Reaction Details |
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Target | Dimer of Gag-Pol polyprotein [489-587] |
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Ligand | BDBM771 |
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Substrate/Competitor | Peptide Substrate |
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Meas. Tech. | Protease Inhibition Assay |
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pH | 5±n/a |
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Temperature | 295.15±n/a K |
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Ki | 15±5 nM |
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Comments | Determination of Ki values with this assay requires analysis under conditions in which substrate concentration resides substantially below Km and the inhibitor concentrations greatly exceeds the Ki value and the enzyme concentration. |
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Citation | Romines, KR; Watenpaugh, KD; Tomich, PK; Howe, WJ; Morris, JK; Lovasz, KD; Mulichak, AM; Finzel, BC; Lynn, JC; Horng, MM Use of medium-sized cycloalkyl rings to enhance secondary binding: discovery of a new class of human immunodeficiency virus (HIV) protease inhibitors. J Med Chem38:1884-91 (1995) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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Dimer of Gag-Pol polyprotein [489-587] |
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Name: | Dimer of Gag-Pol polyprotein [489-587] |
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 [489-587] |
Synonyms: | HIV protease | HIV-1 Protease (NY5-type sequence) | HIV-1 Protease chain A | HIV-1 Protease chain B | POL_HV1N5 | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 10822.21 |
Organism: | Human immunodeficiency virus type 1 |
Description: | P12497[489-587] |
Residue: | 99 |
Sequence: | PQITLWQRPLVTIKIGGQLKEALLDTGADDTVLEEMNLPGRWKPKMIGGIGGFIKVRQYD
QILIEICGHKAIGTVLVGPTPVNIIGRNLLTQIGCTLNF
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Component 2 |
Name: | Gag-Pol polyprotein [489-587] |
Synonyms: | HIV protease | HIV-1 Protease (NY5-type sequence) | HIV-1 Protease chain A | HIV-1 Protease chain B | POL_HV1N5 | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 10822.21 |
Organism: | Human immunodeficiency virus type 1 |
Description: | P12497[489-587] |
Residue: | 99 |
Sequence: | PQITLWQRPLVTIKIGGQLKEALLDTGADDTVLEEMNLPGRWKPKMIGGIGGFIKVRQYD
QILIEICGHKAIGTVLVGPTPVNIIGRNLLTQIGCTLNF
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BDBM771 |
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Peptide Substrate |
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Name: | Peptide Substrate |
Synonyms: | n/a |
Type: | Peptide |
Mol. Mass.: | 1447.64 |
Organism: | n/a |
Description: | The peptide was derivatized with biotin and
fluorescein isothiocyanate at the amino and carboxy termini. |
Residue: | 12 |
Sequence: | |