| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA3887045 | B | Inhibition Assay: Assays for the inhibition of acute HIV infection of T-lymphoid cells were conducted in accordance with Vacca, J.P. et al, Proc. Natl. Acad. Sci. USA 91 : 4096-4100 (1994). Representative compounds of the present invention exhibit inhibition of HIV replication in this assay (also referred to herein as the "spread assay"). For example, as shown by their IC95 values in Table 3 below, some of the compounds set forth in the foregoing Examples were tested in this assay and found to exhibit inhibition of HIV- 1 replication. | 10 | ALA3639148 | cell-based format | BindingDB Database | ||
| 2. | ALA3887078 | B | Inhibition Assay: The inhibition of WT HIV-1 protease was studied using the reaction of the protease (expressed in Eschericia coli) with a peptide substrate [Val-Ser-Gln-Asn-(betanaphthyl)Ala-Pro-Ile-Val (SEQ ID NO:1)]. Compounds were tested using Procedure A. In Procedure A, the test compound was first preincubated with the enzyme in assay buffer (50 mM sodium acetate, pH 5.5, 100 mM NaCl, and 0.1% BSA) for 30 minutes at room temperature. Substrate was then added to 400 micromolar in a total volume of 80 microliters containing 10 picomolar HIV-1 protease and the reaction was incubated for 1 hour at 30° C. The reaction was quenched with the addition of 120 microliters of 10% phosphoric acid. The product formation was determined after separation of product and substrate on a Zorbax Eclipse XDB-C18 column (Agilent Technologies, Santa Clara, Calif.) connected to an Agilent 1100 high performance liquid chromatography system with fluorescence detection (excitation 270 nanometer and emission 330 nanometer). | 130 | ALA3886153 | assay format | BindingDB Database | ||
| 3. | ALA4135243 | B | Inhibition of polymerase activity of recombinant HIV1 reverse polymerase assessed as reduction in extension of an 18 nucleotide DNA primer using template/primer and dNTPs incubated for 30 mins | Human immunodeficiency virus 1 | 21 | ALA4130495 | single protein format | Scientific Literature | |
| 4. | ALA4157399 | B | Binding affinity to HIV1 gag polyprotein V362I mutant containing viral like particle | Human immunodeficiency virus 1 | 2 | ALA4152347 | single protein format | Scientific Literature | |
| 5. | ALA4157400 | B | Binding affinity to HIV1 gag polyprotein V370A mutant containing viral like particle | Human immunodeficiency virus 1 | 2 | ALA4152347 | single protein format | Scientific Literature | |
| 6. | ALA4157401 | B | Binding affinity to HIV1 gag polyprotein delta V370 mutant containing viral like particle | Human immunodeficiency virus 1 | 2 | ALA4152347 | single protein format | Scientific Literature | |
| 7. | ALA4157402 | B | Binding affinity to HIV1 gag polyprotein A364V mutant containing viral like particle | Human immunodeficiency virus 1 | 1 | ALA4152347 | single protein format | Scientific Literature | |
| 8. | ALA4157508 | B | Binding affinity to HIV1 gag polyprotein V370A mutant containing viral like particle assessed as dissociation half life | Human immunodeficiency virus 1 | 2 | ALA4152347 | single protein format | Scientific Literature | |
| 9. | ALA4157509 | B | Binding affinity to HIV1 gag polyprotein delta V370 mutant containing viral like particle assessed as dissociation half life | Human immunodeficiency virus 1 | 2 | ALA4152347 | single protein format | Scientific Literature | |
| 10. | ALA4198589 | B | Inhibition of HIV1 reverse transcriptase polymerase | Human immunodeficiency virus 1 | 2 | ALA4196078 | single protein format | Scientific Literature | |
| 11. | ALA4223422 | B | Binding affinity to CA-SP1 P373S mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells assessed as inhibition of viral maturation by measuring virus yields after 4 to 5 days in presence of 10% FBS by luciferase reporter gene assay | Human immunodeficiency virus 1 | 32 | ALA4219213 | cell-based format | Scientific Literature | |
| 12. | ALA4223423 | B | Binding affinity to CA-SP1 P373S mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells assessed as inhibition of viral maturation by measuring virus yields after 4 to 5 days in presence of 10% FBS/15 mg/ml HSA by luciferase reporter gene assay | Human immunodeficiency virus 1 | 16 | ALA4219213 | cell-based format | Scientific Literature | |
| 13. | ALA4223424 | B | Ratio of EC50 for binding affinity to CA-SP1 P373S mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells in presence of 15 mg/ml HSA to EC50 for binding affinity to CA-SP1 P373S mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells in absence of 15 mg/ml HSA | Human immunodeficiency virus 1 | 16 | ALA4219213 | cell-based format | Scientific Literature | |
| 14. | ALA4223425 | B | Binding affinity to CA-SP1 P373S/V370A double mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells assessed as inhibition of viral maturation by measuring virus yield after 4 to 5 days in presence of 10% FBS by luciferase reporter gene assay | Human immunodeficiency virus 1 | 32 | ALA4219213 | cell-based format | Scientific Literature | |
| 15. | ALA4223431 | B | Binding affinity to CA-SP1 P373S mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells assessed as inhibition of viral maturation by measuring virus yield after 4 to 5 days in presence of 10% FBS/40% human serum by luciferase reporter gene assay | Human immunodeficiency virus 1 | 3 | ALA4219213 | cell-based format | Scientific Literature | |
| 16. | ALA4223432 | B | Ratio of EC50 for binding affinity to CA-SP1 P373S mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells in presence of 40% human serum to EC50 for binding affinity to CA-SP1 P373S mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells in absence of 40% human serum | Human immunodeficiency virus 1 | 3 | ALA4219213 | cell-based format | Scientific Literature | |
| 17. | ALA4223433 | B | Binding affinity to CA-SP1 P373S/V370A double mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells assessed as inhibition of viral maturation by measuring virus yield after 4 to 5 days in presence of 10% FBS/27 mg/ml HSA/40% human serum by luciferase reporter gene assay | Human immunodeficiency virus 1 | 1 | ALA4219213 | cell-based format | Scientific Literature | |
| 18. | ALA4223434 | B | Ratio of EC50 for binding affinity to CA-SP1 P373S//V370A double mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells in presence of 10% FBS/27 mg/ml HSA/40% human serum to EC50 for binding affinity to CA-SP1 P373S//V370A double mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells in absence of 10% FBS/27 mg/ml HSA/40% human serum | Human immunodeficiency virus 1 | 1 | ALA4219213 | cell-based format | Scientific Literature | |
| 19. | ALA4223437 | B | Binding affinity to CA-SP1 P373S/T371A double mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells assessed as inhibition of viral maturation by measuring virus yield after 4 to 5 days in presence of 10% FBS by luciferase reporter gene assay | Human immunodeficiency virus 1 | 3 | ALA4219213 | cell-based format | Scientific Literature | |
| 20. | ALA4223438 | B | Binding affinity to CA-SP1 P373S/V362I double mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells assessed as inhibition of viral maturation by measuring virus yield after 4 to 5 days in presence of 10% FBS by luciferase reporter gene assay | Human immunodeficiency virus 1 | 3 | ALA4219213 | cell-based format | Scientific Literature |
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