Compounds > tmc647055
Page last updated: 2024-11-13

tmc647055

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID44556044
CHEMBL ID2043025
SCHEMBL ID1239667
MeSH IDM0578226

Synonyms (26)

Synonym
CHEMBL2043025
tmc-647055
tmc647055
2,19-methano-3,7:4,1-dimetheno-1h,11h-14,10,2,9,11,17-benzoxathiatetraazacyclodocosine-8,18(9h,15h)-dione, 27-cyclohexyl-12,13,16,17-tetrahydro-22-methoxy-11,17-dimethyl-, 10,10-dioxide
11bd024g7j ,
unii-11bd024g7j
tmc 647055
1204416-97-6
SCHEMBL1239667
113-cyclohexyl-13-methoxy-5,11-dimethyl-17h-8-oxa-4-thia-3,5,11-triaza-1(10,6)-benzo[3,4]azepino[1,2-a]indolacyclododecaphane-2,12-dione 4,4-dioxide
DTXSID90152860
EX-A1252
AC-35964
NCGC00482982-02
us9427440, 1
bdbm243456
DB11822
BCP06459
28-cyclohexyl-22-methoxy-10,16-dimethyl-9,9-dioxo-13-oxa-9lambda6-thia-1,8,10,16-tetrazapentacyclo[16.8.1.12,6.13,26.020,25]nonacosa-2,4,6(29),18,20(25),21,23,26(28)-octaene-7,17-dione
FT-0701433
SB16907
Q27251314
A856345
27-cyclohexyl-12,13,16,17-tetrahydro-22-methoxy-11,17-dimethyl-2,19-methano-3,7:4,1-dimetheno-1h,11h-14,10,2,9,11,17-benzoxathiatetraazacyclodocosine-8,18(9h,15h)-dione 10,10-dioxide
CS-0007798
HY-15591

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (107)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1073456Toxicity in rat assessed as decrease in body weight at 1000 mg/kg/day after 5 days2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073432Cytotoxicity against human HepG2 cells after 3 days by resazurin-based fluorescence analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073447Plasma clearance in Sprague-Dawley rat at 2 mg/kg, iv and 10 mg/kg, po2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073438Volume of distribution at steady state in dog at 10 mg/kg, po2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073444Oral bioavailability in Sprague-Dawley rat at 10 mg/kg2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073422Antiviral activity against Hepatitis C virus genotype 1a infected in human HuH7 by transient replicon assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073379Toxicity in human assessed as effect on ECG profile at 300 to 1250 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073451Binding affinity to His6-tagged Hepatitis C virus Con 1b NS5B delta21 RNA dependent RNA polymerase expressed in Escherichia coli Rosetta 2 (DE3) by surface plasmon resonance analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID666569Inhibition of cytochrome P4502012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
AID1073384Toxicity in HCV genotype 1-infected patient assessed as effect on vital signs at 500 to 1000 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073410Antiviral activity against Hepatitis C virus genotype 1b harboring NS5B NNI-1 site P495L mutant infected in human HuH7 by luciferase reporter gene assay relative to wild-type HCV genotype 1b2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073402Antiviral activity against Hepatitis C virus harboring NS5B D168V mutant infected in human HuH7 by luciferase reporter gene assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073449Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells after 72 hrs by luciferase reporter gene assay in presence of 40% human plasma relative to control2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1645924Antiviral activity against HCV2019European journal of medicinal chemistry, Feb-15, Volume: 164A review on HCV inhibitors: Significance of non-structural polyproteins.
