CCR10
gene geneOn this page
Summary
CCR10 (C-C motif chemokine receptor 10, HGNC:4474) is a protein-coding gene on chromosome 17q21.2, encoding C-C chemokine receptor type 10 (P46092). Receptor for chemokines SCYA27 and SCYA28.
Chemokines are a group of small (approximately 8 to 14 kD), mostly basic, structurally related molecules that regulate cell trafficking of various types of leukocytes through interactions with a subset of 7-transmembrane, G protein-coupled receptors. Chemokines also play fundamental roles in the development, homeostasis, and function of the immune system, and they have effects on cells of the central nervous system as well as on endothelial cells involved in angiogenesis or angiostasis. Chemokines are divided into 2 major subfamilies, CXC and CC, based on the arrangement of the first 2 of the 4 conserved cysteine residues; the 2 cysteines are separated by a single amino acid in CXC chemokines and are adjacent in CC chemokines. CCR10 is the receptor for CCL27 (SCYA27; MIM 604833); CCR10-CCL27 interactions are involved in T cell-mediated skin inflammation (Homey et al., 2002 [PubMed 11821900]).
Source: NCBI Gene 2826 — RefSeq curated summary.
At a glance
- Clinical variants (ClinVar): 44 total
- Druggable target: yes
- MANE Select transcript:
NM_016602
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:4474 |
| Approved symbol | CCR10 |
| Name | C-C motif chemokine receptor 10 |
| Location | 17q21.2 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000184451 |
| Ensembl biotype | protein_coding |
| OMIM | 600240 |
| Entrez | 2826 |
Gene structure
Transcript identifiers
Ensembl transcripts: 3 — 3 protein_coding
ENST00000332438, ENST00000591568, ENST00000591765
RefSeq mRNA: 1 — MANE Select: NM_016602
NM_016602
CCDS: CCDS11435
Canonical transcript exons
ENST00000332438 — 2 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001324962 | 42678889 | 42680617 |
| ENSE00001407622 | 42681800 | 42681843 |
Expression profiles
Bgee: expression breadth ubiquitous, 173 present calls, max score 87.17.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.4142 / max 42.5205, expressed in 182 samples.
FANTOM5 promoters (3 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 166181 | 0.2133 | 88 |
| 166182 | 0.1152 | 55 |
| 166183 | 0.0856 | 31 |
Top tissues by expression
280 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| sural nerve | UBERON:0015488 | 87.17 | gold quality |
| pituitary gland | UBERON:0000007 | 82.78 | gold quality |
| adenohypophysis | UBERON:0002196 | 82.14 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 77.91 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 77.29 | gold quality |
| cerebellar cortex | UBERON:0002129 | 77.22 | gold quality |
| body of uterus | UBERON:0009853 | 76.29 | gold quality |
| cerebellum | UBERON:0002037 | 75.97 | gold quality |
| left uterine tube | UBERON:0001303 | 75.32 | gold quality |
| apex of heart | UBERON:0002098 | 74.63 | gold quality |
| endocervix | UBERON:0000458 | 73.63 | gold quality |
| left ovary | UBERON:0002119 | 72.92 | gold quality |
| right ovary | UBERON:0002118 | 72.90 | gold quality |
| tibial nerve | UBERON:0001323 | 72.80 | gold quality |
| gastrocnemius | UBERON:0001388 | 72.77 | gold quality |
| primary visual cortex | UBERON:0002436 | 72.34 | gold quality |
| right atrium auricular region | UBERON:0006631 | 72.26 | gold quality |
| right coronary artery | UBERON:0001625 | 72.07 | gold quality |
