Reaction Details
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Gag-Pol polyprotein [588-1027]/[588-1147]
Ligand
BDBM3363
Substrate
poly(rA):oligo(dT)(12-18)
Meas. Tech.
HIV-1 RT Assay
pH
8±n/a
Temperature
310.15±n/a K
IC50
1300±n/a nM
Comments
In this assay, AZT triphosphate and Nevirapine were employed as positive controls, and have IC50s of 20 nM and 280 nM, respectively
Citation
Livermore, DG; Bethell, RC; Cammack, N; Hancock, AP; Hann, MM; Green, DV; Lamont, RB; Noble, SA; Orr, DC; Payne, JJ Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines. J Med Chem 36:3784-94 (1993) [PubMed] Article More Info.:
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:
BDBM3363
Synonyms:
5-{2-chloro-5-methylimidazo[1,5-a]pyridazin-7-yl}pentyl benzoate | Imidazopyridazine 15a
Type:
Small organic molecule
Emp. Form.:
C19H20ClN3O2
Mol. Mass.:
357.834
SMILES:
Cc1nc(CCCCCOC(=O)c2ccccc2)n2nc(Cl)ccc12
Structure:
Substrate
Name:
poly(rA):oligo(dT)(12-18)
Synonyms:
n/a
Type:
RNA/DNA duplex
Mol. Mass.:
358.43
Organism:
n/a
Description:
[alpha-35S]TTP as co-substrate.
Residue:
3
Sequence:
NA