Reaction Details |
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Target | Gag-Pol polyprotein [600-1029,C879S]/[600-1159,C879S] |
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Ligand | BDBM17666 |
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Substrate/Competitor | poly(rC)-oligo(dG) |
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Meas. Tech. | HIV-1 RT Enzyme Assay |
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pH | 8±n/a |
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Temperature | 310.15±n/a K |
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IC50 | 110±n/a nM |
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Citation | Morningstar, ML; Roth, T; Farnsworth, DW; Smith, MK; Watson, K; Buckheit, RW; Das, K; Zhang, W; Arnold, E; Julias, JG; Hughes, SH; Michejda, CJ Synthesis, Biological Activity, and Crystal Structure of Potent Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase That Retain Activity against Mutant Forms of the Enzyme. J Med Chem50:4003-4015 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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Gag-Pol polyprotein [600-1029,C879S]/[600-1159,C879S] |
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Name: | Gag-Pol polyprotein [600-1029,C879S]/[600-1159,C879S] |
Synonyms: | HIV-1 Reverse Transcriptase |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | Wild-type p66/p51 HIV-1 RT, derived from BH-10 clone of HIV-1, was expressed in bacteria. |
Components: | This complex has 2 components. |
Component 1 |
Name: | Gag-Pol polyprotein [600-1159,C879S] |
Synonyms: | HIV-1 Reverse Transcriptase Chain A | POL_HV1B1 | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 64425.43 |
Organism: | Human immunodeficiency virus type 1 |
Description: | P03366[600-1159,C879S] |
Residue: | 560 |
Sequence: | PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPV
FAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPL
DEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFKKQNPDIVI
YQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWT
VQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLSKLLRGTKALTEVIPLTEEAE
LELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGA
HTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTP
PLVKLWYQLEKEPIVGAETFYVDGAANRETKLGKAGYVTNKGRQKVVPLTNTTNQKTELQ
AIYLALQDSGLEVNIVTDSQYALGIIQAQPDKSESELVNQIIEQLIKKEKVYLAWVPAHK
GIGGNEQVDKLVSAGIRKIL
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Component 2 |
Name: | Gag-Pol polyprotein [600-1029,C879S] |
Synonyms: | HIV-1 Reverse Transcriptase Chain B | POL_HV1B1 | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 50221.85 |
Organism: | Human immunodeficiency virus type 1 |
Description: | P03366[600-1029,C879S] |
Residue: | 430 |
Sequence: | PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPV
FAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPL
DEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFKKQNPDIVI
YQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWT
VQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLSKLLRGTKALTEVIPLTEEAE
LELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGA
HTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTP
PLVKLWYQLE
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BDBM17666 |
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poly(rC)-oligo(dG) |
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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: | |