| lower esophagus muscularis layer | UBERON:0035833 | 72.07 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 72.06 | gold quality |
| esophagogastric junction muscularis propria | UBERON:0035841 | 72.06 | gold quality |
| lower esophagus | UBERON:0013473 | 71.98 | gold quality |
| right frontal lobe | UBERON:0002810 | 71.52 | gold quality |
| muscle of leg | UBERON:0001383 | 71.42 | gold quality |
| left coronary artery | UBERON:0001626 | 71.19 | gold quality |
| mucosa of stomach | UBERON:0001199 | 71.06 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 70.91 | gold quality |
| cardiac atrium | UBERON:0002081 | 70.76 | gold quality |
| tibial artery | UBERON:0007610 | 70.69 | gold quality |
| popliteal artery | UBERON:0002250 | 70.68 | gold quality |
Single-cell (SCXA)
Detected in 4 experiment(s), a significant marker in 4.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-CURD-88 | yes | 106.80 |
| E-MTAB-8410 | yes | 35.37 |
| E-HCAD-11 | yes | 25.71 |
| E-ANND-3 | yes | 6.68 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
10 targeting CCR10, 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-5193 | 100.00 | 67.26 | 1744 |
| HSA-MIR-124-3P | 99.89 | 73.74 | 3043 |
| HSA-MIR-506-3P | 99.89 | 73.55 | 3057 |
| HSA-MIR-12130 | 99.75 | 65.47 | 452 |
| HSA-MIR-3940-5P | 99.14 | 65.26 | 493 |
| HSA-MIR-4507 | 99.14 | 65.27 | 515 |
| HSA-MIR-6809-5P | 99.13 | 68.45 | 1223 |
| HSA-MIR-4716-5P | 98.82 | 68.57 | 1168 |
| HSA-MIR-6781-3P | 97.44 | 66.85 | 970 |
| HSA-MIR-2114-5P | 96.00 | 64.56 | 617 |
Literature-anchored findings (GeneRIF, showing 24)
- CCR10 and its ligand CCL27 may contribute to the skin infiltration of malignant T-cells in cutaneous T-cell lymphoma. (PMID:15700309)
- gene expression of CCR10 was increased by recombinant ANXA1 and the N-terminal ANXA1 peptide (PMID:16460738)
- CCR10-CTACK/CCL27 interactions between circulating T cells and keratinocytes would seem to play an important role in the pathophysiology of mycosis fungoides. (PMID:16675558)
- CCR10 allows T regulatory (Treg) cells recruited to chronically inflamed liver tissues to respond to CCL28 secreted by epithelial cells, resulting in the accumulation of CCR10+ Tregs at mucosal surfaces. (PMID:16785557)
- CCR4 and CCR10 may play an important role in ATLL invasion into the skin (PMID:17071491)
- CCR4 and CCR10 are expressed on epidermal keratinocytes and that both are functional in terms of skin cytokine production and/or migration to their ligand CCL17 and CCL27, respectively. (PMID:18782672)
- TLR2 ligands induce CCR9 and CCR10 expression by circulating B-cells and increase their chemotaxis. TLR2 stimulation also induced J chain and IgA production demonstrating the induction of mucosal-like antibody secreting cells. (PMID:20947433)
- The high fraction of circulating IgA+ and IgG+ B cells expressing CCR9 and CCR10 in the first months of life indicates activation of naive B cells in the gut, coinciding with bacterial colonization. (PMID:21075690)
- unlike blood plasmacytoid dendritic cells (pDCs), a subset of tonsil pDCs express functional CCR6 and CCR10, and their respective ligands CCL20 and CCL27 are detected in inflamed epithelia (PMID:21937703)
- CCR7 overexpression correlated with expression of metallothionein, while CCR10 was associated with cerebral metastases. CCR7 and CCR10 overexpressions were associated with a worse outcome independent of Breslow’s tumor thickness and Clark level. (PMID:22350183)
