Page last updated: 2024-12-08

bx 471

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

Description

BX 471: a CC chemokine receptor-1 antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID512282
CHEMBL ID232656
CHEMBL ID535607
SCHEMBL ID4586646
MeSH IDM0367733

Synonyms (44)

Synonym
gtpl767
[5-chloro-2-[2-[(2r)-4-[(4-fluorophenyl)methyl]-2-methyl-piperazin-1-yl]-2-oxo-ethoxy]phenyl]urea
urea, n-[5-chloro-2-[2-[(2r)-4-[(4-fluorophenyl)methyl]-2-methyl-1-piperazinyl]-2-oxoethoxy]phenyl]-
bx471
bx-741
bx-471
CHEMBL232656 ,
zk-811752
bx 471
[5-chloro-2-[2-[(2r)-4-[(4-fluorophenyl)methyl]-2-methylpiperazin-1-yl]-2-oxoethoxy]phenyl]urea
CHEMBL535607 ,
bdbm50174703
(r)-1-(2-(2-(4-(4-fluorobenzyl)-2-methylpiperazin-1-yl)-2-oxoethoxy)-5-chlorophenyl)urea hydrochloride
bdbm50208999
(r)-1-(5-chloro-2-(2-(4-(4-fluorobenzyl)-2-methylpiperazin-1-yl)-2-oxoethoxy)phenyl)urea
(r)-1-(2-(2-(4-(4-fluorobenzyl)-2-methylpiperazin-1-yl)-2-oxoethoxy)-5-chlorophenyl)urea
217645-70-0
(2r)-1-(((4-chloro-2-(ureido)phenoxy)methyl)carbonyl)-2-methyl-4-(4-fluorobenzyl)piperazine
bx-471 free base
urea, n-(5-chloro-2-(2-((2r)-4-((4-fluorophenyl)methyl)-2-methyl-1-piperazinyl)-2-oxoethoxy)phenyl)-
unii-76k17zg4zn
76k17zg4zn ,
CS-3283
HY-12080
1-(2-(2-((r)-4-(4-fluorobenzyl)-2-methylpiperazin-1-yl)-2-oxoethoxy)-5-chlorophenyl)urea
c21h24clfn4o3
SCHEMBL4586646
(2r)-1-[[2-[(aminocarbonyl)amino]-4-chlorophenoxy]acetyl]-4-[(4-fluorophenyl)methyl]-2-methylpiperazine
B6060
AC-31379
AKOS024457640
n-[5-chloro-2-[2-[(2r)-4-[(4-fluorophenyl)methyl]-2-methyl-1-piperazinyl]-2-oxoethoxy]phenyl]-urea
DTXSID10176164
J-690262
EX-A519
bx-471free base
mfcd09859709
NCGC00370909-03
bx-471zk 811752
BS-16630
Q27075605
zk-811752(bx-471)
A14409
NCGC00370909-05

Research Excerpts

Treatment

ExcerptReferenceRelevance
"BX 471 treatment did not effectively reduce signs of acute rejection at day 10 but significantly improved allograft function and morphology at day 21 posttransplantation."( Beneficial effects of CCR1 blockade on the progression of chronic renal allograft damage.
Bedke, J; Behnes, CL; Bonrouhi, M; Diedrichs-Moehring, M; Gretz, N; Gröne, HJ; Horuk, R; Kiss, E; Nelson, PJ; Schaefer, L; Wildner, G, 2007
)
1.06

Bioavailability

ExcerptReferenceRelevance
" Pharmacokinetic studies demonstrated that BX 471 was orally active with a bioavailability of 60% in dogs."( Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1.
Bauman, JG; Buckman, B; Dunning, L; Ghannam, A; Harvey, S; Hesselgesser, J; Ho, E; Islam, I; Liang, M; Mallari, C; May, K; Monahan, S; Morrissey, MM; Ng, HP; Oanh, H; Perez, HD; Rosser, M; Shaw, K; Shen, J; Snider, RM; Subramanyam, B; Taub, D; Vergona, R; Wei, GP; Xu, W; Zhao, Z, 2000
)
0.57
"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 (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.75640.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency4.77240.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency21.31740.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency4.77240.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency4.77240.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency4.77240.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency4.77240.01238.964839.8107AID1645842
[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-C chemokine receptor type 1Homo sapiens (human)IC50 (µMol)0.01090.00070.20022.5000AID1573704; AID1573705; AID295387; AID296156; AID296157; AID371426; AID371427
C-C chemokine receptor type 1Homo sapiens (human)Ki0.00100.00100.03300.0740AID707909
C-C chemokine receptor type 1Mus musculus (house mouse)IC50 (µMol)0.61500.00580.91425.0000AID296158
C-C motif chemokine receptor 1 Rattus norvegicus (Norway rat)IC50 (µMol)0.05900.05900.05900.0590AID296159
[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)
C-C chemokine receptor type 1Homo sapiens (human)Kd0.00100.00100.00100.0010AID707902
C-C chemokine receptor type 1Mus musculus (house mouse)Kd0.20000.20000.20000.2000AID707901
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
interferon gamma precursorHomo sapiens (human)AC5039.00000.128015.173038.6100AID1259418; AID1259420
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (67)

