Reaction Details |
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Target | Gag-Pol polyprotein [588-1127,Y768C]/[588-1147,Y768C] |
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Ligand | BDBM2483 |
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Substrate/Competitor | poly r(A).oligo d(T)16 |
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Meas. Tech. | Reverse Transcriptase Assay |
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pH | 7.8±n/a |
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Temperature | 310.15±n/a K |
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IC50 | 40±21 nM |
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Citation | Jones, LH; Allan, G; Barba, O; Burt, C; Corbau, R; Dupont, T; Knöchel, T; Irving, S; Middleton, DS; Mowbray, CE; Perros, M; Ringrose, H; Swain, NA; Webster, R; Westby, M; Phillips, C Novel Indazole Non-Nucleoside Reverse Transcriptase Inhibitors Using Molecular Hybridization Based on Crystallographic Overlays (dagger). J Med Chem52:1219-23 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Gag-Pol polyprotein [588-1127,Y768C]/[588-1147,Y768C] |
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Name: | Gag-Pol polyprotein [588-1127,Y768C]/[588-1147,Y768C] |
Synonyms: | EC: 2.7.7.49 | HIV-1 Reverse Transcriptase Mutant (Y181C) |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
Name: | Gag-Pol polyprotein [588-1147,Y768C] |
Synonyms: | HIV-1 Reverse Transcriptase Mutant (Y181C) Chain A | POL_HV1H2 | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 64426.38 |
Organism: | Human immunodeficiency virus type 1 |
Description: | P04585[588-1147,Y768C] |
Residue: | 560 |
Sequence: | PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPV
FAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPL
DEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFRKQNPDIVI
CQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWT
VQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAE
LELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGA
HTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTP
PLVKLWYQLEKEPIVGAETFYVDGAANRETKLGKAGYVTNRGRQKVVTLTDTTNQKTELQ
AIYLALQDSGLEVNIVTDSQYALGIIQAQPDQSESELVNQIIEQLIKKEKVYLAWVPAHK
GIGGNEQVDKLVSAGIRKVL
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Component 2 |
Name: | Gag-Pol polyprotein [588-1127,Y768C] |
Synonyms: | HIV-1 Reverse Transcriptase Mutant (Y181C) Chain B | POL_HV1H2 | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 51277.10 |
Organism: | Human immunodeficiency virus type 1 |
Description: | P04585[588-1127,Y768C] |
Residue: | 440 |
Sequence: | PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPV
FAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPL
DEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFRKQNPDIVI
CQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWT
VQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAE
LELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGA
HTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTP
PLVKLWYQLEKEPIVGAETF
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BDBM2483 |
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poly r(A).oligo d(T)16 |
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Name: | poly r(A).oligo d(T)16 |
Synonyms: | n/a |
Type: | RNA/DNA duplex |
Mol. Mass.: | 358.43 |
Organism: | n/a |
Description: | Tritium-labeled TTP is co-substrate. |
Residue: | 3 |
Sequence: | |