Page last updated: 2024-11-13

(r)-pfi-2

Description

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(R)-PFI-2: a potent and selective inhibitor of SETD7 methyltransferase; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71300326
CHEMBL ID3414622
SCHEMBL ID23683049
MeSH IDM000599686

Synonyms (25)

Synonym
8-fluoro-n-{(2r)-1-oxo-1-(pyrrolidin-1-yl)-3-[3-(trifluoromethyl)phenyl]propan-2-yl}-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide
1l8 ,
S7294
8-fluoro-n-[(2r)-1-oxo-1-pyrrolidin-1-yl-3-[3-(trifluoromethyl)phenyl]propan-2-yl]-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide
gtpl8235
(r)-pfi-2
CS-4177
1627676-59-8
HY-18627
pfi-2
bdbm50075073
CHEMBL3414622 ,
AKOS030526617
pfi2
pfi 2
6-isoquinolinesulfonamide, 8-fluoro-1,2,3,4-tetrahydro-n-[(1r)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-
NCGC00351479-01
EX-A1603
Q27078107
CCG-269682
A882801
8-fluoro-1,2,3,4-tetrahydro-n-[(1r)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide
SCHEMBL23683049
jckgspaapqrpbw-oaqylsrusa-n
AC-35943

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]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histone-lysine N-methyltransferase SETD7Homo sapiens (human)IC50 (µMol)0.00200.00202.52666.0800AID1199174; AID1602194; AID1667227
Histone-lysine N-methyltransferase SETD7Homo sapiens (human)Ki0.00030.00030.00030.0003AID1199174
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (8)

Processvia Protein(s)Taxonomy
DNA damage responseHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
heterochromatin organizationHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
chromatin organizationHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
chromatin remodelingHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
peptidyl-lysine monomethylationHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
peptidyl-lysine dimethylationHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
response to ethanolHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
heterochromatin organizationHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
p53 bindingHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
protein bindingHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
protein-lysine N-methyltransferase activityHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
histone methyltransferase activityHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
histone H3 methyltransferase activityHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
histone H3K4 monomethyltransferase activityHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
chromatin bindingHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
nucleoplasmHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
chromosomeHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
nucleolusHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
chromosomeHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
nucleusHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID1199185Selectivity ratio of IC50 for human MLL to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199174Inhibition of full-length human SETD7 expressed in Escherichia coli BL21 (DE3) using biotinylated histone H3 (1 to 25) as substrate after 1 hr by Flash Plate assay in presence of [3H]-SAM2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199190Selectivity ratio of IC50 for human PRMT8 to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199177Selectivity ratio of IC50 for human EZH2 to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199182Selectivity ratio of IC50 for human SETD2 to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199180Selectivity ratio of IC50 for human SUV420H1 to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199179Selectivity ratio of IC50 for human SUV39H2 to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199187Selectivity ratio of IC50 for human PRMT1 to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199181Selectivity ratio of IC50 for human SUV420H2 to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1667227Inhibition of recombinant human SET7 expressed in Escherichia coli using [3H] SAM as substrate by scintillation counter assay2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Computational discovery and biological evaluation of novel inhibitors targeting histone-lysine N-methyltransferase SET7.
AID1199183Selectivity ratio of IC50 for human SETD8 to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199184Selectivity ratio of IC50 for human SMYD2 to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199192Selectivity ratio of IC50 for human DNMT1 to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199178Selectivity ratio of IC50 for human EZH1 to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199191Selectivity ratio of IC50 for human DOT1L to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199188Selectivity ratio of IC50 for human PRMT3 to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1602194Inhibition of recombinant full-length human SETD7 (1 to 366 residues) expressed in Escherichia coli BL21 (DE3) using [3H]-SAM-fused biotinylated peptide as substrate by scintillation proximity assay2019European journal of medicinal chemistry, Mar-15, Volume: 166Histone methyl transferases: A class of epigenetic opportunities to counter uncontrolled cell proliferation.
AID1199186Selectivity ratio of IC50 for human WHSC1 to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199189Selectivity ratio of IC50 for human PRMT5 to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199175Selectivity ratio of IC50 for human G9a to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199176Selectivity ratio of IC50 for human GLP to IC50 for full-length human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
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.
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.
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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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.
AID1346075Human SET domain containing lysine methyltransferase 7 (2.1.1.43 Histone methyltransferases (HMTs))2014Proceedings of the National Academy of Sciences of the United States of America, Sep-02, Volume: 111, Issue:35
(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's7 (58.33)24.3611
2020's5 (41.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (8.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (91.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
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