- low CCL27/CCR10 and CXCL12/CXCR4 intratumoral mRNA ratios are associated with melanoma progression (PMID:22526457)
- Findings support the notion that CCR10 and its ligand CCL27 may contribute to the skin infiltration of malignant T-cells in mycosis fungoides and adult T-cell leukemia/lymphoma. (PMID:24970722)
- The chemokine receptor CCR10 is highly expressed in human glioblastoma compared with control brain tissue. (PMID:25149529)
- CCR10/CCL27 crosstalk mediated drug resistance, contributing to failure of proteasome-inhibitors in multiple myeloma. (PMID:27732933)
- CCL27 drives baseline recruitment of Herpes simplex virus-specific CD8 T cells expressing CCR10, while interferon-responsive CXCR3 ligands recruit additional cells in response to virus-driven inflammation. (PMID:28701399)
- CCR10 may be a key regulator in breast cancer cell invasion and migration (PMID:28830025)
- Inflammation-induced TNF promotes hepatocellular CCR10 expression and downstream PI3K/Akt-mediated hepatocarcinogenesis. (PMID:29445190)
- The characterization of CCR10(+) ILC2s in human samples and in mouse asthma models suggests that these cells downregulate allergic inflammation through IFN-gamma production. (PMID:30475388)
- Coordinated co-migration of CCR10(+) antibody-producing B cells with helper T cells for colonic homeostatic regulation. (PMID:32773769)
- SARS-CoV2 pneumonia recovery is linked to expansion of innate lymphoid cells type 2 expressing CCR10. (PMID:34564853)
- Inhibition of CCL28/CCR10-Mediated eNOS Downregulation Improves Skin Wound Healing in the Obesity-Induced Mouse Model of Type 2 Diabetes. (PMID:35899992)
- The CCL27-CCR10 axis contributes to promoting proliferation, migration, and invasion of lung squamous cell carcinoma. (PMID:36169116)
- Mucosal CCL28 Chemokine Improves Protection against Genital Herpes through Mobilization of Antiviral Effector Memory CCR10+CD44+ CD62L-CD8+ T Cells and Memory CCR10+B220+CD27+ B Cells into the Infected Vaginal Mucosa. (PMID:37222480)
- Inhibition of cc chemokine receptor 10 ameliorates osteoarthritis via inhibition of the phosphoinositide-3-kinase/Akt/mammalian target of rapamycin pathway. (PMID:38429844)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | ccr10 | ENSDARG00000040643 |
| mus_musculus | Ccr10 | ENSMUSG00000044052 |
| rattus_norvegicus | Ccr10 | ENSRNOG00000020275 |
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), CCR8 (ENSG00000179934), CXCR2 (ENSG00000180871), GALR2 (ENSG00000182687), CCR3 (ENSG00000183625), CCR4 (ENSG00000183813), CXCR3 (ENSG00000186810)
Protein
Protein identifiers
C-C chemokine receptor type 10 — P46092 (reviewed: P46092)
Alternative names: G-protein coupled receptor 2
All UniProt accessions (3): P46092, K7EPC9, K7ER70
UniProt curated annotations — full annotation on UniProt →
Function. Receptor for chemokines SCYA27 and SCYA28. Subsequently transduces a signal by increasing the intracellular calcium ions level and stimulates chemotaxis in a pre-B cell line.
Subcellular location. Cell membrane.
Tissue specificity. Expressed at high levels in adult testis, small intestine, fetal lung, fetal kidney. Weaker expression was observed in many other adult tissues including spleen, thymus, lymph node, Peyer patches, colon, heart, ovary, peripheral blood lymphocytes, thyroid and spinal cord. Also expressed by melanocytes, dermal fibroblasts, dermal microvascular endothelial cells. Also detected in T-cells and in skin-derived Langerhans cells.
Similarity. Belongs to the G-protein coupled receptor 1 family.
