Reaction Details |
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Target | Gag-Pol polyprotein |
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Ligand | BDBM25352 |
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Substrate/Competitor | Biotinylated Target DNA |
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Meas. Tech. | Microtiter Plate Assay for Strand Transfer |
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pH | 7.8±n/a |
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Temperature | 310.15±n/a K |
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IC50 | 4±n/a nM |
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Citation | Summa, V; Petrocchi, A; Bonelli, F; Crescenzi, B; Donghi, M; Ferrara, M; Fiore, F; Gardelli, C; Gonzalez Paz, O; Hazuda, DJ; Jones, P; Kinzel, O; Laufer, R; Monteagudo, E; Muraglia, E; Nizi, E; Orvieto, F; Pace, P; Pescatore, G; Scarpelli, R; Stillmock, K; Witmer, MV; Rowley, M Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection. J Med Chem51:5843-55 (2008) [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 |
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Name: | Gag-Pol polyprotein |
Synonyms: | HIV-1 reverse transcriptase (HIV-1 RT) | Integrase | POL_HV1H2 | Pr160Gag-Pol | Protease | Reverse transcriptase (HIV-1 RT) | Reverse transcriptase (RT) | Ribonuclease H (RNase H) | gag-pol | p51 RT | p66 RT |
Type: | Protein |
Mol. Mass.: | 162074.74 |
Organism: | Human immunodeficiency virus type 1 group M subtype B (isolate HXB2) |
Description: | P04585 |
Residue: | 1435 |
Sequence: | MGARASVLSGGELDRWEKIRLRPGGKKKYKLKHIVWASRELERFAVNPGLLETSEGCRQI
LGQLQPSLQTGSEELRSLYNTVATLYCVHQRIEIKDTKEALDKIEEEQNKSKKKAQQAAA
DTGHSNQVSQNYPIVQNIQGQMVHQAISPRTLNAWVKVVEEKAFSPEVIPMFSALSEGAT
PQDLNTMLNTVGGHQAAMQMLKETINEEAAEWDRVHPVHAGPIAPGQMREPRGSDIAGTT
STLQEQIGWMTNNPPIPVGEIYKRWIILGLNKIVRMYSPTSILDIRQGPKEPFRDYVDRF
YKTLRAEQASQEVKNWMTETLLVQNANPDCKTILKALGPAATLEEMMTACQGVGGPGHKA
RVLAEAMSQVTNSATIMMQRGNFRNQRKIVKCFNCGKEGHTARNCRAPRKKGCWKCGKEG
HQMKDCTERQANFLREDLAFLQGKAREFSSEQTRANSPTRRELQVWGRDNNSPSEAGADR
QGTVSFNFPQVTLWQRPLVTIKIGGQLKEALLDTGADDTVLEEMSLPGRWKPKMIGGIGG
FIKVRQYDQILIEICGHKAIGTVLVGPTPVNIIGRNLLTQIGCTLNFPISPIETVPVKLK
PGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPVFAIKKKDSTKWRK
LVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPLDEDFRKYTAFTIP
SINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFRKQNPDIVIYQYMDDLYVGSDL
EIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWTVQPIVLPEKDSWT
VNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAELELAENREILKEP
VHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGAHTNDVKQLTEAVQ
KITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTPPLVKLWYQLEKEP
IVGAETFYVDGAANRETKLGKAGYVTNRGRQKVVTLTDTTNQKTELQAIYLALQDSGLEV
NIVTDSQYALGIIQAQPDQSESELVNQIIEQLIKKEKVYLAWVPAHKGIGGNEQVDKLVS
AGIRKVLFLDGIDKAQDEHEKYHSNWRAMASDFNLPPVVAKEIVASCDKCQLKGEAMHGQ
VDCSPGIWQLDCTHLEGKVILVAVHVASGYIEAEVIPAETGQETAYFLLKLAGRWPVKTI
HTDNGSNFTGATVRAACWWAGIKQEFGIPYNPQSQGVVESMNKELKKIIGQVRDQAEHLK
TAVQMAVFIHNFKRKGGIGGYSAGERIVDIIATDIQTKELQKQITKIQNFRVYYRDSRNP
LWKGPAKLLWKGEGAVVIQDNSDIKVVPRRKAKIIRDYGKQMAGDDCVASRQDED
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BDBM25352 |
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Biotinylated Target DNA |
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Name: | Biotinylated Target DNA |
Synonyms: | 3-biotinylated-poly d(GT)10/poly d(CA)10 |
Type: | Duplex DNA |
Mol. Mass.: | 358.43 |
Organism: | n/a |
Description: | The synthesized HIV long terminal repeat (LTR) sequence ligonucleotides (~30 bp) as the donor substrates were immobilized on microtiter plates in strand transfer assay. |
Residue: | 3 |
Sequence: | |