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Target
Gag-Pol polyprotein [600-1027,P835L]/[600-1155,P835L]
Ligand
BDBM1434
Substrate
poly(rC)500:oligo(dG)10
Meas. Tech.
HIV-1 RT Assay
IC50
80±n/a nM
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 Chem 41:2960-71 (1998) [PubMed]  Article 
Target
Name:
Gag-Pol polyprotein [600-1027,P835L]/[600-1155,P835L]
Synonyms:
EC: 2.7.7.49 | HIV-1 Reverse Transcriptase Mutant (P236L)
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Gag-Pol polyprotein [600-1155,P835L]
Synonyms:
HIV-1 Reverse Transcriptase Mutant (P236L) Chain A | POL_HV1B1 | gag-pol
Type:
Enzyme Subunit
Mol. Mass.:
63944.85
Organism:
Human immunodeficiency virus type 1
Description:
P03366[600-1155,P835L]
Residue:
556
Sequence:
PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPVFAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPLDEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFKKQNPDIVIYQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPLFLWMGYELHPDKWTVQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAELELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGAHTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTPPLVKLWYQLEKEPIVGAETFYVDGAANRETKLGKAGYVTNKGRQKVVPLTNTTNQKTELQAIYLALQDSGLEVNIVTDSQYALGIIQAQPDKSESELVNQIIEQLIKKEKVYLAWVPAHKGIGGNEQVDKLVSAGI
  
Component 2
Name:
Gag-Pol polyprotein [600-1027,P835L]
Synonyms:
HIV-1 Reverse Transcriptase Mutant (P236L) Chain B | POL_HV1B1 | gag-pol
Type:
Enzyme Subunit
Mol. Mass.:
49984.68
Organism:
Human immunodeficiency virus type 1
Description:
P03366[600-1027,P835L]
Residue:
428
Sequence:
PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPVFAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPLDEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFKKQNPDIVIYQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPLFLWMGYELHPDKWTVQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVKQLCKLLRGTKALTEVIPLTEEAELELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGAHTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTPPLVKLWYQ
  
Inhibitor
Name:
BDBM1434
Synonyms:
11-cyclopropyl-5,11-dihydro-4-methyl-6H-dipyrido[3,2-b:2 ,3 -e][1,4]diazepin-6-one | 2-cyclopropyl-7-methyl-2,4,9,15-tetraazatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,12,14-hexaen-10-one | BI-RG-587 | CHEMBL57 | Nevirapine | Nevirapine (NVP) | US11420959, Example NVP | Viramune
Type:
Small organic molecule
Emp. Form.:
C15H14N4O
Mol. Mass.:
266.2979
SMILES:
Cc1ccnc2N(C3CC3)c3ncccc3C(=O)Nc12
Structure:
Search PDB for entries with ligand similarity:
Substrate
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:
NA