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Target
Gag-Pol polyprotein [588-1027]/[588-1147]
Ligand
BDBM10903
Substrate
Poly(C)-oligo(dG)
Meas. Tech.
HIV-1 RT Assay
pH
8±n/a
Temperature
310.15±n/a K
IC50
30±n/a nM
Citation
 Dolle, V; Nguyen, CH; Legraverend, M; Aubertin, AM; Kirn, A; Andreola, ML; Ventura, M; Tarrago-Litvak, L; Bisagni, E Synthesis and antiviral activity of 4-benzyl pyridinone derivatives as potent and selective non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors. J Med Chem 43:3949-62 (2000) [PubMed]  Article 
Target
Name:
Gag-Pol polyprotein [588-1027]/[588-1147]
Synonyms:
EC: 2.7.7.49 | HIV-1 Reverse Transcriptase
Type:
Protein Complex
Mol. Mass.:
115684
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Gag-Pol polyprotein [588-1147]
Synonyms:
HIV-1 Reverse Transcriptase Chain A | POL_HV1H2 | gag-pol
Type:
Enzyme Subunit
Mol. Mass.:
64486.41
Organism:
Human immunodeficiency virus type 1
Description:
P04585[588-1147]
Residue:
560
Sequence:
PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPVFAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPLDEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFRKQNPDIVIYQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWTVQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAELELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGAHTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTPPLVKLWYQLEKEPIVGAETFYVDGAANRETKLGKAGYVTNRGRQKVVTLTDTTNQKTELQAIYLALQDSGLEVNIVTDSQYALGIIQAQPDQSESELVNQIIEQLIKKEKVYLAWVPAHKGIGGNEQVDKLVSAGIRKVL
  
Component 2
Name:
Gag-Pol polyprotein [588-1027]
Synonyms:
HIV-1 Reverse Transcriptase Chain B | POL_HV1H2 | gag-pol
Type:
Enzyme Subunit
Mol. Mass.:
51337.13
Organism:
Human immunodeficiency virus type 1
Description:
P04585[588-1027]
Residue:
440
Sequence:
PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPVFAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPLDEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFRKQNPDIVIYQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWTVQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAELELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGAHTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTPPLVKLWYQLEKEPIVGAETF
  
Inhibitor
Name:
BDBM10903
Synonyms:
4-[(3,5-dimethylphenyl)sulfanyl]-5-ethyl-6-methyl-3-nitro-1,2-dihydropyridin-2-one | 5-ethyl-6-meth | 5-ethyl-6-methyl-3-nitro-4-[(3,5-dimethylphenyl)thio]pyridin-2(1H)-one
Type:
Small organic molecule
Emp. Form.:
C16H18N2O3S
Mol. Mass.:
318.391
SMILES:
CCc1c(C)[nH]c(=O)c(c1Sc1cc(C)cc(C)c1)[N+]([O-])=O
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Poly(C)-oligo(dG)
Synonyms:
Poly(C)-oligo(dG)(5:1)
Type:
RNA-DNA duplex
Mol. Mass.:
358.43
Organism:
n/a
Description:
The incorporation of Tritium-labeled [3H]dGTP onto a (poly)C-(oligo)dG template-primer.
Residue:
3
Sequence:
NA