| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA3887380 | B | Enzyme Inhibition Assay: For enzymology studies of these compounds, recombinant guinea pig liver TGase was expressed in Escherichia coli and effectively purified (Gillet, S. M. F. G. et al J. N., Prot. Exp. & Purif. 2004, 33, 256). In addition to being easy to obtain in excellent yield and solubility, guinea pig liver TGase was chosen because it shows 80% homology with human tissue TGase (Aeschlimann, D.; Paulsson, M., Throm. Haemost. 1994, 71, 402) and may thus serve as a model for the evaluation of inhibitors of potential therapeutic utility.The IC50 values of synthetic analogues 14a-38a were determined from inhibition of the reaction of 54.4 mM of the chromogenic TGase substrate N-Cbz-Glu(γ-p-nitrophenyl ester)Gly with 0.010 U of recombinant guinea pig liver TGase as previously reported (Leblanc, A.; Gravel, C.; Labelle, J.; Keillor, J. W. Biochemistry 2001, 40, 8335) and described in detail in the Materials section below. The mode of inhibition was determined for the representative lead compound. | 51 | assay format | BindingDB Database | |||
| 2. | ALA4138602 | B | Inhibition of guinea pig liver transglutaminase 2 | Cavia porcellus | 4 | assay format | Scientific Literature | ||
| 3. | ALA4138603 | B | Inhibition of human transglutaminase 2 | Homo sapiens | 2 | single protein format | Scientific Literature | ||
| 4. | ALA4138604 | P | Drug metabolism assessed as reactivity with GSH by measuring glutathione adduct formation in DMSO-d6 at 12 mM after 10 mins by 1H NMR spectroscopy and mass spectrometry | 2 | small-molecule physicochemical format | Scientific Literature | |||
| 5. | ALA4138607 | B | Inhibition of guinea pig liver transglutaminase 2 using N-Cbz-Glu(gamma-p-nitrophenylester)Gly (AL5) substrate measured over 10 mins by UV-visible spectrophotometry | Cavia porcellus | 2 | assay format | Scientific Literature | ||
| 6. | ALA4138610 | B | Competitive inhibition of human transglutaminase 2 using N-Cbz-Glu(gamma-p-nitrophenylester)Gly (AL5) substrate measured over 10 mins by UV-visible spectrophotometry based Michaelis-Menten analysis | Homo sapiens | 3 | single protein format | Scientific Literature |
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