Page last updated: 2024-11-12

incb3344

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Description

INCB3344: potent and selective small molecule CCR2 chemokine receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10008367
CHEMBL ID1289316
CHEMBL ID2426341
SCHEMBL ID747726
MeSH IDM0492446

Synonyms (35)

Synonym
HY-50674
incb 3344
gtpl777
incb3344
cid 10008367
n-(2-((3s,4s)-1-(cis-4-(benzo[d][1,3]dioxol-5-yl)-4-hydroxycyclohexyl)-4-ethoxypyrrolidin-3-ylamino)-2-oxoethyl)-3-(trifluoromethyl)benzamide
bdbm50331728
CHEMBL1289316 ,
incb-3344
CHEMBL2426341
n-(2-(((3s,4s)-1-(4-(benzo[d][1,3]dioxol-5-yl)-4-hydroxycyclohexyl)-4-ethoxypyrrolidin-3-yl)amino)-2-oxoethyl)-3-(trifluoromethyl)benzamide
709018-37-1
CS-0347
cis-incb3344
CS-M1486
SCHEMBL747726
1262238-11-8
NCGC00378837-01
CS-0058750
HY-50674A
incb3344 r-isomer
benzamide, n-[2-[[(3r,4r)-1-[cis-4-(1,3-benzodioxol-5-yl)-4-hydroxycyclohexyl]-4-ethoxy-3-pyrrolidinyl]amino]-2-oxoethyl]-3-(trifluoromethyl)-, rel-
1285539-85-6
n-(2-(((3s,4s)-1-((1r,4s)-4-(benzo[d][1,3]dioxol-5-yl)-4-hydroxycyclohexyl)-4-ethoxypyrrolidin-3-yl)amino)-2-oxoethyl)-3-(trifluoromethyl)benzamide
CS-13932
n-(2-(((3s,4s)-1-((1s,4r)-4-(benzo[d][1,3]dioxol-5-yl)-4-hydroxycyclohexyl)-4-ethoxypyrrolidin-3-yl)amino)-2-oxoethyl)-3-(trifluoromethyl)benzamide
A906838
F82231
MS-30386
n-[2-[[(3s,4s)-1-[4-(1,3-benzodioxol-5-yl)-4-hydroxycyclohexyl]-4-ethoxypyrrolidin-3-yl]amino]-2-oxoethyl]-3-(trifluoromethyl)benzamide
AKOS037649947
mzeosvpwmsefpw-xycdvdstsa-n
HY-77111
rel-n-[2-[[(3r,4r)-1-[cis-4-(1,3-benzodioxol-5-yl)-4-hydroxycyclohexyl]-4-ethoxy-3-pyrrolidinyl]amino]-2-oxoethyl]-3-(trifluoromethyl)benzamide
DTXSID701100838

Research Excerpts

Treatment

INCB3344 treatment significantly inhibited macrophage infiltration into the laser-irradiated area. Mice treated with the drug exhibited markedly worse functional outcomes and larger infarct volumes.

ExcerptReferenceRelevance
"INCB3344 treatment results in a dose-dependent inhibition of macrophage influx in a mouse model of delayed-type hypersensitivity."( Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344.
Baribaud, F; Brodmerkel, CM; Burn, T; Collier, P; Collins, R; Covington, M; Diamond, S; Feldman, P; Friedman, S; Gallagher, K; Gu, X; Hall, L; Hollis, G; Huber, R; Leffet, L; Newton, RC; Scherle, P; Shin, N; Solomon, K; Stow, M; Thomas, B; Vaddi, K; Wang, A; Xue, CB; Yeleswaram, S, 2005
)
1.27
"INCB3344 treatment significantly inhibited macrophage infiltration into the laser-irradiated area (p<0.001), and suppressed the expression of VEGF protein (pā€Š=ā€Š0.012), VEGF mRNA in infiltrating macrophages (p<0.001) and the phosphorylation of ERK1/2 (p<0.001)."( Suppression and regression of choroidal neovascularization in mice by a novel CCR2 antagonist, INCB3344.
Kamei, M; Matsumura, N; Nishida, K; Sakaguchi, H; Sakimoto, S; Suzuki, M; Xie, P, 2011
)
1.31
"Mice treated with INCB3344 exhibited markedly worse functional outcomes and larger infarct volumes, in association with reduced M2 polarization and increased peroxynitrite production in macrophages, compared with vehicle-treated mice."( Evidence That Ly6C(hi) Monocytes are Protective in Acute Ischemic Stroke by Promoting M2 Macrophage Polarization.
Broughton, BR; Chu, HX; Drummond, GR; Kim, HA; Lee, S; Sobey, CG, 2015
)
0.74

