CCR8
gene geneOn this page
Also known as CY6TER1CKR-L1GPR-CY6CDw198
Summary
CCR8 (C-C motif chemokine receptor 8, HGNC:1609) is a protein-coding gene on chromosome 3p22.1, encoding C-C chemokine receptor type 8 (P51685). G protein-coupled receptor that can bind a variety of chemokines, such as CCL1, CCL8, CCL16, CCL18.
This gene encodes a member of the beta chemokine receptor family, which is predicted to be a seven transmembrane protein similar to G protein-coupled receptors. Chemokines and their receptors are important for the migration of various cell types into the inflammatory sites. This receptor protein preferentially expresses in the thymus. I-309, thymus activation-regulated cytokine (TARC) and macrophage inflammatory protein-1 beta (MIP-1 beta) have been identified as ligands of this receptor. Studies of this receptor and its ligands suggested its role in regulation of monocyte chemotaxis and thymic cell apoptosis. More specifically, this receptor may contribute to the proper positioning of activated T cells within the antigenic challenge sites and specialized areas of lymphoid tissues. This gene is located at the chemokine receptor gene cluster region.
Source: NCBI Gene 1237 — RefSeq curated summary.
At a glance
- GWAS associations: 2
- Clinical variants (ClinVar): 51 total
- Druggable target: yes — 1 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_005201
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:1609 |
| Approved symbol | CCR8 |
| Name | C-C motif chemokine receptor 8 |
| Location | 3p22.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | CY6, TER1, CKR-L1, GPR-CY6, CDw198 |
| Ensembl gene | ENSG00000179934 |
| Ensembl biotype | protein_coding |
| OMIM | 601834 |
| Entrez | 1237 |
Gene structure
Transcript identifiers
Ensembl transcripts: 2 — 2 protein_coding
ENST00000326306, ENST00000414803
RefSeq mRNA: 1 — MANE Select: NM_005201
NM_005201
CCDS: CCDS2684
Canonical transcript exons
ENST00000326306 — 2 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001288442 | 39329709 | 39329829 |
| ENSE00001288452 | 39332318 | 39333680 |
Expression profiles
Bgee: expression breadth broad, 38 present calls, max score 92.66.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.5692 / max 145.6795, expressed in 90 samples.
FANTOM5 promoters (4 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 36126 | 0.3647 | 70 |
| 36125 | 0.1380 | 47 |
| 36127 | 0.0423 | 23 |
| 36124 | 0.0240 | 12 |
Top tissues by expression
262 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 92.66 | gold quality |
| buccal mucosa cell | CL:0002336 | 68.21 | gold quality |
| type B pancreatic cell | CL:0000169 | 67.00 | gold quality |
| diaphragm | UBERON:0001103 | 63.08 | gold quality |
| granulocyte | CL:0000094 | 61.26 | gold quality |
| periodontal ligament | UBERON:0008266 | 60.79 | gold quality |
| vermiform appendix | UBERON:0001154 | 59.28 | gold quality |
| mucosa of urinary bladder | UBERON:0001259 | 57.61 | gold quality |
| gall bladder | UBERON:0002110 | 57.61 | gold quality |
| mucosa of paranasal sinus | UBERON:0005030 | 56.70 | gold quality |
| caecum | UBERON:0001153 | 56.46 | gold quality |
| trabecular bone tissue | UBERON:0002483 | 54.84 | gold quality |
| lymph node | UBERON:0000029 | 54.61 | gold quality |
| ileal mucosa | UBERON:0000331 | 54.07 | silver quality |
| skin of hip | UBERON:0001554 | 53.60 | silver quality |
| thymus | UBERON:0002370 | 53.26 | gold quality |
| upper leg skin | UBERON:0004262 | 52.65 | silver quality |
| epithelial cell of pancreas | CL:0000083 | 52.06 | gold quality |
| blood | UBERON:0000178 | 50.82 | gold quality |
| frontal pole | UBERON:0002795 | 50.41 | gold quality |
| middle frontal gyrus | UBERON:0002702 | 50.30 | gold quality |
| quadriceps femoris | UBERON:0001377 | 50.27 | gold quality |
| paraflocculus | UBERON:0005351 | 50.18 | gold quality |
| Brodmann (1909) area 10 | UBERON:0013541 | 50.18 | gold quality |
| pancreatic ductal cell | CL:0002079 | 50.06 | silver quality |
| vastus lateralis | UBERON:0001379 | 49.32 | gold quality |
| Brodmann (1909) area 46 | UBERON:0006483 | 49.30 | gold quality |
| blood vessel layer | UBERON:0004797 | 49.29 | gold quality |
| cerebellar vermis | UBERON:0004720 | 49.25 | gold quality |
| cervix squamous epithelium | UBERON:0006922 | 49.20 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-CURD-89 | yes | 580.64 |
| E-ANND-3 | no | 2.76 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): STAT6
miRNA regulators (miRDB)
16 targeting CCR8, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-12118 | 100.00 | 65.88 | 1270 |
| HSA-MIR-513A-5P | 100.00 | 69.77 | 2465 |
| HSA-MIR-6891-5P | 99.98 | 66.53 | 1372 |
| HSA-MIR-3173-3P | 99.98 | 66.49 | 1217 |
| HSA-MIR-4307 | 99.82 | 70.45 | 3374 |
| HSA-MIR-3614-5P | 99.30 | 65.25 | 837 |
| HSA-MIR-196A-3P | 99.19 | 67.34 | 1204 |
