Compounds > incb 3284
Page last updated: 2024-11-12

incb 3284

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

Description

INCB 3284: a CCR2 receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11527661
CHEMBL ID1963131
CHEMBL ID1951790
CHEMBL ID1951778
SCHEMBL ID745198
SCHEMBL ID5058152
SCHEMBL ID5058151
SCHEMBL ID14281986
MeSH IDM000603282

Synonyms (34)

Synonym
incb3284
bdbm50363953
chembl1963131 ,
CHEMBL1951790
CHEMBL1951778 ,
SCHEMBL745198
incb 3284 enantiomer 1
CS-3565
CS-M3083
SCHEMBL5058152
SCHEMBL5058151
unii-0w6k09gaqb
benzamide, n-(2-(((3r)-1-(trans-4-hydroxy-4-(6-methoxy-3-pyridinyl)cyclohexyl)-3-pyrrolidinyl)amino)-2-oxoethyl)-3-(trifluoromethyl)-
0w6k09gaqb ,
incb-3284
887401-92-5
SCHEMBL14281986
incb-003284
incb003284
incb 3284
HY-15450A
n-[2-[[(3r)-1-[4-hydroxy-4-(6-methoxypyridin-3-yl)cyclohexyl]pyrrolidin-3-yl]amino]-2-oxoethyl]-3-(trifluoromethyl)benzamide
gtpl9045
compound 13 [pmid: 24900329]
Z3247512485
NCGC00370911-01
Q27231179
incb3284 free base
MS-29653
NCGC00370911-04
nxznybubxwwkcp-dnrqzrrgsa-n
E82922
nxznybubxwwkcp-ldjsfyousa-n
AKOS040733443

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"7 nM in antagonism of chemotaxis activity, an IC50 of 84 μM in inhibition of the hERG potassium current, a free fraction of 58% in protein binding, high selectivity over other chemokine receptors and G-protein-coupled receptors, and acceptable oral bioavailability in rodents and primates."( Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist.
Anand, R; Cao, G; Chen, L; Contel, N; Covington, M; Diamond, S; Emm, T; Feng, H; Friedman, S; Galya, LG; Glenn, J; Han, Q; Hollis, G; Huang, T; Kong, L; Li, M; Meloni, D; Metcalf, B; Modi, D; Newton, R; Robinson, DJ; Scherle, P; Shao, L; Sharief, V; Storace, L; Tanaka, H; Vaddi, K; Wang, A; Xia, M; Xue, CB; Yeleswaram, S; Zhang, K; Zhang, Y; Zheng, C, 2011)		0.37
"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
" In human clinical trials, INCB3284 exhibited a pharmacokinetic profile suitable for once-a-day dosing (T 1/2 = 15 h)."( Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist.
Anand, R; Cao, G; Chen, L; Contel, N; Covington, M; Diamond, S; Emm, T; Feng, H; Friedman, S; Galya, LG; Glenn, J; Han, Q; Hollis, G; Huang, T; Kong, L; Li, M; Meloni, D; Metcalf, B; Modi, D; Newton, R; Robinson, DJ; Scherle, P; Shao, L; Sharief, V; Storace, L; Tanaka, H; Vaddi, K; Wang, A; Xia, M; Xue, CB; Yeleswaram, S; Zhang, K; Zhang, Y; Zheng, C, 2011)		0.37
" Our findings further support the assumption that blockade of the major CCL2 receptor CCR2 is a promising approach to improve FR after HS and document that the dosing of INCB3284 can be optimized."( Effects of chemokine (C-C motif) receptor 2 and 3 antagonists in rat models of hemorrhagic shock.
DeSantis, AJ; Enten, GA; Gao, X; Majetschak, M; McGee, MY; Weche, M, 2023)		0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency21.31740.01237.983543.2770AID1645841
cytochrome P450 2D6Homo sapiens (human)Potency10.68400.00108.379861.1304AID1645840
[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 2Homo sapiens (human)IC50 (µMol)0.00420.00000.67366.6990AID662865; AID662866
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (54)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (8)

Assay IDTitleYearJournalArticle
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.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
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.
AID662866Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy2011ACS medicinal chemistry letters, Dec-08, Volume: 2, Issue:12
Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.
AID662865Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting2011ACS medicinal chemistry letters, Dec-08, Volume: 2, Issue:12
Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.
AID645526Displacement of [125I]MCP1 from CCR2 in human PBMC at 1 uM after 30 mins by gamma counter2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (62.50)24.3611
2020's3 (37.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.36

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.36 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.36)

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%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
glycine
[no description available]		3.4220alpha-amino acid;
amino acid zwitterion;
proteinogenic amino acid;
serine family amino acid		EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor;
fundamental metabolite;
hepatoprotective agent;
micronutrient;
neurotransmitter;
NMDA receptor agonist;
nutraceutical
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		2.110azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
azoxymethane
Azoxymethane: A potent carcinogen and neurotoxic compound. It is particularly effective in inducing colon carcinomas.		2.110
ConditionIndicatedRelationship StrengthStudiesTrials
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		04.0140
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Bleeding
[description not available]		02.610
Hemorrhagic Shock
[description not available]		02.610
Hemorrhage
Bleeding or escape of blood from a vessel.		02.610
Blood Pressure, High
[description not available]		03.0310
Innate Inflammatory Response
[description not available]		03.0310
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		03.0310
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		03.0310
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		02.110
Encephalopathy, Hepatic
[description not available]		02.110
Nervous System Disorders
[description not available]		02.110
Hepatic Encephalopathy
A syndrome characterized by central nervous system dysfunction in association with LIVER FAILURE, including portal-systemic shunts. Clinical features include lethargy and CONFUSION (frequently progressing to COMA); ASTERIXIS; NYSTAGMUS, PATHOLOGIC; brisk oculovestibular reflexes; decorticate and decerebrate posturing; MUSCLE SPASTICITY; and bilateral extensor plantar reflexes (see REFLEX, BABINSKI). ELECTROENCEPHALOGRAPHY may demonstrate triphasic waves. (From Adams et al., Principles of Neurology, 6th ed, pp1117-20; Plum & Posner, Diagnosis of Stupor and Coma, 3rd ed, p222-5)		02.110
Nervous System Diseases
Diseases of the central and peripheral nervous system. This includes disorders of the brain, spinal cord, cranial nerves, peripheral nerves, nerve roots, autonomic nervous system, neuromuscular junction, and muscle.		02.110