# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA866099 | B | Inhibition of Cryptosporidium hominis DHFR | Cryptosporidium hominis | 7 | ALA1145311 | single protein format | Scientific Literature | |
2. | ALA3056823 | B | Ratio of trimethorpin IC50 to compound IC50 for Cryptosporidium parvum recombinant DHFR | Cryptosporidium parvum | 4 | ALA3045961 | single protein format | Scientific Literature | |
3. | ALA3056825 | B | Inhibition of Cryptosporidium parvum recombinant DHFR using dihydrofolate as substrate incubated for 5 min prior to substrate addition by spectrophotometric assay | Cryptosporidium parvum | 12 | ALA3045961 | single protein format | Scientific Literature | |
4. | ALA3136074 | B | Stabilization of Cryptosporidium hominis thymidylate synthase-dihydrofolate reductase assessed as resistance to enzyme sensitivity to trypsin proteolysis at 100 uM by SDS-PAGE mthod | Cryptosporidium hominis | 1 | ALA3132813 | single protein format | Scientific Literature | |
5. | ALA3136075 | B | Destabilization of Cryptosporidium hominis thymidylate synthase-dihydrofolate reductase assessed as increase in enzyme sensitivity to trypsin proteolysis at 750 uM by SDS-PAGE mthod | Cryptosporidium hominis | 1 | ALA3132813 | single protein format | Scientific Literature | |
6. | ALA3136076 | B | Destabilization of Cryptosporidium hominis thymidylate synthase-dihydrofolate reductase assessed as increase in enzyme sensitivity to trypsin proteolysis at 2000 uM by SDS-PAGE mthod | Cryptosporidium hominis | 1 | ALA3132813 | single protein format | Scientific Literature | |
7. | ALA3136078 | B | Inhibition of thymidylate synthase activity of Cryptosporidium hominis thymidylate synthase-dihydrofolate reductase by steady state kinetic assay | Cryptosporidium hominis | 1 | ALA3132813 | single protein format | Scientific Literature | |
8. | ALA3136081 | B | Noncompetitive inhibition of DHFR activity of Cryptosporidium hominis thymidylate synthase-dihydrofolate reductase by Lineweaver-Burk plot | Cryptosporidium hominis | 2 | ALA3132813 | single protein format | Scientific Literature | |
9. | ALA3136082 | B | Noncompetitive inhibition of DHFR activity of Cryptosporidium hominis thymidylate synthase-dihydrofolate reductase assessed as effect on enzyme Km using NADPH substrate by steady state kinetic assay | Cryptosporidium hominis | 2 | ALA3132813 | single protein format | Scientific Literature | |
10. | ALA3136083 | B | Noncompetitive inhibition of DHFR activity of Cryptosporidium hominis thymidylate synthase-dihydrofolate reductase assessed as reduction in enzyme Vmax using NADPH substrate by steady state kinetic assay | Cryptosporidium hominis | 2 | ALA3132813 | single protein format | Scientific Literature | |
11. | ALA3136084 | B | Noncompetitive mixed type inhibition of DHFR activity of Cryptosporidium hominis thymidylate synthase-dihydrofolate reductase assessed as increase in enzyme Km using H2folate substrate by steady state kinetic assay | Cryptosporidium hominis | 2 | ALA3132813 | single protein format | Scientific Literature | |
12. | ALA3136203 | B | Noncompetitive mixed type inhibition of DHFR activity of Cryptosporidium hominis thymidylate synthase-dihydrofolate reductase assessed as reduction in enzyme Vmax using H2folate substrate by steady state kinetic assay | Cryptosporidium hominis | 2 | ALA3132813 | single protein format | Scientific Literature | |
13. | ALA3136204 | B | Inhibition of DHFR activity of Cryptosporidium hominis thymidylate synthase-dihydrofolate reductase by steady state kinetic assay | Cryptosporidium hominis | 2 | ALA3132813 | single protein format | Scientific Literature | |
14. | ALA3364301 | B | Inhibition of thymidylate synthase activity of Cryptosporidium hominis bifunctional dihydrofolate reductase-thymidylate synthase assessed as reduction in conversion of dUMP and CH2H4F to products dTMP and H2F | Cryptosporidium hominis | 1 | ALA3351290 | single protein format | Scientific Literature | |
15. | ALA3364304 | B | Inhibition of DHFR activity of Cryptosporidium hominis bifunctional dihydrofolate reductase-thymidylate synthase assessed as reduction in NADPH oxidation to NAD | Cryptosporidium hominis | 1 | ALA3351290 | single protein format | Scientific Literature | |
16. | ALA3705793 | B | Spectrophotometric Enzyme Assay: Compounds were evaluated in spectrophotometric enzyme assays using ChDHFR-TS and hDHFR. Inhibition constants (IC50) were measured (see Table 4). The lead compound, X, has an inhibition constant of 38 nM and modest selectivity (8-fold). All of the biphenyl compounds are more potent than the initial lead compound X and exhibit greater selectivity for the pathogenic enzyme. The most potent racemic compound, D(rac), a 5′-biphenyl derivative, is also the most selective of the racemic compounds (944-fold). The single R enantiomer of this 5′-biphenyl analog is the most potent (1.1 nM) and most selective (1273-fold) of all known compounds tested against the Cryptosporidium DHFR enzyme. | Cryptosporidium hominis | 11 | ALA3639084 | single protein format | BindingDB Database |