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)
dendritic cell chemotaxisC-C chemokine receptor type 1Homo sapiens (human)
monocyte chemotaxisC-C chemokine receptor type 1Homo sapiens (human)
calcium ion transportC-C chemokine receptor type 1Homo sapiens (human)
intracellular calcium ion homeostasisC-C chemokine receptor type 1Homo sapiens (human)
exocytosisC-C chemokine receptor type 1Homo sapiens (human)
chemotaxisC-C chemokine receptor type 1Homo sapiens (human)
immune responseC-C chemokine receptor type 1Homo sapiens (human)
cell adhesionC-C chemokine receptor type 1Homo sapiens (human)
cell surface receptor signaling pathwayC-C chemokine receptor type 1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerC-C chemokine receptor type 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationC-C chemokine receptor type 1Homo sapiens (human)
cell-cell signalingC-C chemokine receptor type 1Homo sapiens (human)
response to woundingC-C chemokine receptor type 1Homo sapiens (human)
negative regulation of gene expressionC-C chemokine receptor type 1Homo sapiens (human)
cytokine-mediated signaling pathwayC-C chemokine receptor type 1Homo sapiens (human)
positive regulation of cell migrationC-C chemokine receptor type 1Homo sapiens (human)
negative regulation of bone mineralizationC-C chemokine receptor type 1Homo sapiens (human)
positive regulation of osteoclast differentiationC-C chemokine receptor type 1Homo sapiens (human)
positive regulation of calcium ion transportC-C chemokine receptor type 1Homo sapiens (human)
chemokine-mediated signaling pathwayC-C chemokine receptor type 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeC-C chemokine receptor type 1Homo sapiens (human)
positive regulation of monocyte chemotaxisC-C chemokine receptor type 1Homo sapiens (human)
calcium-mediated signalingC-C chemokine receptor type 1Homo sapiens (human)
cell chemotaxisC-C chemokine receptor type 1Homo sapiens (human)
inflammatory responseC-C chemokine receptor type 1Homo 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 (24)

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)
phosphatidylinositol phospholipase C activityC-C chemokine receptor type 1Homo sapiens (human)
chemokine receptor activityC-C chemokine receptor type 1Homo sapiens (human)
protein bindingC-C chemokine receptor type 1Homo sapiens (human)
C-C chemokine receptor activityC-C chemokine receptor type 1Homo sapiens (human)
C-C chemokine bindingC-C chemokine receptor type 1Homo sapiens (human)
chemokine (C-C motif) ligand 7 bindingC-C chemokine receptor type 1Homo sapiens (human)
chemokine (C-C motif) ligand 5 bindingC-C chemokine receptor type 1Homo 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)
plasma membraneC-C chemokine receptor type 1Homo sapiens (human)
external side of plasma membraneC-C chemokine receptor type 1Homo sapiens (human)
external side of plasma membraneC-C chemokine receptor type 1Homo sapiens (human)
cytoplasmC-C chemokine receptor type 1Homo 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 (41)

Assay IDTitleYearJournalArticle
AID295395Bioavailability in rat2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID295389Metabolic stability in human liver microsomes2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID295394Bioavailability in monkey2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID707909Binding affinity to CCR12012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID707899Half life in human2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID295398Plasma clearance in iv dosed rat2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID295392Metabolic stability in monkey liver microsomes2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID1573565Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Pyrrolone Derivatives as Intracellular Allosteric Modulators for Chemokine Receptors: Selective and Dual-Targeting Inhibitors of CC Chemokine Receptors 1 and 2.
AID707902Binding affinity to human CCR1 by radioligand binding assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID1573705Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Discovery and optimization of pyrazole amides as antagonists of CCR1.
AID295390Metabolic stability in rat liver microsomes2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID296157Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Structure-activity relationships of novel, highly potent, selective, and orally active CCR1 antagonists.
AID295399Volume of distribution at steady state in dog2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID295388Activity at CCL3 by chemotaxis assay2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID1573574Increase in [3H]-CCR2-RA-[R] binding to human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor at 10 uM after 120 mins by scintillation spectrometry relative to control2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Pyrrolone Derivatives as Intracellular Allosteric Modulators for Chemokine Receptors: Selective and Dual-Targeting Inhibitors of CC Chemokine Receptors 1 and 2.
AID295403Half life in monkey2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID295401Volume of distribution at steady state in rat2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID371426Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Novel pyrrolidine ureas as C-C chemokine receptor 1 (CCR1) antagonists.
AID707908Lipophilicity, log P of the compound2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID295404Half life in rat2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID295402Half life in dog2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID1573704Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Discovery and optimization of pyrazole amides as antagonists of CCR1.
AID296159Binding affinity at rat CCR12007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Structure-activity relationships of novel, highly potent, selective, and orally active CCR1 antagonists.
AID295400Volume of distribution at steady state in monkey2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID295391Metabolic stability in dog liver microsomes2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID707901Binding affinity to mouse CCR1 by radioligand binding assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID295393Bioavailability in dog2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID295396Plasma clearance in iv dosed dog2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID296158Binding affinity at mouse CCR12007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Structure-activity relationships of novel, highly potent, selective, and orally active CCR1 antagonists.
AID295397Plasma clearance in monkey2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID707900Binding affinity to rat CCR1 by radioligand binding assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID371427Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Novel pyrrolidine ureas as C-C chemokine receptor 1 (CCR1) antagonists.
AID295387Binding Affinity at CCL32007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
AID296156Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Structure-activity relationships of novel, highly potent, selective, and orally active CCR1 antagonists.
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.
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.
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.
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.
AID1346789Human CCR1 (Chemokine receptors)2000The Journal of biological chemistry, Jun-23, Volume: 275, Issue:25
Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (41)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's25 (60.98)29.6817
2010's11 (26.83)24.3611
2020's5 (12.20)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.92

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 Index19.92 (24.57)
Research Supply Index3.83 (2.92)
Research Growth Index6.11 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.92)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (7.14%)5.53%
Reviews5 (11.90%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other34 (80.95%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]