Bioavailability

IncNB3344 exhibited >100-fold selectivity over other homologous chemokine receptors. Free fraction of 24% in human serum and 15% in mouse serum. Oral bioavailability of 47% in mice.

ExcerptReferenceRelevance
" INCB3344 possesses good oral bioavailability and systemic exposure in rodents that allows in vivo pharmacological studies."( Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344.
Baribaud, F; Brodmerkel, CM; Burn, T; Collier, P; Collins, R; Covington, M; Diamond, S; Feldman, P; Friedman, S; Gallagher, K; Gu, X; Hall, L; Hollis, G; Huber, R; Leffet, L; Newton, RC; Scherle, P; Shin, N; Solomon, K; Stow, M; Thomas, B; Vaddi, K; Wang, A; Xue, CB; Yeleswaram, S, 2005
)
1.46
" INCB3344 exhibited >100-fold selectivity over other homologous chemokine receptors, a free fraction of 24% in human serum and 15% in mouse serum, and an oral bioavailability of 47% in mice, suitable as a tool compound for target validation in rodent models."( Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
Anand, R; Brodmerkel, CM; Cao, G; Covington, M; Diamond, S; Feng, H; Friedman, S; Glenn, J; Han, Q; Hollis, G; Huang, T; Kong, L; Li, M; Meloni, D; Metcalf, B; Newton, R; Robinson, DJ; Scherle, P; Shao, L; Storace, L; Vaddi, K; Wang, A; Xia, M; Xue, CB; Yeleswaram, S; Zhang, K; Zhang, Y; Zheng, C, 2010
)
1.64
"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

Dosage Studied

ExcerptRelevanceReference
" We demonstrate that therapeutic dosing of INCB3344 significantly reduces disease in mice subjected to experimental autoimmune encephalomyelitis, a model of multiple sclerosis, as well as a rat model of inflammatory arthritis."( Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344.
Baribaud, F; Brodmerkel, CM; Burn, T; Collier, P; Collins, R; Covington, M; Diamond, S; Feldman, P; Friedman, S; Gallagher, K; Gu, X; Hall, L; Hollis, G; Huber, R; Leffet, L; Newton, RC; Scherle, P; Shin, N; Solomon, K; Stow, M; Thomas, B; Vaddi, K; Wang, A; Xue, CB; Yeleswaram, S, 2005
)
0.81
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.33790.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency11.98770.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency3.37860.00108.379861.1304AID1645840
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)
C-C chemokine receptor type 2Rattus norvegicus (Norway rat)IC50 (µMol)7.30007.30007.30007.3000AID539996
C-C chemokine receptor type 2Homo sapiens (human)IC50 (µMol)0.00450.00000.67366.6990AID539989; AID539991
C-C chemokine receptor type 1Mus musculus (house mouse)IC50 (µMol)1.00000.00580.91425.0000AID539998
C-C chemokine receptor type 5Mus musculus (house mouse)IC50 (µMol)3.00000.00030.00170.0052AID539999
C-C chemokine receptor type 2Mus musculus (house mouse)IC50 (µMol)0.00860.00780.00860.0095AID539990; AID539992
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)13.00000.00091.901410.0000AID539995
[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 motif chemokine 2Homo sapiens (human)Kd0.00080.00020.00080.0012AID771593; AID771594; AID771595; AID771596
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (149)