| HSA-MIR-511-5P | 98.97 | 70.94 | 2268 |
| HSA-MIR-501-5P | 98.77 | 68.88 | 1328 |
| HSA-MIR-4755-3P | 98.77 | 65.59 | 1915 |
| HSA-MIR-500A-5P | 98.76 | 69.13 | 1241 |
| HSA-MIR-1178-3P | 98.57 | 67.09 | 890 |
| HSA-MIR-4289 | 98.26 | 66.90 | 810 |
| HSA-MIR-124-5P | 98.11 | 67.65 | 1095 |
| HSA-MIR-1255B-2-3P | 97.80 | 67.04 | 880 |
| HSA-MIR-4642 | 97.52 | 67.60 | 916 |
Literature-anchored findings (GeneRIF, showing 35)
- CCR8 mediates rescue from dexamethasone-induced apoptosis via an ERK-dependent pathway (PMID:12525579)
- found in the central nervous system and is associated with phagocytic macrophages (PMID:12547701)
- CCR8 genes and surrounding genomic regions these genes are the result of the duplication of an ancestral gene prior to the divergence of teleost fish. (PMID:12551893)
- Transfected human CCR8-dependent activation of the RAS/MAPK pathway mediates anti-apoptotic activity of I-309/ CCL1 and vMIP-I. (PMID:12645948)
- The induction of CCR8 under conditions associated with vascular smooth muscle cell proliferation and migration raises the possibility that CCR8 may play an important role in vessel wall pathology. (PMID:14576057)
- the axis CCL1-CCR8 links adaptive and innate immune functions that play a role in the initiation and amplification of atopic skin inflammation (PMID:15814739)
- CCR8 ligands are allotropic, binding to distinct sites within CCR8; the human immune system may have evolved to use CCL7 as a selective antagonist of viral chemokine activity at CCR8 but not those of the host ligand (PMID:17023422)
- CCR8 is expressed by a small and heterogeneous population of peripheral blood CD4 memory T cells enriched in T helper type 2 (Th2) effector and T regulatory (Treg) cells. (PMID:17082609)
- CCR8-expressing CD4-positive T lymphocytes are preferentially recruited from the periphery into the lungs of asthmatic individuals, driven by elevated CCL1 levels produced almost exclusively by mast cells and basophils. (PMID:17641040)
- The combination of 17beta-E(2) with the environmental pollutant TCDD is involved in the pathogenesis of endometriosis via up-regulating the chemokine CCR8-I-309. (PMID:17693327)
- There may be a role for CCR8 in the recruitment of T cells to the lung in asthmatics. (PMID:20455898)
- The functional data from human macrophages suggest a potential cross talk between the CCR8 and the Toll-like receptor 4 (TLR4) pathways, both of which are present in chronic obstructive pulmonary disease patients. (PMID:21976223)
- C-terminal clipping of chemokine CCL1/I-309 enhances CCR8-mediated intracellular calcium release and anti-apoptotic activity (PMID:22479563)
- Data show that CCR8 expression by newly activated naive T cells is regulated by skin-specific factor(s) derived primarily from epidermal keratinocytes. (PMID:23043070)
- CCR8(+) myeloid cell subset is expanded in patients with cancer. (PMID:23363815)
- CCL1-CCR8 interaction may play a critical role in lymphocytic recruitment in IgG4-related sclerosing cholangitis and type 1 autoimmune pancreatitis, leading to duct-centred inflammation and obliterative phlebitis. (PMID:23811304)
- Identification of human CCR8 as a CCL18 receptor. (PMID:23999500)
- findings suggest that CCR8 expression in ALCL is more closely related to the presence of DUSP22 rearrangements than to cutaneous involvement and that the function of CCR8 may extend beyond its skin-homing properties in this disease (PMID:25390351)
- Epidermal-derived vitamin D3 metabolites and prostaglandins provide an essential cue for the localization of CCR8+ immune surveillance T cells within healthy human skin. (PMID:26002980)
- High CCR8 expression is associated with high recurrence in kidney cancer. (PMID:26716905)
- Role of Conserved Disulfide Bridges and Aromatic Residues in Extracellular Loop 2 of Chemokine Receptor CCR8 for Chemokine and Small Molecule Binding. (PMID:27226537)
- Authors demonstrate the pivotal role of CCR8(+) Treg cells in restraining immunity and highlight the potential clinical implications of this discovery. (PMID:28533380)
- Long-lived memory T cells in human skin can be defined by the expression of CCR8. (PMID:29427415)
- Blocking CCR8 via a small molecule inhibitor or short hairpin (sh)RNA mitigated the decrease in Ecadherin, and increase in MMP2 and VEGFC, caused by human recombinant (r)CCL18. CCR8 knockdown by shRNA reversed rCCL18induced cancer cell invasion, migration and epithelialmesenchymal transition (PMID:30592282)
- ARNT-dependent CCR8 reprogrammed LDH isoform expression correlates with poor clinical outcomes of prostate cancer. (PMID:32319143)
- Clinical and prognostic significance of CC chemokine receptor type 8 protein expression in gastrointestinal stromal tumors. (PMID:32884223)