RefSeq proteins (1): NP_057686* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000276 | GPCR_Rhodpsn | Family |
| IPR000355 | Chemokine_rcpt | Family |
| IPR005382 | Chemokine_CCR10 | Family |
| IPR017452 | GPCR_Rhodpsn_7TM | Domain |
| IPR050119 | CCR1-9-like | Family |
Pfam: PF00001
UniProt features (23 total): topological domain 8, transmembrane region 7, sequence conflict 3, compositionally biased region 2, chain 1, region of interest 1, disulfide bond 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P46092-F1 | 76.61 | 0.29 |
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 (1): 113–191
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: 115 (showing top):
AHRARNT_01, GOBP_CELL_CHEMOTAXIS, GOBP_RESPONSE_TO_PEPTIDE, GOCC_CELL_SURFACE, GAURNIER_PSMD4_TARGETS, GOBP_TAXIS, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, CCANNAGRKGGC_UNKNOWN, SHETH_LIVER_CANCER_VS_TXNIP_LOSS_PAM5, BLALOCK_ALZHEIMERS_DISEASE_UP, GGGNNTTTCC_NFKB_Q6_01, HAHTOLA_SEZARY_SYNDROM_UP, MAF_Q6, SPIELMAN_LYMPHOBLAST_EUROPEAN_VS_ASIAN_UP, NERF_Q2
GO Biological Process (8): immune response (GO:0006955), 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), chemotaxis (GO:0006935), signal transduction (GO:0007165), chemokine-mediated signaling pathway (GO:0070098)
GO Molecular Function (5): G protein-coupled receptor activity (GO:0004930), C-C chemokine receptor activity (GO:0016493), C-C chemokine binding (GO:0019957), chemokine receptor activity (GO:0004950), protein binding (GO:0005515)
GO Cellular Component (5): endoplasmic reticulum (GO:0005783), plasma membrane (GO:0005886), external side of plasma membrane (GO:0009897), cell surface (GO:0009986), 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 |
|---|---|
| G protein-coupled receptor signaling pathway | 2 |
| chemokine binding | 2 |
| cellular anatomical structure | 2 |
| immune system process | 1 |
| response to stimulus | 1 |
| G protein-coupled receptor activity | 1 |
| signal transduction | 1 |
| regulation of biological quality | 1 |
| intracellular signaling cassette | 1 |
| chemotaxis | 1 |
| cell migration | 1 |
| cellular response to chemical stimulus | 1 |
| response to chemical | 1 |
| taxis | 1 |
| cell communication | 1 |
| cellular process | 1 |
| signaling | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| cytokine-mediated signaling pathway | 1 |
| cellular response to chemokine | 1 |
| transmembrane signaling receptor activity | 1 |
| chemokine receptor activity | 1 |
| C-C chemokine binding | 1 |
| G protein-coupled chemoattractant receptor activity | 1 |
| cytokine receptor activity | 1 |
| chemokine-mediated signaling pathway | 1 |
| binding | 1 |
| cytoplasm | 1 |
| endomembrane system | 1 |
| intracellular membrane-bounded organelle | 1 |
| membrane | 1 |
| cell periphery | 1 |
| plasma membrane | 1 |
| cell surface | 1 |
| side of membrane | 1 |
Protein interactions and networks
STRING
906 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CCR10 | CCL27 | Q9Y4X3 | 999 |
| CCR10 | CCL17 | Q92583 | 978 |
| CCR10 | CCL22 | O00626 | 904 |
| CCR10 | CCL21 | O00585 | 903 |
| CCR10 | CCL28 | Q9NRJ3 | 882 |
| CCR10 | CXCL12 | P48061 | 783 |
| CCR10 | CCR1 | P32246 | 765 |
| CCR10 | CCL20 | P78556 | 761 |
| CCR10 | MADCAM1 | Q13477 | 756 |
| CCR10 | CCL1 | P22362 | 735 |
| CCR10 | CCL5 | P13501 | 735 |
| CCR10 | CCL2 | P13500 | 715 |
| CCR10 | CD4 | P01730 | 711 |
