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TargetHIV-1 Protease
LigandBDBM579
Substrate/CompetitorFluorogenic substrate
Meas. Tech.Protease Inhibition Assay
pH6.2±n/a
Temperature310.15±n/a K
Ki 0.0055±n/a nM
Km22000±n/a nM
CommentsThe 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)
Citation Kageyama SMimoto TMurakawa YNomizu MFord HShirasaka TGulnik SErickson JTakada KHayashi H In vitro anti-human immunodeficiency virus (HIV) activities of transition state mimetic HIV protease inhibitors containing allophenylnorstatine. Antimicrob Agents Chemother 37:810-7 (1993) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
HIV-1 Protease
Name:HIV-1 Protease
Synonyms:n/a
Type:Protein Complex
Mol. Mass.:n/a
Description:n/a
Components:This complex has 2 components.
Component 1
Name:HIV-1 Protease chain A
Synonyms:HIV-1 Protease (NY5-type sequence)
Type:Enzyme Subunit
Mol. Mass.:10822.21
Organism:Human immunodeficiency virus type 1
Description:n/a
Residue:99
Sequence:
PQITLWQRPLVTIKIGGQLKEALLDTGADDTVLEEMNLPGRWKPKMIGGIGGFIKVRQYD
QILIEICGHKAIGTVLVGPTPVNIIGRNLLTQIGCTLNF
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Component 2
Name:HIV-1 Protease chain A
Synonyms:HIV-1 Protease (NY5-type sequence)
Type:Enzyme Subunit
Mol. Mass.:10822.21
Organism:Human immunodeficiency virus type 1
Description:n/a
Residue:99
Sequence:
PQITLWQRPLVTIKIGGQLKEALLDTGADDTVLEEMNLPGRWKPKMIGGIGGFIKVRQYD
QILIEICGHKAIGTVLVGPTPVNIIGRNLLTQIGCTLNF
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  Blast E-value cutoff:
BDBM579
Fluorogenic substrate
Name:Fluorogenic substrate
Synonyms:n/a
Type:Peptide
Mol. Mass.:4443.87
Organism:n/a
Description:n/a
Residue:41
Sequence:
Arg-Glu(EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Lys(DABCYL)-Arg