- Chemokine (C-C Motif) Ligand 1 Derived from Tumor-Associated Macrophages Contributes to Esophageal Squamous Cell Carcinoma Progression via CCR8-Mediated Akt/Proline-Rich Akt Substrate of 40 kDa/Mammalian Target of Rapamycin Pathway. (PMID:33460563)
- Immunomodulation of T Helper Cells by Tumor Microenvironment in Oral Cancer Is Associated With CCR8 Expression and Rapid Membrane Vitamin D Signaling Pathway. (PMID:34025655)
- Chemokine CCL18 Promotes Phagocytosis Through Its Receptor CCR8 Rather than PITPNM3 in Human Microglial Cells. (PMID:35041514)
- CCR8-targeted specific depletion of clonally expanded Treg cells in tumor tissues evokes potent tumor immunity with long-lasting memory. (PMID:35140181)
- Differential expression of CCR8 in tumors versus normal tissue allows specific depletion of tumor-infiltrating T regulatory cells by GS-1811, a novel Fc-optimized anti-CCR8 antibody. (PMID:36352891)
- Development of a cellular model to study CCR8 signaling in tumor-infiltrating regulatory T cells. (PMID:38231448)
- Unveiling the structural mechanisms of nonpeptide ligand recognition and activation in human chemokine receptor CCR8. (PMID:38306437)
- Cryo-EM Structure and Biochemical Analysis of the Human Chemokine Receptor CCR8. (PMID:38985857)
- The chemokine receptor CCR8 is not a high-affinity receptor for the human chemokine CCL18. (PMID:39259753)
Cross-species orthologs
8 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | ccr11.1 | ENSDARG00000070755 |
| danio_rerio | ccr2 | ENSDARG00000079829 |
| danio_rerio | cabz01093075.1 | ENSDARG00000086616 |
| danio_rerio | ccr8.1 | ENSDARG00000095789 |
| danio_rerio | si:ch211-207g17.3 | ENSDARG00000105363 |
| danio_rerio | si:cabz01093077.1 | ENSDARG00000105467 |
| mus_musculus | Ccr8 | ENSMUSG00000042262 |
| rattus_norvegicus | Ccr8 | ENSRNOG00000026759 |
Paralogs (23): CCR6 (ENSG00000112486), CCRL2 (ENSG00000121797), CCR2 (ENSG00000121807), CXCR4 (ENSG00000121966), CCR7 (ENSG00000126353), ACKR4 (ENSG00000129048), ACKR3 (ENSG00000144476), ACKR2 (ENSG00000144648), RGR (ENSG00000148604), CXCR5 (ENSG00000160683), CCR5 (ENSG00000160791), CXCR1 (ENSG00000163464), CCR1 (ENSG00000163823), CX3CR1 (ENSG00000168329), CXCR6 (ENSG00000172215), XCR1 (ENSG00000173578), CCR9 (ENSG00000173585), CXCR2 (ENSG00000180871), GALR2 (ENSG00000182687), CCR3 (ENSG00000183625), CCR4 (ENSG00000183813), CCR10 (ENSG00000184451), CXCR3 (ENSG00000186810)
Protein
Protein identifiers
C-C chemokine receptor type 8 — P51685 (reviewed: P51685)
Alternative names: CC chemokine receptor CHEMR1, CMKBRL2, Chemokine receptor-like 1, GPR-CY6, TER1
All UniProt accessions (2): P51685, C9JIP9
UniProt curated annotations — full annotation on UniProt →
Function. G protein-coupled receptor that can bind a variety of chemokines, such as CCL1, CCL8, CCL16, CCL18. Regulates monocyte and eosinophil chemotaxis. Undergoes internalization upon CCL18 binding, leading to induced migration and calcium flux of highly polarized Th2 cells. In microglial cells, promotes phagocytosis with CCL18 through NF-kappa-B and Src signaling pathways. Stimulation of the CCL1-CCR8 signaling axis protects the gut from acute intestinal damage. (Microbial infection) Acts as a coreceptor for HIV-1 and HIV-2 viruses. (Microbial infection) Acts as a receptor for Kaposi virus protein vCCL1/K6 and thereby inhibits apoptosis in the targeted cells.
Subunit / interactions. Interacts with GNAI1. (Microbial infection) Interacts with Kaposi virus proteins vCCL1 and vCCL2.
Subcellular location. Cell membrane.
Tissue specificity. Expressed in unstimulated CD4(+) and CD8(+) T-cells and polymorphonuclear cells.
Similarity. Belongs to the G-protein coupled receptor 1 family.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P51685-1 | 1 | yes |
| P51685-2 | 2 |
RefSeq proteins (1): NP_005192* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000276 | GPCR_Rhodpsn | Family |
| IPR000355 | Chemokine_rcpt | Family |
| IPR004068 | Chemokine_CCR8 | Family |
| IPR017452 | GPCR_Rhodpsn_7TM | Domain |
| IPR050119 | CCR1-9-like | Family |
Pfam: PF00001
UniProt features (38 total): helix 9, topological domain 8, transmembrane region 7, mutagenesis site 3, strand 3, turn 3, disulfide bond 2, chain 1, splice variant 1, sequence variant 1
Structure
Experimental structures (PDB)
6 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 8XML | ELECTRON MICROSCOPY | 2.58 |
| 8TLM | ELECTRON MICROSCOPY | 2.9 |
| 8KFX | ELECTRON MICROSCOPY | 2.96 |
| 8KFY | ELECTRON MICROSCOPY | 3.06 |
| 8U1U | ELECTRON MICROSCOPY | 3.1 |
| 8KFZ | ELECTRON MICROSCOPY | 3.3 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P51685-F1 | 82.21 | 0.57 |
Antibody-complex structures (SAbDab): 6 — 8KFX, 8KFY, 8KFZ, 8TLM, 8U1U, 8XML
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Disulfide bonds (2): 25–272, 106–183
Mutagenesis-validated functional residues (3):
| Position | Phenotype |
|---|---|