| CCR10 | CCR7 | P32248 | 694 |
| CCR10 | CCR2 | P41597 | 686 |
IntAct
17 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CCR10 | S100A10 | psi-mi:“MI:2364”(proximity) | 0.630 |
| CCR10 | S100A10 | psi-mi:“MI:0407”(direct interaction) | 0.630 |
| ARPC3 | CCR10 | psi-mi:“MI:0915”(physical association) | 0.560 |
| CCR10 | ANXA2 | psi-mi:“MI:2364”(proximity) | 0.420 |
| CCR10 | ANXA2 | psi-mi:“MI:0914”(association) | 0.420 |
| FYN | CCR10 | psi-mi:“MI:0915”(physical association) | 0.400 |
| GRB2 | CCR10 | psi-mi:“MI:0915”(physical association) | 0.400 |
| NCK1 | CCR10 | psi-mi:“MI:0915”(physical association) | 0.400 |
| CCR10 | ACTB | psi-mi:“MI:0403”(colocalization) | 0.380 |
| CCR10 | ACTB | psi-mi:“MI:2364”(proximity) | 0.380 |
| CCR10 | S100A10 | psi-mi:“MI:0914”(association) | 0.350 |
| ARPC3 | CCR10 | psi-mi:“MI:0915”(physical association) | 0.000 |
| PRRC2A | CCR10 | psi-mi:“MI:0915”(physical association) | 0.000 |
BioGRID (3): CCR10 (Two-hybrid), CCR10 (Affinity Capture-RNA), CCR10 (Two-hybrid)
ESM2 similar proteins: A0A6I8PUB9, O00155, O00270, O14842, O14843, O15529, O43603, O46685, O60755, O88626, O88634, O88853, O88854, O88855, P0C5I1, P46092, P46093, P50132, Q149R9, Q15722, Q15743, Q1JQB3, Q3T181, Q3UFD7, Q3ZC80, Q4KLH9, Q6XKD3, Q76JU8, Q76JU9, Q76JV1, Q86VZ1, Q8BUD0, Q8BYC4, Q8HYC3, Q8K3T4, Q8TDS5, Q8TDU9, Q920E0, Q924U0, Q96G91
Diamond homologs: A0A4W3GG95, A0A6I8PUB9, B2GV46, B5X337, D4A7K7, E7FEL0, E9QJ73, F8VQN3, O00270, O08726, O08858, O14842, O14843, O15529, O42179, O43603, O46685, O60755, O77408, O88410, O88626, O88634, O88853, P21109, P23944, P25024, P25025, P35344, P35383, P35414, P41231, P41232, P46092, P46093, P49652, P49682, P49683, P50132, P51675, P51679
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
44 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 40 |
| Likely benign | 2 |
| Benign | 2 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
0 predictions. Top by Δscore:
AlphaMissense
2241 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 17:42680237:G:C | S135R | 0.997 |
| 17:42680237:G:T | S135R | 0.997 |
| 17:42680239:T:G | S135R | 0.997 |
| 17:42679874:G:C | F256L | 0.993 |
| 17:42679874:G:T | F256L | 0.993 |
| 17:42679876:A:G | F256L | 0.993 |
| 17:42680550:C:G | C31S | 0.992 |
| 17:42680551:A:T | C31S | 0.992 |
| 17:42680058:A:C | F195C | 0.991 |
| 17:42679857:G:T | P262H | 0.989 |
| 17:42680465:A:C | N59K | 0.989 |
| 17:42680465:A:T | N59K | 0.989 |
| 17:42679994:G:C | F216L | 0.988 |
| 17:42679994:G:T | F216L | 0.988 |
| 17:42679996:A:G | F216L | 0.988 |
| 17:42680379:T:A | D88V | 0.988 |
| 17:42679692:A:C | F317C | 0.987 |
| 17:42680543:C:A | K33N | 0.987 |
| 17:42680543:C:G | K33N | 0.987 |
| 17:42680550:C:T | C31Y | 0.987 |
| 17:42679691:G:C | F317L | 0.986 |
| 17:42679691:G:T | F317L | 0.986 |
| 17:42679693:A:G | F317L | 0.986 |
| 17:42680146:A:G | W166R | 0.986 |
| 17:42680146:A:T | W166R | 0.986 |
| 17:42679724:A:C | N306K | 0.985 |
| 17:42679724:A:T | N306K | 0.985 |
| 17:42679850:G:C | S264R | 0.985 |
| 17:42679850:G:T | S264R | 0.985 |
| 17:42679852:T:G | S264R | 0.985 |
dbSNP variants (sampled 300 via entrez): RS1000284310 (17:42678731 C>A,T), RS1001097202 (17:42680678 G>A), RS1001277959 (17:42680357 C>G), RS1002087060 (17:42679337 G>T), RS1002695110 (17:42681018 T>A), RS1003292726 (17:42682605 T>C,G), RS1004998048 (17:42683254 A>T), RS1005121408 (17:42682955 C>A,G,T), RS1006745061 (17:42680735 G>A,C), RS1007139911 (17:42679695 C>A,G,T), RS1008094184 (17:42681123 C>A,G), RS1008679870 (17:42682629 G>A,C), RS1009087759 (17:42682225 A>C), RS1009752891 (17:42681751 T>A), RS1010539667 (17:42682622 A>G)
