Reaction Details |
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Target | Gag-Pol polyprotein [588-1027,K690N]/[588-1147,K690N] |
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Ligand | BDBM2483 |
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Substrate/Competitor | poly(rC)-oligo(dG)(12-18) |
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Meas. Tech. | HIV-1 RT 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 | 3400±300 nM |
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Citation | Silvestri, R; De Martino, G; La Regina, G; Artico, M; Massa, S; Vargiu, L; Mura, M; Loi, AG; Marceddu, T; La Colla, P Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies. J Med Chem46:2482-93 (2003) [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 [588-1027,K690N]/[588-1147,K690N] |
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Name: | Gag-Pol polyprotein [588-1027,K690N]/[588-1147,K690N] |
Synonyms: | EC: 2.7.7.49 | HIV-1 Reverse Transcriptase Mutant (K103N) |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
Name: | Gag-Pol polyprotein [588-1147,K690N] |
Synonyms: | HIV-1 Reverse Transcriptase Mutant (K103N) Chain A | POL_HV1H2 | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 64471.33 |
Organism: | Human immunodeficiency virus type 1 |
Description: | P04585[588-1147,K690N] |
Residue: | 560 |
Sequence: | PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPV
FAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKNKSVTVLDVGDAYFSVPL
DEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFRKQNPDIVI
YQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWT
VQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAE
LELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGA
HTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTP
PLVKLWYQLEKEPIVGAETFYVDGAANRETKLGKAGYVTNRGRQKVVTLTDTTNQKTELQ
AIYLALQDSGLEVNIVTDSQYALGIIQAQPDQSESELVNQIIEQLIKKEKVYLAWVPAHK
GIGGNEQVDKLVSAGIRKVL
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Component 2 |
Name: | Gag-Pol polyprotein [588-1027,K690N] |
Synonyms: | HIV-1 Reverse Transcriptase Mutant (K103N) Chain B | POL_HV1H2 | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 51280.01 |
Organism: | Human immunodeficiency virus type 1 |
Description: | P04585[588-1027,K690N] |
Residue: | 440 |
Sequence: | PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPV
FAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKNKSVTVLDVGDAYFSVPL
DEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFKKQNPDIVI
YQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWT
VQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAE
LELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGA
HTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTP
PLVKLWYNLEKEPIVGAETF
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BDBM2483 |
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poly(rC)-oligo(dG)(12-18) |
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Name: | poly(rC)-oligo(dG)(12-18) |
Synonyms: | n/a |
Type: | RNA/DNA duplex |
Mol. Mass.: | 358.43 |
Organism: | n/a |
Description: | The incorporation of Tritium-labeled dGTP onto a poly(rC)-oligo(dG)(12-18) template-primer
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Residue: | 3 |
Sequence: | |