AID1073389Toxicity in human assessed as grade-4 adverse events at 300 to 1250 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073401Antiviral activity against Hepatitis C virus harboring NS5B L31V mutant infected in human HuH7 by luciferase reporter gene assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073377Selectivity ratio of EC50 for Hepatitis C virus genotype 2b to EC50 for wild-type Hepatitis C virus Con 1b2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073430Binding affinity to Hepatitis C virus Con 1b wild-type NS5B by surface plasmon resonance analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073385Toxicity in human assessed as effect on vital signs at 300 to 1250 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073426Binding affinity to Hepatitis C virus genotype 3a NS5B by surface plasmon resonance analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073445Ratio of drug level in liver to plasma in Sprague-Dawley rat at 10 mg/kg, po after 7 hrs2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073455Toxicity in rat after 5 days2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073442Cmax in dog at 10 mg/kg, po2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073368Apparent permeability from apical to basolateral side in human Caco2 cells2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID666572Plasma clearance in dog at 10 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
AID1073375Antiviral activity against Hepatitis C virus genotype 1a infected in po dosed human assessed as decrease in HCV RNA level administered bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073436Selectivity ratio of Kd for Hepatitis C virus genotype 2b NS5B to Kd for Hepatitis C virus Con 1b wild-type NS5B2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073403Antiviral activity against Hepatitis C virus harboring NS5B A156V mutant infected in human HuH7 by luciferase reporter gene assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073431Cytotoxicity against African green monkey Vero E6 cells after 3 days by resazurin-based fluorescence analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID668702Metabolic stability in rat liver microsomes assessed as compound metabolized at 5 uM after 15 mins2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
AID666563Ratio of drug uptake in Sprague-Dawley rat liver to plasma at 10 mg/kg, po measured after 7 hrs2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
AID668704Clearance in Sprague-Dawley rat at 2 mg/kg, iv and 10 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
AID1073417Antiviral activity against Hepatitis C virus genotype 3a infected in human HuH7 by transient replicon assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073392Toxicity in HCV genotype 1-infected patient assessed as gastrointestinal side-effects at 500 to 1000 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073420Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 by transient replicon assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073374Antiviral activity against Hepatitis C virus genotype 1a infected in human assessed as log10 reduction in HCV RNA level at 500 mg, po bid for 5 days followed by morning dose on day 6 relative to control2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073395Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 assessed as suppression of formation of resistant colonies at 1.5 uM preincubated for 2 weeks followed by 3 week rebound phase by RT-PCR analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073413Selectivity ratio of EC50 for Hepatitis C virus genotype 2a to EC50 for wild-type Hepatitis C virus Con 1b2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073406Antiviral activity against Hepatitis C virus harboring NS5B S96T mutant infected in human HuH7 by luciferase reporter gene assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID666568Cmax in dog at 10 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
AID1073387Toxicity in human assessed as effect on laboratory parameters at 300 to 1250 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID668700Antiviral activity against Hepatitic C virus genotype 1b clone ET infected in human Huh7 replicon cells after 72 hrs by luciferase reporter gene assay2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
AID1073415Antiviral activity against Hepatitis C virus genotype 6a infected in human HuH7 by transient replicon assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073388Toxicity in HCV genotype 1-infected patient assessed as grade-4 adverse events at 500 to 1000 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073452Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells after 72 hrs by luciferase reporter gene assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073418Antiviral activity against Hepatitis C virus genotype 2b infected in human HuH7 by transient replicon assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073405Antiviral activity against Hepatitis C virus harboring NS5B S282T mutant infected in human HuH7 by luciferase reporter gene assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073440AUC (0 to infinity) in dog at 10 mg/kg, po2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073439Plasma clearance in dog at 10 mg/kg, po2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID668701Selectivity index, ratio of CC50 for human Huh7 cells to EC50 for Hepatitic C virus genotype 1b clone ET2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