Disease associations
OMIM: gene MIM:600240 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
0 associations (top):
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL2321628 (SINGLE PROTEIN)
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 (1 total), top 1:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| BI-6901 | Antagonist | 9.0 | pIC50 |
ChEMBL bioactivities
68 potent at pChembl≥5 of 69 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.40 | IC50 | 0.3981 | nM | CHEMBL3889627 |
| 9.00 | IC50 | 1 | nM | CHEMBL3889627 |
| 8.90 | IC50 | 1.259 | nM | CHEMBL3889627 |
| 8.70 | IC50 | 1.995 | nM | CHEMBL3889627 |
| 8.70 | IC50 | 1.995 | nM | CHEMBL3951018 |
| 8.50 | IC50 | 3.162 | nM | CHEMBL3951018 |
| 8.47 | IC50 | 3.4 | nM | CHEMBL3951018 |
| 8.10 | IC50 | 7.943 | nM | CHEMBL3923733 |
| 8.10 | IC50 | 7.943 | nM | CHEMBL3904154 |
| 8.00 | IC50 | 10 | nM | CHEMBL3971826 |
| 8.00 | IC50 | 10 | nM | CHEMBL3891692 |
| 8.00 | IC50 | 10 | nM | CHEMBL3889627 |
| 7.90 | IC50 | 12.59 | nM | CHEMBL3971886 |
| 7.90 | IC50 | 12.59 | nM | CHEMBL3951018 |
| 7.80 | IC50 | 15.85 | nM | CHEMBL3951018 |
| 7.80 | IC50 | 15.85 | nM | CHEMBL3923733 |
| 7.70 | IC50 | 19.95 | nM | CHEMBL3951018 |
| 7.70 | IC50 | 19.95 | nM | CHEMBL3918664 |
| 7.60 | IC50 | 25.12 | nM | CHEMBL3909737 |
| 7.60 | IC50 | 25.12 | nM | CHEMBL3889627 |
| 7.40 | IC50 | 39.81 | nM | CHEMBL3959737 |
| 7.30 | IC50 | 50.12 | nM | CHEMBL3975141 |
| 7.30 | IC50 | 50.12 | nM | CHEMBL3908230 |
| 7.28 | IC50 | 53 | nM | CHEMBL3908230 |
| 7.20 | IC50 | 63.1 | nM | CHEMBL3919363 |
| 7.20 | IC50 | 63.1 | nM | CHEMBL3960764 |
| 7.20 | IC50 | 63.1 | nM | CHEMBL3890608 |
| 7.10 | IC50 | 79.43 | nM | CHEMBL3933303 |
| 7.00 | IC50 | 100 | nM | CHEMBL3933303 |
| 6.90 | IC50 | 125.9 | nM | CHEMBL3891289 |
| 6.90 | IC50 | 125.9 | nM | CHEMBL3945769 |
| 6.90 | IC50 | 125.9 | nM | CHEMBL3960700 |
| 6.80 | IC50 | 158.5 | nM | CHEMBL3969321 |
| 6.80 | IC50 | 158.5 | nM | CHEMBL3951018 |
| 6.70 | IC50 | 199.5 | nM | CHEMBL3971886 |
| 6.60 | IC50 | 251.2 | nM | CHEMBL3979967 |
| 6.60 | IC50 | 251.2 | nM | CHEMBL3942284 |
| 6.60 | IC50 | 251.2 | nM | CHEMBL3901006 |
| 6.60 | IC50 | 251.2 | nM | CHEMBL3964547 |
| 6.60 | IC50 | 251.2 | nM | CHEMBL3908230 |
| 6.40 | IC50 | 398.1 | nM | CHEMBL3946799 |
| 6.36 | IC50 | 440 | nM | CHEMBL4168948 |
| 6.30 | IC50 | 501.2 | nM | CHEMBL3951650 |
| 6.30 | IC50 | 501.2 | nM | CHEMBL3964547 |
| 6.30 | IC50 | 501.2 | nM | CHEMBL3908983 |
| 6.30 | IC50 | 501.2 | nM | CHEMBL3926111 |
| 6.20 | IC50 | 631 | nM | CHEMBL3908230 |
| 6.20 | IC50 | 631 | nM | CHEMBL3926111 |
| 6.20 | IC50 | 631 | nM | CHEMBL3955499 |
| 6.16 | IC50 | 690 | nM | CHEMBL3908230 |
PubChem BioAssay actives
68 with measured affinity, of 96 total; 38 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 |
|---|---|---|---|---|
| N-[4-(2-cyanopyrrol-1-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]-1H-indole-4-sulfonamide | 1323906: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by FLIPR assay | ic50 | 0.0004 | uM |
| 4-amino-3,5-dichloro-N-[4-(2-cyanopyrrol-1-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]benzenesulfonamide | 1323906: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by FLIPR assay | ic50 | 0.0020 | uM |
