Ki Summary new BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetHIV-1 Protease
LigandBDBM517
Substrate/CompetitorHIV Peptide Substrate
Meas. Tech.Protease Inhibition Assay
pH5.6±n/a
Temperature310.15±n/a K
Ki 0.6±0.1 nM
Km36000±8000 nM
CommentsKcat/Km=7520 min-1nM-1
Citation Kovalevsky AYTie YLiu FBoross PIWang YFLeshchenko SGhosh AKHarrison RWWeber IT Effectiveness of nonpeptide clinical inhibitor TMC-114 on HIV-1 protease with highly drug resistant mutations D30N, I50V, and L90M. J Med Chem 49:1379-87 (2006) [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:n/a
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
Component 2
Name:HIV-1 Protease chain A
Synonyms:n/a
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM517
HIV Peptide Substrate
Name:HIV Peptide Substrate
Synonyms:n/a
Type:Peptide
Mol. Mass.:3156.95
Organism:n/a
Description:n/a
Residue:27
Sequence:
Ac-RE(Edans)SQNY*PIVRK(Dabcyl)R-CO-NH2