ALA3706053 | Binding | Enzymatic Assay: The cytidine deaminase (CDA) enzymatic assay described by Cacciamani, T. et al., Arch. Biochem. Biophys. 1991, 290, 285-92; Cohen R. et al., J. Biol. Chem., 1971, 246, 7566-8; and Vincenzetti S. et al., Protein Expr. Purif. 1996, 8, 247-53 was used to determine the inhibitory activity (IC50) of compounds described herein. Using this assay, the IC50 of these compounds was determined by following the decrease of substrate (cytidine) caused by the deamination reaction catalyzed by CDA. Disappearance of substrate (cytidine) over time was monitored by the absorbance at 280 nm of the reaction. The assay reaction was carried out in potassium phosphate buffer (pH 7.4, 20 mM, containing 1 mM DTT) in a total volume of 100 ul in a 96-well plate format. The final reaction mixture contained cytidine (50 uM) and purified human recombinant CDA. Purified enzyme was diluted so as to produce an absorbance change of approximately 2 milli-absorbance units/minute. | Homo sapiens | 5 | ALA3638855 | single protein format | BindingDB Database | |
| 15. | ALA872484 | Binding | Binding affinity against cytidine deaminase of human liver | 6 | ALA1121843 | assay format | Scientific Literature | ||
| 16. | ALA665296 | Binding | Binding affinity against cytidine deaminase of human liver; No data | 5 | ALA1121843 | assay format | Scientific Literature | ||
| 17. | ALA665297 | Binding | Cytidine Deaminase Inhibition in human liver | 4 | ALA1121466 | tissue-based format | Scientific Literature | ||
| 18. | ALA665301 | Binding | Compound was tested for its binding affinity against human cytidine deaminase;16-fold less potent than that of zebularine (16.5 uM) | 1 | ALA1131016 | single protein format | Scientific Literature | ||
| 19. | ALA665302 | Binding | Susceptibility to Cyd deaminase at a substrate concentration of 2.0 mM | 4 | ALA1136621 | single protein format | Scientific Literature | ||
| 20. | ALA665306 | Binding | Inhibitory concentration of mouse or human Cytidine deaminase; No inhibition | 1 | ALA1131016 | single protein format | Scientific Literature |
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