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Target
Gag-Pol polyprotein [588-1027,K691N,Y769C]/[588-1147,K691N,Y769C]
Ligand
BDBM27588
Substrate
poly rC/biotin-dG15
Meas. Tech.
Reverse Transcriptase Assay
IC50
1390±n/a nM
Citation
 Gagnon, A; Landry, S; Coulombe, R; Jakalian, A; Guse, I; Thavonekham, B; Bonneau, PR; Yoakim, C; Simoneau, B Investigation on the role of the tetrazole in the binding of thiotetrazolylacetanilides with HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases. Bioorg Med Chem Lett 19:1199-205 (2009) [PubMed]  Article 
Target
Name:
Gag-Pol polyprotein [588-1027,K691N,Y769C]/[588-1147,K691N,Y769C]
Synonyms:
HIV-1 Reverse Transcriptase Mutant (103N/181C)
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Gag-Pol polyprotein [588-1147,K691N,Y769C]
Synonyms:
HIV-1 Reverse Transcriptase Mutant (103N/181C) Chain A | POL_HV1H2 | gag-pol
Type:
Enzyme Subunit
Mol. Mass.:
64411.30
Organism:
Human immunodeficiency virus type 1
Description:
P04585[588-1147,K691N,Y769C]
Residue:
560
Sequence:
PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPVFAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKNKSVTVLDVGDAYFSVPLDEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFRKQNPDIVICQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWTVQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAELELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGAHTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTPPLVKLWYQLEKEPIVGAETFYVDGAANRETKLGKAGYVTNRGRQKVVTLTDTTNQKTELQAIYLALQDSGLEVNIVTDSQYALGIIQAQPDQSESELVNQIIEQLIKKEKVYLAWVPAHKGIGGNEQVDKLVSAGIRKVL
  
Component 2
Name:
Gag-Pol polyprotein [588-1027,K691N,Y769C]
Synonyms:
HIV-1 Reverse Transcriptase Mutant (103N/181C) Chain B | POL_HV1H2 | gag-pol
Type:
Enzyme Subunit
Mol. Mass.:
51262.02
Organism:
Human immunodeficiency virus type 1
Description:
P04585[588-1027,K691N,Y769C]
Residue:
440
Sequence:
PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPVFAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKNKSVTVLDVGDAYFSVPLDEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFRKQNPDIVICQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWTVQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAELELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGAHTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTPPLVKLWYQLEKEPIVGAETF
  
Inhibitor
Name:
BDBM27588
Synonyms:
2-[4-(3-chloro-4-{2-[2-(2-chloro-4-methylphenyl)phenoxy]acetamido}phenyl)phenyl]acetic acid | phenylether compound, 11
Type:
Small organic molecule
Emp. Form.:
C29H23Cl2NO4
Mol. Mass.:
520.403
SMILES:
Cc1ccc(c(Cl)c1)-c1ccccc1OCC(=O)Nc1ccc(cc1Cl)-c1ccc(CC(O)=O)cc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
poly rC/biotin-dG15
Synonyms:
n/a
Type:
RNA/DNA duplex
Mol. Mass.:
358.43
Organism:
n/a
Description:
The incorporation of [3H]dGTP onto a (poly)rC:(biotin)dG template:primer.
Residue:
3
Sequence:
NA