Page last updated: 2024-11-12

tfc 007

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 CID16040067
CHEMBL ID4238186
SCHEMBL ID23195705
MeSH IDM0568609

Synonyms (16)

Synonym
AKOS025142049
tfc 007
927878-49-7
n-[4-[4-(4-morpholinylcarbonyl)-1-piperidinyl]phenyl]-2-phenoxy-5-pyrimidinecarboxamide
SCHEMBL23195705
NCGC00387231-01
EX-A3539
tfc-007
n-(4-(4-(morpholine-4-carbonyl)piperidin-1-yl)phenyl)-2-phenoxypyrimidine-5-carboxamide
CHEMBL4238186 ,
bdbm50463722
n-[4-[4-(morpholine-4-carbonyl)piperidin-1-yl]phenyl]-2-phenoxypyrimidine-5-carboxamide
gtpl11392
tfc007
CS-0033029
HY-110167

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 (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GVesicular stomatitis virusPotency11.98770.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency11.98770.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Hematopoietic prostaglandin D synthaseHomo sapiens (human)IC50 (µMol)0.17100.07100.92223.8000AID1685233; AID1685234; AID1685249; AID1833083; AID1858478
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Hematopoietic prostaglandin D synthaseHomo sapiens (human)Kd0.00040.00040.00040.0004AID1399746
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (51)

Processvia Protein(s)Taxonomy
prostaglandin biosynthetic processHematopoietic prostaglandin D synthaseHomo sapiens (human)
prostaglandin metabolic processHematopoietic prostaglandin D synthaseHomo sapiens (human)
signal transductionHematopoietic prostaglandin D synthaseHomo sapiens (human)
locomotory behaviorHematopoietic prostaglandin D synthaseHomo sapiens (human)
negative regulation of male germ cell proliferationHematopoietic prostaglandin D synthaseHomo sapiens (human)
glutathione metabolic processHematopoietic prostaglandin D synthaseHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
magnesium ion bindingHematopoietic prostaglandin D synthaseHomo sapiens (human)
glutathione transferase activityHematopoietic prostaglandin D synthaseHomo sapiens (human)
prostaglandin-D synthase activityHematopoietic prostaglandin D synthaseHomo sapiens (human)
calcium ion bindingHematopoietic prostaglandin D synthaseHomo sapiens (human)
protein bindingHematopoietic prostaglandin D synthaseHomo sapiens (human)
protein homodimerization activityHematopoietic prostaglandin D synthaseHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
nucleoplasmHematopoietic prostaglandin D synthaseHomo sapiens (human)
cytoplasmHematopoietic prostaglandin D synthaseHomo sapiens (human)
cytosolHematopoietic prostaglandin D synthaseHomo sapiens (human)
intracellular membrane-bounded organelleHematopoietic prostaglandin D synthaseHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (18)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
AID1833083Inhibition of H-PGDS (unknown origin) using fluorescent probe by competition binding assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Discovery of a Highly Potent and Selective Degrader Targeting Hematopoietic Prostaglandin D Synthase via In Silico Design.
AID1685234Binding affinity to recombinant human HPGDS expressed in Escherichia coli BL21 (DE3) measured after 1 hr by fluorescence polarization assay2021ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2
Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer.
AID1685231Induction of CRBN-mediated HPGDS degradation in human KU812 cells at 10 to 100 nM incubated for 24 hrs followed by compound washout and further incubated for 6 hrs in compound-free medium by Western blot analysis2021ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2
Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer.
AID1858479PROTAC activity at CRBN/H-PGDS in human KU812 cells assessed as reduction in H-PGDS levels incubated for 24 hrs by Western blotting analysis2022RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12
Structure-activity relationship study of PROTACs against hematopoietic prostaglandin D
AID1685230Inhibition of HPGDS in human KU812 cells assessed as reduction in PGD2 level at 10 to 100 nM incubated for 24 hrs followed by A23187 treatment and measured after 30 mins by ELISA2021ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2
Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer.
AID1685227Inhibition of HPGDS in human KU812 cells assessed as reduction in PGD2 level at 10 to 100 nM incubated for 24 hrs followed by A23187 treatment and measured after 30 mins and subsequent compound washout then further incubated for 6 hrs in compound-free med2021ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2
Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer.
AID1858489Inhibition of H-PGDS in human KU812 cells assessed as reduction in A23187-stimulated PGD2 levels at 10 nM preincubated for 24 hrs followed by A23187 stimulation for 30 mins by ELISA analysis2022RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12
Structure-activity relationship study of PROTACs against hematopoietic prostaglandin D
AID1685239Induction of HPGDS degradation in human KU812 cells at 1 uM measured after 6 hrs in presence of pomalidomide by Western blot analysis2021ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2
Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer.
AID1685233Inhibition of recombinant human HPGDS expressed in Escherichia coli BL21 (DE3) measured after 3 mins by spectrophotometric analysis2021ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2
Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer.
AID1833090Suppression of PGD2 production in human KU812 cells measured in presence of compound 43 up to 3000 pM incubated for 6 hrs by LC-MS analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Discovery of a Highly Potent and Selective Degrader Targeting Hematopoietic Prostaglandin D Synthase via In Silico Design.
AID1399746Binding affinity to full length recombinant human N-terminal His6-tagged H-PGDS expressed in Escherichia coli BL21(DE3) by SPR analysis2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
Characterization of crystal water molecules in a high-affinity inhibitor and hematopoietic prostaglandin D synthase complex by interaction energy studies.
AID1858478Binding affinity to recombinant human H-PGDS incubated for 1 hrs by competitive fluorescence polarization assay2022RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12
Structure-activity relationship study of PROTACs against hematopoietic prostaglandin D
AID1685249Inhibition of recombinant human HPGDS using [14C]-PGH2 as substrate preincubated for 1 min in presence of MgCl2 followed by substrate addition and measured after 45 mins by radioactive imaging analysis2021ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2
Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's2 (28.57)24.3611
2020's5 (71.43)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.84

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 Index17.84 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.73 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.84)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]