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-C motif chemokine 2Homo sapiens (human)
monocyte chemotaxisC-C motif chemokine 2Homo sapiens (human)
protein phosphorylationC-C motif chemokine 2Homo sapiens (human)
chemotaxisC-C motif chemokine 2Homo sapiens (human)
humoral immune responseC-C motif chemokine 2Homo sapiens (human)
cytoskeleton organizationC-C motif chemokine 2Homo sapiens (human)
cell adhesionC-C motif chemokine 2Homo sapiens (human)
signal transductionC-C motif chemokine 2Homo sapiens (human)
cell surface receptor signaling pathwayC-C motif chemokine 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayC-C motif chemokine 2Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerC-C motif chemokine 2Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATC-C motif chemokine 2Homo sapiens (human)
regulation of cell shapeC-C motif chemokine 2Homo sapiens (human)
response to bacteriumC-C motif chemokine 2Homo sapiens (human)
animal organ morphogenesisC-C motif chemokine 2Homo sapiens (human)
viral genome replicationC-C motif chemokine 2Homo sapiens (human)
cytokine-mediated signaling pathwayC-C motif chemokine 2Homo sapiens (human)
sensory perception of painC-C motif chemokine 2Homo sapiens (human)
cellular homeostasisC-C motif chemokine 2Homo sapiens (human)
negative regulation of glial cell apoptotic processC-C motif chemokine 2Homo sapiens (human)
helper T cell extravasationC-C motif chemokine 2Homo sapiens (human)
negative regulation of neuron apoptotic processC-C motif chemokine 2Homo sapiens (human)
astrocyte cell migrationC-C motif chemokine 2Homo sapiens (human)
cellular response to fibroblast growth factor stimulusC-C motif chemokine 2Homo sapiens (human)
macrophage chemotaxisC-C motif chemokine 2Homo sapiens (human)
positive regulation of T cell activationC-C motif chemokine 2Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processC-C motif chemokine 2Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicC-C motif chemokine 2Homo sapiens (human)
cellular response to lipopolysaccharideC-C motif chemokine 2Homo sapiens (human)
cellular response to type II interferonC-C motif chemokine 2Homo sapiens (human)
cellular response to interleukin-1C-C motif chemokine 2Homo sapiens (human)
cellular response to tumor necrosis factorC-C motif chemokine 2Homo sapiens (human)
positive regulation of calcium ion importC-C motif chemokine 2Homo sapiens (human)
positive regulation of NMDA glutamate receptor activityC-C motif chemokine 2Homo sapiens (human)
negative regulation of vascular endothelial cell proliferationC-C motif chemokine 2Homo sapiens (human)
negative regulation of G1/S transition of mitotic cell cycleC-C motif chemokine 2Homo sapiens (human)
positive regulation of endothelial cell apoptotic processC-C motif chemokine 2Homo sapiens (human)
positive regulation of apoptotic cell clearanceC-C motif chemokine 2Homo sapiens (human)
negative regulation of natural killer cell chemotaxisC-C motif chemokine 2Homo sapiens (human)
positive regulation of cell migrationC-C motif chemokine 2Homo sapiens (human)
positive regulation of GTPase activityC-C motif chemokine 2Homo sapiens (human)
antimicrobial humoral immune response mediated by antimicrobial peptideC-C motif chemokine 2Homo sapiens (human)
inflammatory responseC-C motif chemokine 2Homo sapiens (human)
eosinophil chemotaxisC-C motif chemokine 2Homo sapiens (human)
chemokine-mediated signaling pathwayC-C motif chemokine 2Homo sapiens (human)
cytokine-mediated signaling pathwayC-C chemokine receptor type 2Homo sapiens (human)
blood vessel remodelingC-C chemokine receptor type 2Homo sapiens (human)
dendritic cell chemotaxisC-C chemokine receptor type 2Homo sapiens (human)
monocyte chemotaxisC-C chemokine receptor type 2Homo sapiens (human)
regulation of T cell cytokine productionC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of T-helper 1 type immune responseC-C chemokine receptor type 2Homo sapiens (human)
negative regulation of type 2 immune responseC-C chemokine receptor type 2Homo sapiens (human)
intracellular calcium ion homeostasisC-C chemokine receptor type 2Homo sapiens (human)
chemotaxisC-C chemokine receptor type 2Homo sapiens (human)
humoral immune responseC-C chemokine receptor type 2Homo sapiens (human)
cellular defense responseC-C chemokine receptor type 2Homo sapiens (human)
negative regulation of adenylate cyclase activityC-C chemokine receptor type 2Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATC-C chemokine receptor type 2Homo sapiens (human)
response to woundingC-C chemokine receptor type 2Homo sapiens (human)
regulation of vascular endothelial growth factor productionC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of T cell chemotaxisC-C chemokine receptor type 2Homo sapiens (human)
negative regulation of angiogenesisC-C chemokine receptor type 2Homo sapiens (human)
sensory perception of painC-C chemokine receptor type 2Homo sapiens (human)
cellular homeostasisC-C chemokine receptor type 2Homo sapiens (human)
hemopoiesisC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of type II interferon productionC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of interleukin-2 productionC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of tumor necrosis factor productionC-C chemokine receptor type 2Homo sapiens (human)
monocyte extravasationC-C chemokine receptor type 2Homo sapiens (human)
T-helper 17 cell chemotaxisC-C chemokine receptor type 2Homo sapiens (human)
negative regulation of eosinophil degranulationC-C chemokine receptor type 2Homo sapiens (human)
regulation of T cell differentiationC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of alpha-beta T cell proliferationC-C chemokine receptor type 2Homo sapiens (human)
homeostasis of number of cells within a tissueC-C chemokine receptor type 2Homo sapiens (human)
regulation of inflammatory responseC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of inflammatory responseC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of T cell activationC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicC-C chemokine receptor type 2Homo sapiens (human)
leukocyte adhesion to vascular endothelial cellC-C chemokine receptor type 2Homo sapiens (human)
chemokine-mediated signaling pathwayC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of monocyte chemotaxisC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of immune complex clearance by monocytes and macrophagesC-C chemokine receptor type 2Homo sapiens (human)
inflammatory response to woundingC-C chemokine receptor type 2Homo sapiens (human)
neutrophil clearanceC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of cold-induced thermogenesisC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of leukocyte tethering or rollingC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of NMDA glutamate receptor activityC-C chemokine receptor type 2Homo sapiens (human)
macrophage migrationC-C chemokine receptor type 2Homo sapiens (human)
regulation of macrophage migrationC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of thymocyte migrationC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of monocyte extravasationC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of CD8-positive, alpha-beta T cell extravasationC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of astrocyte chemotaxisC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of hematopoietic stem cell migrationC-C chemokine receptor type 2Homo sapiens (human)
cell chemotaxisC-C chemokine receptor type 2Homo sapiens (human)
calcium-mediated signalingC-C chemokine receptor type 2Homo sapiens (human)
inflammatory responseC-C chemokine receptor type 2Homo sapiens (human)
immune responseC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationC-C chemokine receptor type 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo 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 (39)