| 113 | strong decrease in ability to mediate calcium mobilization. |
| 172 | strong decrease in ability to mediate calcium mobilization. |
| 286 | strong decrease in ability to mediate calcium mobilization. |
Function
Pathways and Gene Ontology
Reactome pathways
8 pathways
| ID | Pathway |
|---|---|
| R-HSA-380108 | Chemokine receptors bind chemokines |
| R-HSA-418594 | G alpha (i) signalling events |
| R-HSA-162582 | Signal Transduction |
| R-HSA-372790 | Signaling by GPCR |
| R-HSA-373076 | Class A/1 (Rhodopsin-like receptors) |
| R-HSA-375276 | Peptide ligand-binding receptors |
| R-HSA-388396 | GPCR downstream signalling |
| R-HSA-500792 | GPCR ligand binding |
MSigDB gene sets: 122 (showing top):
GOBP_CELL_CHEMOTAXIS, GOBP_RESPONSE_TO_PEPTIDE, MODULE_64, GOCC_CELL_SURFACE, GOBP_TAXIS, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, MODULE_289, chr3p22, GAVIN_FOXP3_TARGETS_CLUSTER_P3, MARSON_BOUND_BY_FOXP3_UNSTIMULATED, GOCC_SIDE_OF_MEMBRANE, BOCHKIS_FOXA2_TARGETS, GOMF_CYTOKINE_BINDING, REACTOME_CLASS_A_1_RHODOPSIN_LIKE_RECEPTORS, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY
GO Biological Process (11): chemotaxis (GO:0006935), immune response (GO:0006955), cell adhesion (GO:0007155), G protein-coupled receptor signaling pathway (GO:0007186), positive regulation of cytosolic calcium ion concentration (GO:0007204), calcium-mediated signaling (GO:0019722), cell chemotaxis (GO:0060326), signal transduction (GO:0007165), cell surface receptor signaling pathway (GO:0007166), chemokine-mediated signaling pathway (GO:0070098), cellular response to cytokine stimulus (GO:0071345)
GO Molecular Function (5): G protein-coupled receptor activity (GO:0004930), chemokine receptor activity (GO:0004950), coreceptor activity (GO:0015026), C-C chemokine receptor activity (GO:0016493), C-C chemokine binding (GO:0019957)
GO Cellular Component (3): plasma membrane (GO:0005886), external side of plasma membrane (GO:0009897), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-6 pathways:
| Category | Pathways |
|---|---|
| Signaling by GPCR | 2 |
| Peptide ligand-binding receptors | 1 |
| GPCR downstream signalling | 1 |
| Signal Transduction | 1 |
| GPCR ligand binding | 1 |
| Class A/1 (Rhodopsin-like receptors) | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular process | 2 |
| signal transduction | 2 |
| G protein-coupled receptor signaling pathway | 2 |
| chemokine binding | 2 |
| response to chemical | 1 |
| taxis | 1 |
| immune system process | 1 |
| response to stimulus | 1 |
| G protein-coupled receptor activity | 1 |
| regulation of biological quality | 1 |
| intracellular signaling cassette | 1 |
| chemotaxis | 1 |
| cell migration | 1 |
| cellular response to chemical stimulus | 1 |
| cell communication | 1 |
| signaling | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| cytokine-mediated signaling pathway | 1 |
| cellular response to chemokine | 1 |
| response to cytokine | 1 |
| transmembrane signaling receptor activity | 1 |
| G protein-coupled chemoattractant receptor activity | 1 |
| cytokine receptor activity | 1 |
| chemokine-mediated signaling pathway | 1 |
| signaling receptor activity | 1 |
| chemokine receptor activity | 1 |
| C-C chemokine binding | 1 |
| membrane | 1 |
| cell periphery | 1 |
| plasma membrane | 1 |
| cell surface | 1 |
| side of membrane | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
1230 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CCR8 | CCL1 | P22362 | 997 |
| CCR8 | CCL17 | Q92583 | 992 |
| CCR8 | CCL18 | P55774 | 992 |
| CCR8 | CCL22 | O00626 | 988 |
| CCR8 | CCL4 | P13236 | 951 |
| CCR8 | CCL8 | P78388 | 939 |
| CCR8 | CCL16 | O15467 | 916 |
| CCR8 | TERT | O14746 | 880 |
| CCR8 | CCL20 | P78556 | 856 |
| CCR8 | CCR2 | P41597 | 828 |
| CCR8 | CCR3 | P51677 | 821 |
| CCR8 | CCL5 | P13501 | 809 |
| CCR8 | CCRL2 | O00421 | 795 |
| CCR8 | CCL19 | Q99731 | 791 |
| CCR8 | CCL2 | P13500 | 783 |
IntAct
22 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CCR8 | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| RAMP1 | CCR8 | psi-mi:“MI:0915”(physical association) | 0.400 |
| CCR8 | RAMP2 | psi-mi:“MI:0915”(physical association) | 0.400 |
| RAMP3 | CCR8 | psi-mi:“MI:0915”(physical association) | 0.400 |
| RAMP2 | CCR8 | psi-mi:“MI:0915”(physical association) | 0.400 |
| CCR8 | RAMP3 | psi-mi:“MI:0915”(physical association) | 0.400 |
| SPP1 | CCR8 | psi-mi:“MI:0915”(physical association) | 0.370 |
| SPNS1 | CCR8 | psi-mi:“MI:0915”(physical association) | 0.370 |
| RTN3 | CCR8 | psi-mi:“MI:0915”(physical association) | 0.370 |
| PAQR6 | CCR8 | psi-mi:“MI:0915”(physical association) | 0.370 |
| NAGPA | CCR8 | psi-mi:“MI:0915”(physical association) | 0.370 |
| THY1 | CCR8 | psi-mi:“MI:0915”(physical association) | 0.370 |
| ATP2A1 | CCR8 | psi-mi:“MI:0915”(physical association) | 0.370 |
