Reaction Details |
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Target | Gag-Pol polyprotein [600-1027,Y780C]/[600-1155,Y780C] |
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Ligand | BDBM1544 |
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Substrate/Competitor | poly(rC):oligo(dG) |
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Meas. Tech. | HIV-1 RT Assay |
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IC50 | 210±n/a nM |
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Citation | Proudfoot, JR; Hargrave, KD; Kapadia, SR; Patel, UR; Grozinger, KG; McNeil, DW; Cullen, E; Cardozo, M; Tong, L; Kelly, TA Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes. J Med Chem38:4830-8 (1995) [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 [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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BDBM1544 |
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poly(rC):oligo(dG) |
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Name: | poly(rC):oligo(dG) |
Synonyms: | n/a |
Type: | RNA-DNA duplex |
Mol. Mass.: | 358.43 |
Organism: | n/a |
Description: | The incorporation of Tritium-labeled [3H]dGTP onto a (poly)rC:(oligo)dG template:primer. |
Residue: | 3 |
Sequence: | |