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)
protein kinase activityC-C motif chemokine 2Homo sapiens (human)
signaling receptor bindingC-C motif chemokine 2Homo sapiens (human)
protein bindingC-C motif chemokine 2Homo sapiens (human)
CCR2 chemokine receptor bindingC-C motif chemokine 2Homo sapiens (human)
chemokine activityC-C motif chemokine 2Homo sapiens (human)
CCR chemokine receptor bindingC-C motif chemokine 2Homo sapiens (human)
chemokine receptor activityC-C chemokine receptor type 2Homo sapiens (human)
protein bindingC-C chemokine receptor type 2Homo sapiens (human)
CCR2 chemokine receptor bindingC-C chemokine receptor type 2Homo sapiens (human)
chemokine (C-C motif) ligand 2 bindingC-C chemokine receptor type 2Homo sapiens (human)
chemokine (C-C motif) ligand 12 bindingC-C chemokine receptor type 2Homo sapiens (human)
chemokine (C-C motif) ligand 7 bindingC-C chemokine receptor type 2Homo sapiens (human)
identical protein bindingC-C chemokine receptor type 2Homo sapiens (human)
C-C chemokine bindingC-C chemokine receptor type 2Homo sapiens (human)
C-C chemokine receptor activityC-C chemokine receptor type 2Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo 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 (28)