AID1073425Binding affinity to Hepatitis C virus genotype 4a NS5B by surface plasmon resonance analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073434Cytotoxicity against human MRC5 cells after 3 days by resazurin-based fluorescence analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073450Fraction unbound in human plasma2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073441Oral bioavailability in dog at 10 mg/kg2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073370Antiviral activity against Hepatitis C virus genotype 1a infected in human assessed as reduction in plasma HCV RNA level administered for 10 days measured on day 112014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073419Antiviral activity against Hepatitis C virus genotype 2a infected in human HuH7 by transient replicon assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID666565Cmax in Sprague-Dawley rat at 10 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
AID1073427Binding affinity to Hepatitis C virus genotype 2b NS5B by surface plasmon resonance analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073373Antiviral activity against Hepatitis C virus genotype 1a infected in human assessed as log10 reduction in HCV RNA level at 1000 mg, po bid for 5 days followed by morning dose on day 6 relative to control2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073435Antiviral activity against Hepatitis C virus genotype 1a infected in human HuH7-SG cells after 3 days by RT-PCR analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073421Antiviral activity against wild-type Hepatitis C virus Con 1b infected in human HuH7 by transient replicon assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073446Drug uptake in Sprague-Dawley rat liver at 10 mg/kg, po after 7 hrs2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073399Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 assessed as clearance of replicon cells at 3.75 uM preincubated for 2 weeks followed by 3 week rebound phase by RT-PCR analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID666564Oral bioavailability in Sprague-Dawley rat at 10 mg/kg2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
AID1073424Binding affinity to Hepatitis C virus genotype 5a NS5B by surface plasmon resonance analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID666567Volume of distribution at steady state in dog at 10 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
AID1073423Binding affinity to Hepatitis C virus genotype 6a NS5B by surface plasmon resonance analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073454Cytotoxicity against human HuH7 cells2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID668705Drug uptake in Sprague-Dawley rat liver at 10 mg/kg, po measured after 7 hrs2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
AID1073408Antiviral activity against Hepatitis C virus harboring NS5B M414T mutant infected in human HuH7 by luciferase reporter gene assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073380Toxicity in HCV genotype 1-infected patient assessed as effect on appetite at 500 to 1000 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073453Cytotoxicity against human MT4 cells2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073400Antiviral activity against Hepatitis C virus harboring NS5B Y93H mutant infected in human HuH7 by luciferase reporter gene assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID666566AUC (0 to infinity) in dog at 10 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
AID1073381Toxicity in human assessed as effect on appetite at 300 to 1250 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073433Cytotoxicity against HEK293T cells after 3 days by resazurin-based fluorescence analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073386Toxicity in HCV genotype 1-infected patient assessed as effect on laboratory parameters at 500 to 1000 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073448Drug metabolism in human liver microsomes at 5 uM after 15 mins2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073382Toxicity in HCV genotype 1-infected patient assessed as effect on food consumption at 500 to 1000 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073378Toxicity in HCV genotype 1-infected patient assessed as effect on ECG profile at 500 to 1000 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073404Antiviral activity against Hepatitis C virus harboring NS5B R155K mutant infected in human HuH7 by luciferase reporter gene assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073383Toxicity in human assessed as effect on food consumption at 300 to 1250 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073372Antiviral activity against Hepatitis C virus genotype 1b infected in human assessed as log10 reduction in HCV RNA level at 500 mg, po bid for 5 days followed by morning dose on day 6 relative to control2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073414Binding affinity to Hepatitis C virus genotype 1b NS5B assessed as half life by surface plasmon resonance analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID666571Oral bioavailability in dog at 10 mg/kg2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
AID1073393Toxicity in human assessed as gastrointestinal side-effects at 300 to 1250 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073398Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 assessed as rebound of replicon RNA at 3.75 uM preincubated for 2 weeks followed by 3 week rebound phase by RT-PCR analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID666570Drug metabolism in Sprague-Dawley rat assessed as reactive acyl glucuronides formation2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
AID1073376Drug metabolism in human assessed as CYP3A4-induced 4-beta-hydroxycholesterol level at 300 to 1250 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073428Binding affinity to Hepatitis C virus genotype 1b NS5B by surface plasmon resonance analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073390Toxicity in HCV genotype 1-infected patient assessed as grade-3 adverse events at 500 to 1000 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073369Antiviral activity against Hepatitis C virus genotype 1b infected in human assessed as reduction in plasma HCV RNA level administered for 10 days measured on day 112014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID668703Metabolic stability in human liver microsomes assessed as compound metabolized at 5 uM after 15 mins2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