| 4-amino-3,5-dichloro-N-[(2R)-4-(2-cyanopyrrol-1-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]benzenesulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.0079 | uM |
| N-[4-(2-cyanopyrrol-1-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]-1H-indole-6-sulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.0079 | uM |
| N-[4-(2-cyanopyrrol-1-yl)-1-oxo-1-[4-(trifluoromethyl)piperidin-1-yl]butan-2-yl]-1H-indole-4-sulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.0100 | uM |
| N-[4-(2-cyanopyrrol-1-yl)-1-oxo-1-piperidin-1-ylbutan-2-yl]-1H-indole-4-sulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.0100 | uM |
| N-[4-(2-cyanopyrrol-1-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]-1H-indole-5-sulfonamide | 1323904: Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ic50 | 0.0126 | uM |
| N-[4-(2-cyanopyrrol-1-yl)-1-(2-methylpiperidin-1-yl)-1-oxobutan-2-yl]-1H-indole-4-sulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.0199 | uM |
| N-[1-(azepan-1-yl)-4-(2-cyanopyrrol-1-yl)-1-oxobutan-2-yl]-1H-indole-4-sulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.0251 | uM |
| 2-amino-4,6-dichloro-N-[4-(2-cyanopyrrol-1-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]benzenesulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.0398 | uM |
| 4-amino-3,5-dichloro-N-[1-(4-methylpiperidin-1-yl)-4-(2-nitroimidazol-1-yl)-1-oxobutan-2-yl]benzenesulfonamide | 1323904: Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ic50 | 0.0501 | uM |
| N-[4-(2-cyanopyrrol-1-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]naphthalene-1-sulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.0501 | uM |
| 4-amino-3,5-dichloro-N-[4-(5-cyanopyrazol-1-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]benzenesulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.0631 | uM |
| 4-amino-2,5-dichloro-N-[4-(2-cyanopyrrol-1-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]benzenesulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.0631 | uM |
| N-[4-(2-cyanopyrrol-1-yl)-1-(3-methylpiperidin-1-yl)-1-oxobutan-2-yl]-1H-indole-4-sulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.0631 | uM |
| 3-amino-N-[4-(2-cyanopyrrol-1-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]-2,4-dimethylbenzenesulfonamide | 1323904: Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ic50 | 0.0794 | uM |
| 4-amino-3,5-dichloro-N-[4-(2-chlorophenyl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]benzenesulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.1259 | uM |
| N-[4-(2-cyanopyrrol-1-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]-1-methylindole-4-sulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.1259 | uM |
| N-[4-(2-cyanopyrrol-1-yl)-1-(4-hydroxypiperidin-1-yl)-1-oxobutan-2-yl]-1H-indole-4-sulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.1259 | uM |
| 4-amino-3,5-dichloro-N-[4-(2-cyanopyrrol-1-yl)-1-oxo-1-piperidin-1-ylbutan-2-yl]benzenesulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.1585 | uM |
| 4-amino-N-[1-(azepan-1-yl)-4-(2-cyanopyrrol-1-yl)-1-oxobutan-2-yl]-3,5-dichlorobenzenesulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.2512 | uM |
| 4-amino-3,5-dichloro-N-[4-(2-chloroimidazol-1-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]benzenesulfonamide | 1323904: Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ic50 | 0.2512 | uM |