| ERGIC3 | CCR8 | psi-mi:“MI:0915”(physical association) | 0.370 |
| GABRD | CCR8 | psi-mi:“MI:0915”(physical association) | 0.370 |
| PLEKHB1 | CCR8 | psi-mi:“MI:0915”(physical association) | 0.370 |
| UCKL1 | CCR8 | psi-mi:“MI:0915”(physical association) | 0.370 |
| EI24 | CCR8 | psi-mi:“MI:0915”(physical association) | 0.370 |
| GABBR1 | CCR8 | psi-mi:“MI:0915”(physical association) | 0.370 |
BioGRID (14): SPP1 (Two-hybrid), SPNS1 (Two-hybrid), RTN3 (Two-hybrid), PAQR6 (Two-hybrid), NAGPA (Two-hybrid), THY1 (Two-hybrid), ATP2A1 (Two-hybrid), ERGIC3 (Two-hybrid), GABRD (Two-hybrid), PLEKHB1 (Two-hybrid), UCKL1 (Two-hybrid), EI24 (Two-hybrid), GABBR1 (Two-hybrid), CCR8 (Affinity Capture-MS)
ESM2 similar proteins: A0A4W3GG95, B0F9W3, B3G515, E7FEL0, F7EQ49, O00398, O08878, O46685, O70526, O97665, P25023, P25105, P30411, P32299, P46093, P47774, P49684, P50132, P51679, P51680, P51685, P51686, P55085, P55086, P56484, P79960, Q15743, Q1JQB3, Q1WLP9, Q28642, Q2HJA4, Q2TAD5, Q4KLH9, Q4VA82, Q63645, Q80Z39, Q8BFQ3, Q8BFU7, Q8BLG2, Q8BMP4
Diamond homologs: A0A287A2K5, C8YUV0, O00155, O02836, O08786, O15973, O18935, O19012, O19014, O19025, O19032, O19054, O19091, O62729, O77408, O77700, O77721, O77830, O97665, O97772, P04761, P08482, P0C5I1, P11229, P12657, P17200, P18089, P19328, P22270, P25021, P30545, P30551, P30552, P30553, P30796, P32211, P32238, P32239, P32302, P46627
SIGNOR signaling
1 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| CCL1 | up-regulates | CCR8 | binding |
Disease & clinical
Clinical variants and AI predictions
ClinVar
51 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 43 |
| Likely benign | 4 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
470 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 3:39329830:G:GG | donor_gain | 1.0000 |
| 3:39329830:GTAT:G | donor_loss | 1.0000 |
| 3:39332316:A:AC | acceptor_loss | 1.0000 |
| 3:39329828:AG:A | donor_gain | 0.9900 |
| 3:39329829:GG:G | donor_gain | 0.9900 |
| 3:39332309:T:TA | acceptor_gain | 0.9900 |
| 3:39332311:T:TA | acceptor_gain | 0.9900 |
| 3:39332316:A:AG | acceptor_gain | 0.9900 |
| 3:39332317:G:GG | acceptor_gain | 0.9900 |
| 3:39332603:A:AG | acceptor_gain | 0.9900 |
| 3:39332604:G:GG | acceptor_gain | 0.9900 |
| 3:39329825:CTAAG:C | donor_gain | 0.9800 |
| 3:39332317:GGT:G | acceptor_gain | 0.9800 |
| 3:39332317:GGTC:G | acceptor_gain | 0.9700 |
| 3:39332604:GACCT:G | acceptor_gain | 0.9700 |
| 3:39329826:TAAG:T | donor_gain | 0.9600 |
| 3:39329827:AAG:A | donor_gain | 0.9600 |
| 3:39330787:G:GG | donor_gain | 0.9500 |
| 3:39332301:T:G | acceptor_gain | 0.9500 |
| 3:39332317:GGTCC:G | acceptor_gain | 0.9500 |
| 3:39332599:TTTCA:T | acceptor_loss | 0.9500 |
| 3:39332600:TTCAG:T | acceptor_loss | 0.9500 |
| 3:39332601:TCAGA:T | acceptor_loss | 0.9500 |
| 3:39332602:CAGA:C | acceptor_loss | 0.9500 |
| 3:39332603:AGAC:A | acceptor_loss | 0.9500 |
| 3:39332604:G:T | acceptor_loss | 0.9500 |
| 3:39332316:AG:A | acceptor_gain | 0.9300 |
| 3:39332317:GG:G | acceptor_gain | 0.9300 |
| 3:39332604:GAC:G | acceptor_gain | 0.9300 |
| 3:39332303:T:TA | acceptor_gain | 0.9100 |
AlphaMissense
2356 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 3:39332713:A:C | S128R | 0.996 |
| 3:39332715:T:A | S128R | 0.996 |
| 3:39332715:T:G | S128R | 0.996 |
| 3:39332628:G:C | W99C | 0.995 |
| 3:39332628:G:T | W99C | 0.995 |
| 3:39332803:T:A | W158R | 0.993 |
| 3:39332803:T:C | W158R | 0.993 |
| 3:39332626:T:A | W99R | 0.992 |
| 3:39332626:T:C | W99R | 0.992 |
| 3:39333250:T:C | F307L | 0.991 |
| 3:39333252:C:A | F307L | 0.991 |
| 3:39333252:C:G | F307L | 0.991 |
| 3:39332647:T:A | C106S | 0.990 |
| 3:39332648:G:C | C106S | 0.990 |
| 3:39332686:A:C | S119R | 0.990 |
| 3:39332688:C:A | S119R | 0.990 |
| 3:39332688:C:G | S119R | 0.990 |
| 3:39332878:T:A | C183S | 0.990 |
| 3:39332879:G:C | C183S | 0.990 |
| 3:39332476:A:C | S49R | 0.988 |
| 3:39332478:T:A | S49R | 0.988 |
| 3:39332478:T:G | S49R | 0.988 |
| 3:39332878:T:C | C183R | 0.985 |
| 3:39333089:C:G | P253R | 0.985 |
| 3:39332647:T:C | C106R | 0.983 |
| 3:39332880:T:G | C183W | 0.983 |
| 3:39332490:C:A | N53K | 0.981 |
| 3:39332490:C:G | N53K | 0.981 |
| 3:39332648:G:A | C106Y | 0.981 |
| 3:39332649:C:G | C106W | 0.981 |
dbSNP variants (sampled 300 via entrez): RS1000796519 (3:39330857 T>A,C), RS1000878714 (3:39332009 C>T), RS1001187760 (3:39330410 G>A,T), RS1002149306 (3:39330236 G>C), RS1002246639 (3:39330531 A>G), RS1002875454 (3:39332464 C>T), RS1003519559 (3:39328910 C>T), RS1004226735 (3:39328679 A>G), RS1004363206 (3:39332671 T>C), RS1004665543 (3:39332310 G>A,C), RS1006034691 (3:39331237 G>T), RS1006338914 (3:39330753 C>A,T), RS1007109339 (3:39328047 G>T), RS1007258564 (3:39331660 G>A), RS1007330680 (3:39331396 C>T)
Disease associations
OMIM: gene MIM:601834 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
