Target
Gag-Pol polyprotein [588-1027]/[588-1147]
Ligand
BDBM1288
Substrate
(poly)rC:(oligo)dG
Meas. Tech.
HIV-1 RT Assay
pH
8.2±n/a
IC50
460±40 nM
Citation
 Saari, WSWai, JSFisher, TEThomas, CMHoffman, JMRooney, CSSmith, AMJones, JHBamberger, DLGoldman, ME Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one. J Med Chem 35:3792-802 (1992) [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:
BDBM1288
Synonyms:
3-Aminopyridin-2(1H)-one analogue 8 | 5-ethyl-6-methyl-3-[(naphthalen-2-ylmethyl)amino]-1,2-dihydropyridin-2-one | CHEMBL318730 | Pyridinone deriv. 10
Type:
Small organic molecule
Emp. Form.:
C19H20N2O
Mol. Mass.:
292.3749
SMILES:
CCc1cc(NCc2ccc3ccccc3c2)c(=O)[nH]c1C
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
(poly)rC:(oligo)dG
Synonyms:
n/a
Type:
RNA-DNA duplex
Mol. Mass.:
358.43
Organism:
n/a
Description:
The incorporation of Tritium-labeled [3H]dGTP onto a (poly)rC:(oligo)dG template:primer.
Residue:
3
Sequence:
NA