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)
extracellular regionC-C motif chemokine 2Homo sapiens (human)
extracellular spaceC-C motif chemokine 2Homo sapiens (human)
fibrillar centerC-C chemokine receptor type 2Homo sapiens (human)
cytoplasmC-C chemokine receptor type 2Homo sapiens (human)
cytosolC-C chemokine receptor type 2Homo sapiens (human)
plasma membraneC-C chemokine receptor type 2Homo sapiens (human)
membraneC-C chemokine receptor type 2Homo sapiens (human)
dendriteC-C chemokine receptor type 2Homo sapiens (human)
neuronal cell bodyC-C chemokine receptor type 2Homo sapiens (human)
perikaryonC-C chemokine receptor type 2Homo sapiens (human)
perinuclear region of cytoplasmC-C chemokine receptor type 2Homo sapiens (human)
cytoplasmC-C chemokine receptor type 2Homo sapiens (human)
external side of plasma membraneC-C chemokine receptor type 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo 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 (29)

Assay IDTitleYearJournalArticle
AID539993Protein binding in human serum assessed as unbound fraction2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID539989Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID539997Inhibition of cynomolgus CCR22010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID539990Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID539995Inhibition of human ERG2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID540003Cmax in CD-1 mouse at 10 mg/kg, po2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID540000Clearance in CD-1 mouse at 5 mg/kg, iv2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID539992Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID539991Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID540002Half life in CD-1 mouse at 5 mg/kg, iv2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID539994Protein binding in mouse serum assessed as unbound fraction2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID540007AUC in BALB/c mouse at 10 mg/kg, po2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID540006Cmax in BALB/c mouse at 10 mg/kg, po2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID540001Volume of distribution at steady state in CD-1 mouse at 5 mg/kg, iv2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID540004AUC in CD-1 mouse at 10 mg/kg, po2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID539999Inhibition of mouse CCR52010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID539998Inhibition of mouse CCR12010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID539996Inhibition of rat CCR22010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
AID540005Oral bioavailability in CD-1 mouse at 10 mg/kg, po2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
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.
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.
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.
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.
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.
AID1346744Mouse CCR2 (Chemokine receptors)2005Journal of immunology (Baltimore, Md. : 1950), Oct-15, Volume: 175, Issue:8
Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344.
AID771594Displacement of [3H]INCB3344 from human CCR2 receptor expressed in human U2OS cell membranes assessed as association and dissociation of radioligand2013Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19
Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists.
AID771595Displacement of [3H]INCB3344 from human CCR2 receptor expressed in human U2OS cell membranes2013Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19
Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists.
AID771593Displacement of [3H]INCB3344 from human CCR2 receptor expressed in human U2OS cell membranes assessed as association and dissociation of compound by competition association assay2013Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19
Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists.
AID771596Displacement of [3H]INCB3344 from human CCR2 receptor expressed in human U2OS cell membranes by saturation binding assay2013Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19
Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (23)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (13.04)29.6817
2010's15 (65.22)24.3611
2020's5 (21.74)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.25

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 Index21.25 (24.57)
Research Supply Index3.18 (2.92)
Research Growth Index5.13 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.25)

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%
Other23 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]