2 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST003518_42 | Daytime sleep phenotypes | 8.000000e-06 |
| GCST007932_44 | Medication use (thyroid preparations) | 4.000000e-11 |
EFO canonical traits (2, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0007828 | daytime rest measurement |
| EFO:0009933 | Thyroid preparation use measurement |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL4596 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 748 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL2205807 | ABAMETAPIR | 4 | 748 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: gpcr — Chemokine receptors
Most potent curated ligand interactions (7 total), top 7:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| vMIP-I | Full agonist | 9.9 | pIC50 |
| CCL1 | Full agonist | 9.8 | pIC50 |
| [125I]CCL1 (human) | Full agonist | 9.7 | pKd |
| vMCC-I | Antagonist | 9.41 | pIC50 |
| [125I]CCL1 (mouse) | Full agonist | 8.7 | pKd |
| vMIP-II | Antagonist | 8.1 | pIC50 |
| ZK 756326 | Full agonist | 5.7 | pIC50 |
ChEMBL bioactivities
248 potent at pChembl≥5 of 256 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.77 | Ki | 0.17 | nM | CHEMBL218374 |
| 9.52 | Ki | 0.3 | nM | CHEMBL374939 |
| 9.52 | IC50 | 0.3 | nM | CHEMBL374939 |
| 9.15 | Ki | 0.7 | nM | CHEMBL386308 |
| 9.15 | Ki | 0.7 | nM | CHEMBL221865 |
| 9.00 | IC50 | 1 | nM | CHEMBL205993 |
| 9.00 | Ki | 1 | nM | CHEMBL386308 |
| 9.00 | IC50 | 1 | nM | CHEMBL5424187 |
| 8.96 | Ki | 1.1 | nM | CHEMBL373739 |
| 8.92 | IC50 | 1.2 | nM | CHEMBL5404620 |
| 8.89 | IC50 | 1.3 | nM | CHEMBL5397693 |
| 8.82 | Ki | 1.5 | nM | CHEMBL375854 |
| 8.80 | Ki | 1.6 | nM | CHEMBL218375 |
| 8.80 | Ki | 1.6 | nM | CHEMBL221867 |
| 8.80 | Ki | 1.6 | nM | CHEMBL376910 |
| 8.77 | IC50 | 1.7 | nM | CHEMBL5411391 |
| 8.77 | IC50 | 1.7 | nM | CHEMBL5412884 |
| 8.66 | Ki | 2.2 | nM | CHEMBL220701 |
| 8.64 | Ki | 2.3 | nM | CHEMBL218037 |
| 8.62 | IC50 | 2.399 | nM | CHEMBL567417 |
| 8.60 | Ki | 2.5 | nM | CHEMBL220753 |
| 8.58 | IC50 | 2.63 | nM | CHEMBL568523 |
| 8.58 | IC50 | 2.63 | nM | CHEMBL579072 |
| 8.55 | IC50 | 2.818 | nM | CHEMBL568294 |
| 8.46 | Ki | 3.5 | nM | CHEMBL221130 |
| 8.40 | IC50 | 4 | nM | CHEMBL380492 |
| 8.40 | IC50 | 4 | nM | CHEMBL5399936 |
| 8.40 | IC50 | 4 | nM | CHEMBL221251 |
| 8.39 | Ki | 4.1 | nM | CHEMBL221904 |
| 8.38 | Ki | 4.2 | nM | CHEMBL221251 |
| 8.38 | Ki | 4.2 | nM | CHEMBL385108 |
| 8.38 | IC50 | 4.2 | nM | CHEMBL374527 |
| 8.36 | Ki | 4.4 | nM | CHEMBL218503 |
| 8.31 | IC50 | 4.898 | nM | CHEMBL574655 |
| 8.29 | IC50 | 5.1 | nM | CHEMBL221790 |
| 8.28 | Ki | 5.21 | nM | CHEMBL375315 |
| 8.27 | Ki | 5.4 | nM | CHEMBL218036 |
| 8.25 | IC50 | 5.623 | nM | CHEMBL568522 |
| 8.22 | Ki | 6 | nM | CHEMBL205993 |
| 8.22 | IC50 | 6 | nM | CHEMBL5404280 |
| 8.22 | IC50 | 6 | nM | CHEMBL5412094 |
| 8.21 | IC50 | 6.1 | nM | CHEMBL221586 |
| 8.20 | Ki | 6.3 | nM | CHEMBL218218 |
| 8.18 | IC50 | 6.607 | nM | CHEMBL584087 |
| 8.17 | Ki | 6.7 | nM | CHEMBL221977 |
| 8.16 | IC50 | 6.9 | nM | CHEMBL218297 |
| 8.14 | Ki | 7.2 | nM | CHEMBL374979 |
| 8.12 | IC50 | 7.65 | nM | CHEMBL220652 |
| 8.09 | IC50 | 8.128 | nM | CHEMBL566543 |
| 8.07 | IC50 | 8.44 | nM | CHEMBL5407071 |
PubChem BioAssay actives
248 with measured affinity, of 394 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| ethyl 4-[(4-benzamidonaphthalen-1-yl)sulfonylamino]piperidine-1-carboxylate | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0002 | uM |
| N-[4-[(1-butanoylpiperidin-4-yl)sulfamoyl]naphthalen-1-yl]-2-methylbenzamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0003 | uM |
| 2-methyl-N-[4-[[1-[(2S)-pyrrolidine-2-carbonyl]piperidin-4-yl]sulfamoyl]naphthalen-1-yl]benzamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0007 | uM |
| N-methyl-4-[[4-[(2-methylbenzoyl)amino]naphthalen-1-yl]sulfonylamino]piperidine-1-carboxamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0007 | uM |
| 2-[3-[[1-[[3-(2-chlorophenoxy)phenyl]methyl]piperidin-4-yl]carbamoyl]-3-phenylpyrrolidin-1-yl]-2-methylpropanoic acid | 264168: Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8 | ic50 | 0.0010 | uM |
| N-[2-chloro-6-methyl-4-[[(1R)-1-(1-methylpiperidin-4-yl)ethyl]sulfamoyl]phenyl]-2-methylbenzamide | 2029995: Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay | ic50 | 0.0010 | uM |
| 2-methyl-N-[4-[[1-(pyrrolidine-1-carbonyl)piperidin-4-yl]sulfamoyl]naphthalen-1-yl]benzamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0011 | uM |
| 2-methyl-N-[4-[[(1R)-1-(1-methylpiperidin-4-yl)ethyl]sulfamoyl]naphthalen-1-yl]benzamide | 2029995: Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay | ic50 | 0.0012 | uM |
| 3-chloro-2-methyl-N-[2-methyl-4-[[(1R)-1-(1-methylpiperidin-4-yl)ethyl]sulfamoyl]phenyl]benzamide | 2029995: Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay | ic50 | 0.0013 | uM |
