Target
Dimer of Gag-Pol polyprotein [489-587,L499I,L508Q,K509R,E524D,M525I,S526N,M535I,I539V,I543V,I551V,L552P,A560V,V571A,L579M]
Ligand
BDBM577
Substrate
fluorescence peptide substrate
Meas. Tech.
Fluorometric Activity Assay
pH
5.5±n/a
Temperature
303.15±n/a K
Ki
58±15 nM
Comments
Determined with the fluorometric activity assay.
Citation
 Hanlon, MHPorter, DJFurfine, ESSpaltenstein, ACarter, HLDanger, DShu, AYKaldor, IWMiller, JFSamano, VA Inhibition of wild-type and mutant human immunodeficiency virus type 1 proteases by GW0385 and other arylsulfonamides. Biochemistry 43:14500-7 (2004) [PubMed]  Article 
Target
Name:
Dimer of Gag-Pol polyprotein [489-587,L499I,L508Q,K509R,E524D,M525I,S526N,M535I,I539V,I543V,I551V,L552P,A560V,V571A,L579M]
Synonyms:
HIV-1 Protease Mutant (L10I,L19Q,K20R,E35D,M36I, ..)
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Gag-Pol polyprotein [489-587,L499I,L508Q,K509R,E524D,M525I,S526N,M535I,I539V,I543V,I551V,L552P,A560V,V571A,L579M]
Synonyms:
HIV-1 Protease Mutant (L10I,L19Q,K20R,E35D,M36I, ..) Chain A | HIV-1 Protease Mutant (L10I,L19Q,K20R,E35D,M36I, ..) Chain B | HIV-1 Protease Mutant (L10I,L19Q,K20R,E35D,M36I,S37N,M46I,I50V,I54V,I62V, L63P,A71V,V82A,L90M) | POL_HV1H2 | gag-pol
Type:
Enzyme Subunit
Mol. Mass.:
10760.98
Organism:
Human immunodeficiency virus type 1
Description:
P04585[489-587,L499I,L508Q,K509R,E524D,M525I,S526N,M535I,I539V,I543V,I551V,L552P,A560V,V571A,L579M]
Residue:
99
Sequence:
PQVTLWQRPIVTIKIGGQQREALLDTGADDTVLEDINLPGRWKPKIIGGVGGFVKVRQYDQVPIEICGHKVIGTVLVGPTPANIIGRNLMTQIGCTLNF
  
Component 2
Name:
Gag-Pol polyprotein [489-587,L499I,L508Q,K509R,E524D,M525I,S526N,M535I,I539V,I543V,I551V,L552P,A560V,V571A,L579M]
Synonyms:
HIV-1 Protease Mutant (L10I,L19Q,K20R,E35D,M36I, ..) Chain A | HIV-1 Protease Mutant (L10I,L19Q,K20R,E35D,M36I, ..) Chain B | HIV-1 Protease Mutant (L10I,L19Q,K20R,E35D,M36I,S37N,M46I,I50V,I54V,I62V, L63P,A71V,V82A,L90M) | POL_HV1H2 | gag-pol
Type:
Enzyme Subunit
Mol. Mass.:
10760.98
Organism:
Human immunodeficiency virus type 1
Description:
P04585[489-587,L499I,L508Q,K509R,E524D,M525I,S526N,M535I,I539V,I543V,I551V,L552P,A560V,V571A,L579M]
Residue:
99
Sequence:
PQVTLWQRPIVTIKIGGQQREALLDTGADDTVLEDINLPGRWKPKIIGGVGGFVKVRQYDQVPIEICGHKVIGTVLVGPTPANIIGRNLMTQIGCTLNF
  
Inhibitor
Name:
BDBM577
Synonyms:
(3S)-oxolan-3-yl N-[(2S,3R)-4-[(4-aminobenzene)(2-methylpropyl)sulfonamido]-3-hydroxy-1-phenylbutan-2-yl]carbamate | 141W94 | APV | Agenerase | Amprenavir | BDBM50215393 | CHEMBL116 | VX-478
Type:
Small organic molecule
Emp. Form.:
C25H35N3O6S
Mol. Mass.:
505.627
SMILES:
CC(C)CN(C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)O[C@H]1CCOC1)S(=O)(=O)c1ccc(N)cc1 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
fluorescence peptide substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
3467.28
Organism:
n/a
Description:
n/a
Residue:
30
Sequence:
AMINENYLTHRILENLEPHEPNGLNARGNH