AID1073416Antiviral activity against Hepatitis C virus genotype 4a infected in human HuH7 by transient replicon assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073411Antiviral activity against Hepatitis C virus genotype 1b harboring NS5B NNI-1 site V494A mutant infected in human HuH7 by luciferase reporter gene assay relative to wild-type HCV genotype 1b2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073371Antiviral activity against Hepatitis C virus genotype 1b infected in human assessed as log10 reduction in HCV RNA level at 1000 mg, po bid for 5 days followed by morning dose on day 6 relative to control2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073391Toxicity in human assessed as grade-3 adverse events at 300 to 1250 mg, po bid for 5 days followed by morning dose on day 62014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073409Antiviral activity against Hepatitis C virus harboring NS5B M423T mutant infected in human HuH7 by luciferase reporter gene assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073429Binding affinity to Hepatitis C virus genotype 1a NS5B by surface plasmon resonance analysis2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073412Antiviral activity against Hepatitis C virus genotype 1b harboring NS5B NNI-1 site L392I mutant infected in human HuH7 by luciferase reporter gene assay relative to wild-type HCV genotype 1b2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073407Antiviral activity against Hepatitis C virus harboring NS5B C316Y mutant infected in human HuH7 by luciferase reporter gene assay2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
AID1073437Inhibition of His6-tagged Hepatitis C virus Con 1b NS5B delta21 RNA dependent RNA polymerase expressed in Escherichia coli Rosetta 2 (DE3) after 2 hrs by surface plasmon resonance analysis in presence of 5'-biotinylated rG13 primer2014Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (66.67)24.3611
2020's2 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.74

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index17.74 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.74)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (83.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
imiquimod
Imiquimod: A topically-applied aminoquinoline immune modulator that induces interferon production. It is used in the treatment of external genital and perianal warts, superficial CARCINOMA, BASAL CELL; and ACTINIC KERATOSIS.. imiquimod : An imidazoquinoline fused [4,5-c] carrying isobutyl and amino substituents at N-1 and C-4 respectively. A prescription medication, it acts as an immune response modifier and is used to treat genital warts, superficial basal cell carcinoma, and actinic keratosis.		3.3110imidazoquinolineantineoplastic agent;
interferon inducer
biln 2061
BILN 2061: a macrocyclic NS3 protease inhibitor and antiviral agent; structure in first source		3.3110
sm360320
SM360320: Proc Natl Acad Sci U S A 2006 Feb 7;103(6):1828-33		3.3110
danoprevir
[no description available]		3.3110
narlaprevir
narlaprevir: an antiviral agent that inhibits hepatitis C virus NS3 protease. narlaprevir : An azabicyclohexane that is (1R,5S)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane substituted by [(3S)-1-(cyclopropylamino)-1,2-dioxoheptan-3-yl]aminoacyl and N-({1-[(tert-butylsulfonyl)methyl]cyclohexyl}carbamoyl)-3-methyl-L-valyl groups at positions 2S and 3, respectively. It is a hepatitis C virus (HCV) NS3/4A serine protease inhibitor (Ki = 6 nM) that is used for the treatment of chronic hepatitis C.		3.3110azabicyclohexane;
cyclopropanes;
pyrrolidinecarboxamide;
secondary carboxamide;
sulfone;
tertiary carboxamide;
ureas		anticoronaviral agent;
antiviral drug;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
hepatitis C protease inhibitor
bms-650032
asunaprevir: an NS3 protease inhibitor against hepatitis C virus		3.3110oligopeptide
mk-7009
vaniprevir: inhibits hepatitis C virus NS3/4a protease. vaniprevir : An azamacrocyclic compound that is a hepatitis C virus (HCV) NS3/4A protease inhibitor which is approved for the treatment of hepatitis C virus infections in Japan.		3.3110azamacrocycle;
carbamate ester;
cyclopropanes;
N-sulfonylcarboxamide;
pyrrolidinecarboxamide		antiviral drug;
hepatitis C protease inhibitor
simeprevir
[no description available]		2.110azamacrocycle;
lactam
bi 201335
faldaprevir: inhibits hepatitis C virus NS3 protease		3.3110
grazoprevir
grazoprevir: has antiviral activity; component of Zepatier. grazoprevir : An azamacrocyclic compound that is a hepatitis C protease inhibitor used in combination with elbasvir (under the brand name Zepatier) for treatment of chronic HCV genotypes 1 or 4 infection in adults.		3.3110aromatic ether;
azamacrocycle;
carbamate ester;
cyclopropanes;
lactam;
N-sulfonylcarboxamide;
quinoxaline derivative		antiviral drug;
hepatitis C protease inhibitor;
hepatoprotective agent
ConditionIndicatedRelationship StrengthStudiesTrials
Hepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted
[description not available]		03.1210
Hepatitis C
INFLAMMATION of the LIVER in humans caused by HEPATITIS C VIRUS, a single-stranded RNA virus. Its incubation period is 30-90 days. Hepatitis C is transmitted primarily by contaminated blood parenterally and is often associated with transfusion and intravenous drug abuse. However, in a significant number of cases, the source of hepatitis C infection is unknown.		15.1210
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510