| N-[4-[[1-(azetidine-3-carbonyl)piperidin-4-yl]sulfamoyl]naphthalen-1-yl]-2-methylbenzamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0015 | uM |
| ethyl 4-[[4-[(2-methylbenzoyl)amino]naphthalen-1-yl]sulfonylamino]piperidine-1-carboxylate | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0016 | uM |
| N,N-dimethyl-4-[[4-[(2-methylbenzoyl)amino]naphthalen-1-yl]sulfonylamino]piperidine-1-carboxamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0016 | uM |
| N-[4-[[1-(4-aminobutanoyl)piperidin-4-yl]sulfamoyl]naphthalen-1-yl]-2-methylbenzamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0016 | uM |
| 4-chloro-2-methyl-N-[2-methyl-4-[[(1R)-1-(1-methylpiperidin-4-yl)ethyl]sulfamoyl]phenyl]benzamide | 2029995: Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay | ic50 | 0.0017 | uM |
| 5-chloro-2-methyl-N-[2-methyl-4-[[(1R)-1-(1-methylpiperidin-4-yl)ethyl]sulfamoyl]phenyl]benzamide | 2029995: Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay | ic50 | 0.0017 | uM |
| N-ethyl-4-[[4-[(2-methylbenzoyl)amino]naphthalen-1-yl]sulfonylamino]piperidine-1-carboxamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0022 | uM |
| ethyl 4-[(5-benzamidonaphthalen-1-yl)sulfonylamino]piperidine-1-carboxylate | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0023 | uM |
| (5-amino-2-pyridinyl)-[9-[(2-ethyl-2-propyl-3H-1-benzofuran-4-yl)methyl]-3,9-diazaspiro[5.5]undecan-3-yl]methanone | 442859: Antagonist activity at human CCR8 | ic50 | 0.0024 | uM |
| 2-methyl-N-[4-[(1-propanoylpiperidin-4-yl)sulfamoyl]naphthalen-1-yl]benzamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0025 | uM |
| (5-amino-2-pyridinyl)-[9-[(2,2-dimethyl-3H-1-benzofuran-7-yl)methyl]-3,9-diazaspiro[5.5]undecan-3-yl]methanone | 442859: Antagonist activity at human CCR8 | ic50 | 0.0026 | uM |
| (5-amino-2-pyridinyl)-[9-[(3,3-difluoro-2,2-dimethyl-1-benzofuran-7-yl)methyl]-3,9-diazaspiro[5.5]undecan-3-yl]methanone | 442859: Antagonist activity at human CCR8 | ic50 | 0.0026 | uM |
| (5-amino-2-pyridinyl)-[9-[(2-tert-butyl-2-methyl-3H-1-benzofuran-4-yl)methyl]-3,9-diazaspiro[5.5]undecan-3-yl]methanone | 442859: Antagonist activity at human CCR8 | ic50 | 0.0028 | uM |
| N-[4-[[1-(azetidine-1-carbonyl)piperidin-4-yl]sulfamoyl]naphthalen-1-yl]-2-methylbenzamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0035 | uM |
| 2-[4-[[1-[[3-(2-chlorophenoxy)phenyl]methyl]piperidin-4-yl]carbamoyl]-4-phenylpiperidin-1-yl]-2-methylpropanoic acid | 264168: Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8 | ic50 | 0.0040 | uM |
| 2-methyl-N-[4-[[1-(4-methylpiperazine-1-carbonyl)piperidin-4-yl]sulfamoyl]naphthalen-1-yl]benzamide | 2029995: Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay | ic50 | 0.0040 | uM |
| N-[2,5-dimethyl-4-[[(1R)-1-(1-methylpiperidin-4-yl)ethyl]sulfamoyl]phenyl]-2-methylbenzamide | 2029995: Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay | ic50 | 0.0040 | uM |
| N-[4-[[1-(2-aminoacetyl)piperidin-4-yl]sulfamoyl]naphthalen-1-yl]-2-methylbenzamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0041 | uM |
| 3-pyrrolidin-1-ylpropyl 4-[[4-[(2-methylbenzoyl)amino]naphthalen-1-yl]sulfonylamino]piperidine-1-carboxylate | 277748: Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay | ic50 | 0.0042 | uM |
| 2-methyl-N-[4-[[1-(piperidine-1-carbonyl)piperidin-4-yl]sulfamoyl]naphthalen-1-yl]benzamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0042 | uM |
| N-[4-(cyclohexylsulfamoyl)naphthalen-1-yl]benzamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0044 | uM |
| [9-[[3-(2-methoxyphenoxy)phenyl]methyl]-3,9-diazaspiro[5.5]undecan-3-yl]-pyrimidin-4-ylmethanone | 442859: Antagonist activity at human CCR8 | ic50 | 0.0049 | uM |
| N-[4-[(1-butanoylpiperidin-4-yl)sulfamoyl]naphthalen-1-yl]-3-methylbenzamide | 277748: Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay | ic50 | 0.0051 | uM |
| ethyl 4-[[4-[(2-methylphenyl)carbamoyl]naphthalen-1-yl]sulfonylamino]piperidine-1-carboxylate | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0052 | uM |
| N-[4-[[1-(2-hydroxyacetyl)piperidin-4-yl]sulfamoyl]naphthalen-1-yl]-2-methylbenzamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0054 | uM |
| (2-amino-4-pyridinyl)-[9-[(2,2-dimethylchromen-8-yl)methyl]-3,9-diazaspiro[5.5]undecan-3-yl]methanone | 442859: Antagonist activity at human CCR8 | ic50 | 0.0056 | uM |
| N-[5-chloro-2-methyl-4-[[(1R)-1-(1-methylpiperidin-4-yl)ethyl]sulfamoyl]phenyl]-2-methylbenzamide | 2029995: Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay | ic50 | 0.0060 | uM |
| N-[5-fluoro-2-methyl-4-[[(1R)-1-(1-methylpiperidin-4-yl)ethyl]sulfamoyl]phenyl]-2-methylbenzamide | 2029995: Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay | ic50 | 0.0060 | uM |
| N-[4-[(1-butanoylpiperidin-4-yl)sulfamoyl]naphthalen-1-yl]cyclohexanecarboxamide | 277748: Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay | ic50 | 0.0061 | uM |
