Page last updated: 2024-11-13

amg 487

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 CID24957182
CHEMBL ID397983
SCHEMBL ID335753
MeSH IDM0536776

Synonyms (29)

Synonym
C15830
vuf-10085
amg-487
CHEMBL397983 ,
(-)-(r)-n-(1-(3-(4-ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl)ethyl)-n-(pyridin-3-ylmethyl)-2-(4-(trifluoromethoxy)phenyl)acetamide
bdbm50211114
(r)-n-(1-(3-(4-ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl)ethyl)-n-(pyridin-3-ylmethyl)-2-(4-(trifluoromethoxy)phenyl)acetamide ,
S8682
HY-15319
SCHEMBL335753
amg 487 ,
473719-41-4
benzeneacetamide, n-((1r)-1-(3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido(2,3-d)pyrimidin-2-yl)ethyl)-n-(3-pyridinylmethyl)-4-(trifluoromethoxy)-
unii-355cgr2cbl
355cgr2cbl ,
n-[(1r)-1-[3-(4-ethoxyphenyl)-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-n-(pyridin-3-ylmethyl)-2-[4-(trifluoromethoxy)phenyl]acetamide
amg487
AKOS030526817
NCGC00378587-01
wqtknbpcjkrypa-oaqylsrusa-n
amg 487; amg487
BCP23713
amg-487-(+/-)
Q27256426
MS-30643
n-[1-[3-(4-ethoxyphenyl)-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-n-(pyridin-3-ylmethyl)-2-[4-(trifluoromethoxy)phenyl]acetamide
n-((1r)-1-(3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido(2,3-d)pyrimidin-2-yl)ethyl)-n-(3-pyridinylmethyl)-4-(trifluoromethoxy)-benzeneacetamide
DTXSID501025828
AC-36575

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 (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency4.77240.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency0.95220.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency26.83700.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency0.95220.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency0.95220.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency0.95220.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency0.95220.01238.964839.8107AID1645842
[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)
C-X-C chemokine receptor type 3Homo sapiens (human)IC50 (µMol)0.03140.00500.35886.5600AID290628; AID290633; AID290634; AID290635; AID290636; AID290637; AID313785; AID313786; AID313790; AID313791; AID313792; AID348583; AID449699; AID468547; AID641650; AID641651; AID707874
C-X-C chemokine receptor type 3Homo sapiens (human)Ki0.09920.00160.06660.1585AID712528; AID712529
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.00800.00040.16800.9772AID290628
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (56)

Processvia Protein(s)Taxonomy
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)
angiogenesisC-X-C chemokine receptor type 3Homo sapiens (human)
regulation of leukocyte migrationC-X-C chemokine receptor type 3Homo sapiens (human)
apoptotic processC-X-C chemokine receptor type 3Homo sapiens (human)
chemotaxisC-X-C chemokine receptor type 3Homo sapiens (human)
inflammatory responseC-X-C chemokine receptor type 3Homo sapiens (human)
cell adhesionC-X-C chemokine receptor type 3Homo sapiens (human)
cell surface receptor signaling pathwayC-X-C chemokine receptor type 3Homo sapiens (human)
regulation of cell adhesionC-X-C chemokine receptor type 3Homo sapiens (human)
chemokine-mediated signaling pathwayC-X-C chemokine receptor type 3Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationC-X-C chemokine receptor type 3Homo sapiens (human)
calcium-mediated signalingC-X-C chemokine receptor type 3Homo sapiens (human)
immune responseC-X-C chemokine receptor type 3Homo sapiens (human)
cell chemotaxisC-X-C chemokine receptor type 3Homo 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
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)
chemokine receptor activityC-X-C chemokine receptor type 3Homo sapiens (human)
protein bindingC-X-C chemokine receptor type 3Homo sapiens (human)
C-X-C chemokine receptor activityC-X-C chemokine receptor type 3Homo sapiens (human)
chemokine bindingC-X-C chemokine receptor type 3Homo sapiens (human)
C-C chemokine receptor activityC-X-C chemokine receptor type 3Homo sapiens (human)
C-C chemokine bindingC-X-C chemokine receptor type 3Homo 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 (22)

Processvia Protein(s)Taxonomy
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)
cell surfaceC-X-C chemokine receptor type 3Homo sapiens (human)
cytoplasmC-X-C chemokine receptor type 3Homo sapiens (human)
plasma membraneC-X-C chemokine receptor type 3Homo sapiens (human)
external side of plasma membraneC-X-C chemokine receptor type 3Homo 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 (73)

