Reaction Details |
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Target | Gag-Pol polyprotein [588-1027] |
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Ligand | BDBM27613 |
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Substrate/Competitor | RNA:Biotin-DNA template:primer |
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Meas. Tech. | HIV-1 Reverse Transcriptase Assay |
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pH | 8±n/a |
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Temperature | 303.15±n/a K |
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IC50 | 5±n/a nM |
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EC50 | 2±n/a nM |
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Citation | Sweeney, ZK; Harris, SF; Arora, SF; Javanbakht, H; Li, Y; Fretland, J; Davidson, JP; Billedeau, JR; Gleason, SK; Hirschfeld, D; Kennedy-Smith, JJ; Mirzadegan, T; Roetz, R; Smith, M; Sperry, S; Suh, JM; Wu, J; Tsing, S; Villaseñor, AG; Paul, A; Su, G; Heilek, G; Hang, JQ; Zhou, AS; Jernelius, JA; Zhang, FJ; Klumpp, K Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase. J Med Chem51:7449-58 (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 [588-1027] |
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Name: | Gag-Pol polyprotein [588-1027] |
Synonyms: | HIV-1 Reverse Transcriptase |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
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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Component 2 |
Name: | Gag-Pol polyprotein [588-1027] |
Synonyms: | HIV-1 Reverse Transcriptase Chain B | POL_HV1H2 | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 51337.13 |
Organism: | Human immunodeficiency virus type 1 |
Description: | P04585[588-1027] |
Residue: | 440 |
Sequence: | PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPV
FAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPL
DEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFRKQNPDIVI
YQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWT
VQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAE
LELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGA
HTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTP
PLVKLWYQLEKEPIVGAETF
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BDBM27613 |
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RNA:Biotin-DNA template:primer |
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Name: | RNA:Biotin-DNA template:primer |
Synonyms: | n/a |
Type: | RNA/DNA duplex |
Mol. Mass.: | 2957.49 |
Organism: | n/a |
Description: | The incorporation of [3H]dATP onto a RNA:(biotin)DNA template:primer. |
Residue: | 38 |
Sequence: | 5-GGG UCU CUC UGG UUA GAC CAC UCU AGC AGU GGC GCC CGA ACA GG
G AC-3
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