| 2-methyl-N-[4-[[1-(morpholine-4-carbonyl)piperidin-4-yl]sulfamoyl]naphthalen-1-yl]benzamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0063 | uM |
| (2-amino-4-pyridinyl)-[9-[(2,2-dimethyl-1,3-benzodioxol-4-yl)methyl]-3,9-diazaspiro[5.5]undecan-3-yl]methanone | 442859: Antagonist activity at human CCR8 | ic50 | 0.0066 | uM |
| N-[4-[(1-acetylpiperidin-4-yl)sulfamoyl]naphthalen-1-yl]-2-methylbenzamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0067 | uM |
| N-[4-[(1-butanoylpiperidin-4-yl)sulfamoyl]naphthalen-1-yl]-4-tert-butylbenzamide | 277748: Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay | ic50 | 0.0069 | uM |
| N-[4-[[1-(cyclopropanecarbonyl)piperidin-4-yl]sulfamoyl]naphthalen-1-yl]-2-methylbenzamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0072 | uM |
| N-[4-[(1-butanoylpiperidin-4-yl)sulfamoyl]naphthalen-1-yl]-2-phenylbutanamide | 277748: Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay | ic50 | 0.0076 | uM |
| (5-amino-2-pyridinyl)-[9-[(2,2-dimethyl-3H-1-benzofuran-4-yl)methyl]-3,9-diazaspiro[5.5]undecan-3-yl]methanone | 442859: Antagonist activity at human CCR8 | ic50 | 0.0081 | uM |
| 2-methyl-N-[2-methyl-4-[[(1R)-1-(1-methylpiperidin-4-yl)ethyl]sulfamoyl]phenyl]benzamide | 2030002: Inhibition of CCR8 (unknown origin)-mediated beta-arrestin downstream signalling in CCL1-induced CHO cells assessed as beta-lactamase level by Tango assay | ic50 | 0.0084 | uM |
| N-[4-[[1-(cyclopentanecarbonyl)piperidin-4-yl]sulfamoyl]naphthalen-1-yl]-2-methylbenzamide | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0091 | uM |
| ethyl 4-[[4-(cyclohexylcarbamoyl)naphthalen-1-yl]sulfonylamino]piperidine-1-carboxylate | 277746: Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay | ki | 0.0095 | uM |
| N-[4-[(1-butanoylpiperidin-4-yl)sulfamoyl]naphthalen-1-yl]-4-methylbenzamide | 277748: Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay | ic50 | 0.0095 | uM |
| 3-(dimethylamino)propyl 4-[[4-[(2-methylbenzoyl)amino]naphthalen-1-yl]sulfonylamino]piperidine-1-carboxylate | 277748: Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay | ic50 | 0.0098 | uM |
CTD chemical–gene interactions
23 total (human), top 23 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| nickel sulfate | affects expression, increases expression | 2 |
| fluorene-9-bisphenol | increases expression | 1 |
| terbufos | increases methylation | 1 |
| hydroxyhydroquinone | decreases expression | 1 |
| zinc chloride | decreases expression | 1 |
| ferrous sulfate | decreases expression | 1 |
| benzo(e)pyrene | increases methylation | 1 |
| aflatoxin B2 | increases methylation | 1 |
| 1-nitropyrene | decreases expression | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| Arsenic Trioxide | decreases expression | 1 |
| Arsenic | affects expression | 1 |
| Benzo(a)pyrene | increases methylation | 1 |
| Calcium | affects abundance | 1 |
| Cyclophosphamide | decreases expression | 1 |
| Fonofos | increases methylation | 1 |
| Methapyrilene | increases methylation | 1 |
| Parathion | increases methylation | 1 |
| Silicon Dioxide | decreases expression | 1 |
| Cyclosporine | increases methylation | 1 |
| Aflatoxin B1 | decreases methylation | 1 |
| Antirheumatic Agents | decreases expression | 1 |
| Soot | decreases expression | 1 |
ChEMBL screening assays
41 unique, capped per target: 23 binding, 18 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1045844 | Functional | Antagonist activity at human CCR8 | Increasing selectivity of CC chemokine receptor 8 antagonists by engineering nondesolvation related interactions with the intended and off-target binding sites. — J Med Chem |
| CHEMBL2039639 | Binding | Inhibition of human CCR8 by FLIPR analysis | The design and synthesis of novel, potent and orally bioavailable N-aryl piperazine-1-carboxamide CCR2 antagonists with very high hERG selectivity. — Bioorg Med Chem Lett |
Cellosaurus cell lines
10 cell lines: 5 cancer cell line, 3 spontaneously immortalized cell line, 2 transformed cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_1R22 | NP-2/CCR8 | Cancer cell line | Male |
| CVCL_1R28 | NP-2/CD4/CCR8 | Cancer cell line | Male |
| CVCL_C8V8 | 4DE4-CCR8 | Cancer cell line | |
| CVCL_E6A2 | CHO-CCR8 | Spontaneously immortalized cell line | Female |
| CVCL_E6AC | HEK293-CCR8 | Transformed cell line | Female |
| CVCL_E6P6 | Genomeditech CHO-K1 H_CCR8 | Spontaneously immortalized cell line | Female |
| CVCL_E6TD | Genomeditech HEK-293 H_CCR8 | Transformed cell line | Female |
| CVCL_E6VP | Genomeditech Jurkat H_CCR8 | Cancer cell line | Male |
| CVCL_KW62 | PathHunter CHO-K1 CCR8 beta-arrestin | Spontaneously immortalized cell line | Female |
| CVCL_S494 | GHOST(3).CCR8 | Cancer cell line | Female |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.