Assay IDTitleYearJournalArticle
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.
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.
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.
AID1218824Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1218828Ratio of IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition to IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 92012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID712527Antagonist activity at human CXCR3 expressed in HEK293T cells co-expressing Galphaqi5 assessed as inhibition of CXCL10-induced [3H]-inositolphosphates levels2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
CXCR3 antagonists: quaternary ammonium salts equipped with biphenyl- and polycycloaliphatic-anchors.
AID290643Half life in cynomolgus monkey at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID1218843Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins followed by substrate addition by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID290639Clearance in dog at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID642275Drug level in C57BL/6 mouse blood at 10 mg/kg, sc after 1 hr2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Discovery of potent and specific CXCR3 antagonists.
AID1218848Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins followed by substrate addition by LC-MS/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID290628Displacement of [125I ]IP10 from CXCR3 receptor expressed in PBMC2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID1218847Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins followed by substrate addition by LC-MS/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID290645Bioavailability in cynomolgus monkey at 5 mg/kg, po2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID642273Receptor occupancy of CXCR3 in mouse whole blood assessed as inhibition of ITAC binding by fluorescence quenching based FACS analysis2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Discovery of potent and specific CXCR3 antagonists.
AID1218827Ratio of IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition to IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID290642Half life in dog at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID641650Displacement of [125I]-IP-10 from CXCR32012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Discovery of potent and specific CXCR3 antagonists.
AID1218853Ratio of IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins to IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1218845Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins followed by substrate addition by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1218851Ratio of IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins to IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID348586Binding affinity to human muscarinic M3 receptor2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists.
AID1218849Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins followed by substrate addition by LC-MS/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID290635Inhibition of ITAC-induced CXCR3 mediated cell migration2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID1218823Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1218826Ratio of IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition to IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 32012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID712528Displacement of [125I]-CXCL11 from human CXCR3 expressed in HEK293 cells2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
CXCR3 antagonists: quaternary ammonium salts equipped with biphenyl- and polycycloaliphatic-anchors.
AID290646Inhibition of cell migration in mouse assessed as reduction of bleomycin-induced cellular infiltration into lungs at 3 mg/kg, sc2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID290636Inhibition of MIG-induced CXCR3 mediated cell migration2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID468582Drug level in bleomycin-induced mouse blood at 1 mg/mL, sc2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID468581Drug level in bleomycin-induced mouse blood at 3 mg/mL, sc2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID348583Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists.
AID1218854Ratio of IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins to IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID290638Inhibition of cell migration in subcutaneously dosed mouse assessed as reduction of bleomycin-induced cellular infiltration into lungs2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID712529Displacement of [125I]-CXCL10 from human CXCR3 expressed in HEK293 cells2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
CXCR3 antagonists: quaternary ammonium salts equipped with biphenyl- and polycycloaliphatic-anchors.
AID1218844Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins followed by substrate addition by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID707874Binding affinity to CXCR32012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID290641Half life in rat at 0.5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID313790Antagonist activity at CXCR3 assessed as IP-10-mediated cell migration2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists.
AID641651Displacement of [125I]-IP-10 from CXCR3 in presence of 100% human serum2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Discovery of potent and specific CXCR3 antagonists.
AID1218846Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins followed by substrate addition by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID468550Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID1218825Ratio of IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition to IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1218817Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1218850Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins followed by substrate addition by LC-MS/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID313785Displacement of [125I]IP-10 from CXCR3 receptor2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists.
AID642276Drug level in C57BL/6 mouse blood at 1 mg/kg, sc after 1 hr2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Discovery of potent and specific CXCR3 antagonists.
AID449699Displacement of [125I]IP10 from CXCR3 receptor expressed in PBMC2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Imidazo-pyrazine derivatives as potent CXCR3 antagonists.
AID348585Binding affinity to human muscarinic M2 receptor2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists.
AID1218818Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1218822Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1218820Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1218852Ratio of IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins to IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID290630Clearance in rat at 0.5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID290640Clearance in cynomolgus monkey at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID707908Lipophilicity, log P of the compound2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID468547Displacement of [125I]-1P10 from human CXCR3 expressed in PBMC after 2 hrs in RPMI buffer by scintillation counting2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID1218819Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID313791Antagonist activity at CXCR3 assessed as ITAC-mediated cell migration2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists.
AID313786Displacement of [125I]ITAC from CXCR3 receptor2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists.
AID290644Bioavailability in dog at 2.5 mg/kg, po2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID290634Inhibition of IP10-induced CXCR3 mediated cell migration2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID290637Antagonist activity at human CXCR3 assessed as inhibition of ITAC-induced calcium mobilization2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID468580Drug level in bleomycin-induced mouse blood at 10 mg/mL, sc2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID313792Antagonist activity at CXCR3 assessed as MIG-mediated cell migration2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists.
AID1218856Time dependent inhibition of CYP3A4 in human liver microsomes assessed as conversion of testosterone to 6beta-hydroxytestosterone at 0.3 to 75 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID290633Displacement of [125I] ITAC from the CXCR3 receptor2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID290631Bioavailability in rat at 2 mg/kg, po2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
AID1218821Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1218855Time dependent inhibition of CYP3A4 in human liver microsomes assessed as conversion of midazolam to 1'-hydroxymidazolam at 0.3 to 75 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID348584Binding affinity to human muscarinic M1 receptor2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists.
[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's5 (41.67)29.6817
2010's5 (41.67)24.3611
2020's2 (16.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 31.50

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 Index31.50 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.60 (4.65)
Search Engine Demand Index32.77 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (31.50)

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%
Other12 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]