| Reaction Details |
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 | Report a problem with these data |
| Target | Dimer of Gag-Pol polyprotein [489-587] |
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| Ligand | BDBM793 |
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| Substrate/Competitor | Fluorogenic substrate |
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| Meas. Tech. | Protease Inhibition Assay |
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| pH | 6.2±n/a |
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| Temperature | 310.15±n/a K |
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| Ki | 0.0068±n/a nM |
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| Km | 22000±n/a nM |
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| Comments | The estimated Ki value is approximately 1,000 times lower than the IC50 reported in Chem. Pharm. Bull. 40:2251-2253. This discrepancy can be explained by the fact that apparent IC50 will exceed actual Ki value for tight-binding inhibitor when the enzyme concentrationis higher than the Ki value. In general, the lower the Ki, thegreater will be the discrepancy. In addition, Ki values for HIV protease inhibitors are known to be lower at higher ionic strengths (Antiviral Chem. Chemother. 2:65-73) |
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| Citation |  Kageyama, S; Mimoto, T; Murakawa, Y; Nomizu, M; Ford, H; Shirasaka, T; Gulnik, S; Erickson, J; Takada, K; Hayashi, H In vitro anti-human immunodeficiency virus (HIV) activities of transition state mimetic HIV protease inhibitors containing allophenylnorstatine. Antimicrob Agents Chemother37:810-7 (1993) [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] |
|---|
| Name: | Dimer of Gag-Pol polyprotein [489-587] |
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| Synonyms: | HIV-1 Protease |
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| Type: | Protein Complex |
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| Mol. Mass.: | n/a |
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| Description: | n/a |
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| Components: | This complex has 2 components. |
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| 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 |
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| Type: | Enzyme Subunit |
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| Mol. Mass.: | 10822.21 |
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| Organism: | Human immunodeficiency virus type 1 |
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| Description: | P12497[489-587] |
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| Residue: | 99 |
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| 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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| BDBM793 |
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| Fluorogenic substrate |
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| Name: | Fluorogenic substrate |
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| Synonyms: | n/a |
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| Type: | Peptide |
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| Mol. Mass.: | 4443.87 |
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| Organism: | n/a |
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| Description: | n/a |
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| Residue: | 41 |
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| Sequence: | Arg-Glu(EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Lys(DABCYL)-Arg
|
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