Reaction Details |
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Target | Dimer of Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A] |
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Ligand | BDBM9185 |
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Substrate/Competitor | HIV Protease substrate |
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Meas. Tech. | Protease Inhibition Assay |
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pH | 6.4±n/a |
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Temperature | 298.15±n/a K |
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Ki | 0.13±n/a nM |
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IC50 | 550±50 nM |
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Citation | Sherrill, RG; Andrews, CW; Bock, WJ; Davis-Ward, RG; Furfine, ES; Hazen, RJ; Rutkowske, RD; Spaltenstein, A; Wright, LL Optimization of pyrrolidinone based HIV protease inhibitors. Bioorg Med Chem Lett15:81-4 (2005) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Dimer of Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A] |
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Name: | Dimer of Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A] |
Synonyms: | HIV-1 Protease |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
Name: | Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A] |
Synonyms: | HIV-1 Protease chain A | POL_HV1BR | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 10732.11 |
Organism: | Human immunodeficiency virus type 1 |
Description: | The HIV-1 protease (Genbank HIVHXB2CG) clone was constructed with the substitutions Q7K, L33I, and L63I, to minimize the autoproteolysis of the protease, and C67A and C95A, to prevent cysteine-thiol oxidation. |
Residue: | 99 |
Sequence: | PQITLWKRPLVTIKIGGQLKEALLDTGADDTVIEEMSLPGRWKPKMIGGIGGFIKVRQYD
QIIIEIAGHKAIGTVLVGPTPVNIIGRNLLTQIGATLNF
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Component 2 |
Name: | Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A] |
Synonyms: | HIV-1 Protease chain A | POL_HV1BR | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 10732.11 |
Organism: | Human immunodeficiency virus type 1 |
Description: | The HIV-1 protease (Genbank HIVHXB2CG) clone was constructed with the substitutions Q7K, L33I, and L63I, to minimize the autoproteolysis of the protease, and C67A and C95A, to prevent cysteine-thiol oxidation. |
Residue: | 99 |
Sequence: | PQITLWKRPLVTIKIGGQLKEALLDTGADDTVIEEMSLPGRWKPKMIGGIGGFIKVRQYD
QIIIEIAGHKAIGTVLVGPTPVNIIGRNLLTQIGATLNF
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BDBM9185 |
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HIV Protease substrate |
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Name: | HIV Protease substrate |
Synonyms: | Fluorogenic Peptide Substrate |
Type: | Peptide |
Mol. Mass.: | 3467.28 |
Organism: | n/a |
Description: | n/a |
Residue: | 30 |
Sequence: | 2-(aminobenzoyl)-Thr-Ile-Nle-Phe(p-NO2)-Gln-ArgNH2
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