Reaction Details |
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Target | Gag-Pol polyprotein [600-1027,Y780C]/[600-1155,Y780C] |
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Ligand | BDBM2074 |
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Substrate/Competitor | poly(rC)500:oligo(dG)10 |
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Meas. Tech. | HIV-1 RT Assay |
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pH | 7.8±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 1200±n/a nM |
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Citation | Klunder, JM; Hoermann, M; Cywin, CL; David, E; Brickwood, JR; Schwartz, R; Barringer, KJ; Pauletti, D; Shih, CK; Erickson, DA; Sorge, CL; Joseph, DP; Hattox, SE; Adams, J; Grob, PM Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 7. 8-Arylethyldipyridodiazepinones as potent broad-spectrum inhibitors of wild-type and mutant enzymes. J Med Chem41:2960-71 (1998) [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 [600-1027,Y780C]/[600-1155,Y780C] |
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Name: | Gag-Pol polyprotein [600-1027,Y780C]/[600-1155,Y780C] |
Synonyms: | EC: 2.7.7.49 | HIV-1 Reverse Transcriptase Mutant (Y181C) |
Type: | Protein Complex |
Mol. Mass.: | 115564 |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
Name: | Gag-Pol polyprotein [600-1155,Y780C] |
Synonyms: | HIV-1 Reverse Transcriptase Mutant (Y181C) Chain A | POL_HV1B1 | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 63868.77 |
Organism: | Human immunodeficiency virus type 1 |
Description: | P03366[600-1155,Y780C] |
Residue: | 556 |
Sequence: | PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPV
FAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPL
DEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFKKQNPDIVI
CQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWT
VQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAE
LELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGA
HTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTP
PLVKLWYQLEKEPIVGAETFYVDGAANRETKLGKAGYVTNKGRQKVVPLTNTTNQKTELQ
AIYLALQDSGLEVNIVTDSQYALGIIQAQPDKSESELVNQIIEQLIKKEKVYLAWVPAHK
GIGGNEQVDKLVSAGI
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Component 2 |
Name: | Gag-Pol polyprotein [600-1027,Y780C] |
Synonyms: | HIV-1 Reverse Transcriptase Mutant (Y181C) Chain B | POL_HV1B1 | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 49908.60 |
Organism: | Human immunodeficiency virus type 1 |
Description: | P03366[600-1027,Y780C] |
Residue: | 428 |
Sequence: | PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPV
FAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPL
DEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFKKQNPDIVI
CQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWT
VQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVKQLCKLLRGTKALTEVIPLTEEAE
LELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGA
HTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTP
PLVKLWYQ
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BDBM2074 |
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poly(rC)500:oligo(dG)10 |
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Name: | poly(rC)500:oligo(dG)10 |
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 template:primer. |
Residue: | 3 |
Sequence: | |