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Target
Ribonuclease H1
Ligand
BDBM33419
Substrate
RNA/DNA hybrid
Meas. Tech.
Fluorescence-Based RNase H Assay
pH
8±n/a
Temperature
293.15±n/a K
IC50
48500±n/a nM
Comments
IC50 is the mean of 48 and 49 uM.
Citation
Kirschberg, TA; Balakrishnan, M; Squires, NH; Barnes, T; Brendza, KM; Chen, X; Eisenberg, EJ; Jin, W; Kutty, N; Leavitt, S; Liclican, A; Liu, Q; Liu, X; Mak, J; Perry, JK; Wang, M; Watkins, WJ; Lansdon, EB RNase H active site inhibitors of human immunodeficiency virus type 1 reverse transcriptase: design, biochemical activity, and structural information. J Med Chem 52:5781-4 (2009) [PubMed] Article
More Info.:
Target
Name:
Ribonuclease H1
Synonyms:
RNASEH1 | RNH1 | RNH1_HUMAN | RNase H1 | Ribonuclease H type II
Type:
Enzyme
Mol. Mass.:
32076.45
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
286
Sequence:
MSWLLFLAHRVALAALPCRRGSRGFGMFYAVRRGRKTGVFLTWNECRAQVDRFPAARFKKFATEDEAWAFVRKSASPEVSEGHENQHGQESEAKASKRLREPLDGDGHESAEPYAKHMKPSVEPAPPVSRDTFSYMGDFVVVYTDGCCSSNGRRRPRAGIGVYWGPGHPLNVGIRLPGRQTNQRAEIHAACKAIEQAKTQNINKLVLYTDSMFTINGITNWVQGWKKNGWKTSAGKEVINKEDFVALERLTQGMDIQWMHVPGHSGFIGNEEADRLAREGAKQSED
Inhibitor
Name:
BDBM33419
Synonyms:
pyrimidinol carboxylic acid, 11
Type:
Small organic molecule
Emp. Form.:
C14H8BrClN2O4S
Mol. Mass.:
415.646
SMILES:
OC(=O)c1nc(Cc2c(Br)sc3ccc(Cl)cc23)[nH]c(=O)c1O
Substrate
Name:
RNA/DNA hybrid
Synonyms:
n/a
Type:
fluorescein-labeled RNA annealed to DNA
Mol. Mass.:
2134.40
Organism:
n/a
Description:
It is a 18-nucleotide 3-fluorescein-labeled RNA annealed to a complementary 18-nucleotide 5-Dabcyl-modified DNA.
Residue:
23
Sequence:
GACGAGCCGGGAGCFLRESCEIN