| 4-amino-3,5-dichloro-N-[4-(5-chloropyrazol-1-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]benzenesulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.2512 | uM |
| N-[4-(2-cyanopyrrol-1-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]-1H-indole-7-sulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.2512 | uM |
| 4-amino-3,5-dichloro-N-[4-(2-cyanopyrrol-1-yl)-1-oxo-1-[4-(trifluoromethyl)piperidin-1-yl]butan-2-yl]benzenesulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.3981 | uM |
| methyl (2S)-1-[(2R)-2-[methyl-[(2S)-2-[[(2S)-4-methyl-2-[methyl-[2-[[(2S)-1-[(2R,3S)-3-methyl-2-[(E)-3-phenylprop-2-enoyl]oxypentanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]pentanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]pyrrolidine-2-carboxylate | 1350790: Antagonist activity at human CCR10 expressed in human U2OS cells assessed as inhibition of CCL27-induced beta-arrestin recruitment pre-incubated for 30 mins before CCL27 stimulation for 90 or 180 mins by chemiluminescence method | ic50 | 0.4400 | uM |
| 4-amino-3,5-dichloro-N-[(2R)-1-(4-methylpiperidin-1-yl)-4-(2-nitroimidazol-1-yl)-1-oxobutan-2-yl]benzenesulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.5012 | uM |
| 4-amino-3,5-dichloro-N-[(2R)-1-(4-methylpiperidin-1-yl)-1-oxo-4-phenylbutan-2-yl]benzenesulfonamide | 1323904: Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ic50 | 0.5012 | uM |
| 4-amino-3,5-dichloro-N-[4-(2-cyanoimidazol-1-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]benzenesulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.5012 | uM |
| 4-amino-3,5-dichloro-N-[4-(2-cyanopyrrol-1-yl)-1-(3-methylpiperidin-1-yl)-1-oxobutan-2-yl]benzenesulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.6310 | uM |
| 4-amino-3,5-dichloro-N-[4-(2-cyanopyrrol-1-yl)-1-(2-methylpiperidin-1-yl)-1-oxobutan-2-yl]benzenesulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 0.7943 | uM |
| 4-amino-3,5-dichloro-N-[1-(4-methylpiperidin-1-yl)-1-oxo-4-(triazol-2-yl)butan-2-yl]benzenesulfonamide | 1323904: Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ic50 | 1.2589 | uM |
| 4-amino-3,5-dichloro-N-[1-(4-methylpiperidin-1-yl)-1-oxo-4-pyrazol-1-ylbutan-2-yl]benzenesulfonamide | 1323904: Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ic50 | 1.2589 | uM |
| N-[4-(2-cyanopyrrol-1-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutan-2-yl]benzenesulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 1.2589 | uM |
| methyl (2S)-1-[(2R)-2-[methyl-[(2S)-2-[[(2S)-4-methyl-2-[methyl-[2-[[(2S)-1-[(2R,3S)-3-methyl-2-[(Z)-3-phenylprop-2-enoyl]oxypentanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]pentanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]pyrrolidine-2-carboxylate | 1350790: Antagonist activity at human CCR10 expressed in human U2OS cells assessed as inhibition of CCL27-induced beta-arrestin recruitment pre-incubated for 30 mins before CCL27 stimulation for 90 or 180 mins by chemiluminescence method | ic50 | 2.7100 | uM |
| methyl (2S)-1-[(2R)-2-[methyl-[(2S)-2-[[(2S)-4-methyl-2-[methyl-[2-[[(2S)-1-[(2R,3S)-3-methyl-2-(3-phenylpropanoyloxy)pentanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]pentanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]pyrrolidine-2-carboxylate | 1350790: Antagonist activity at human CCR10 expressed in human U2OS cells assessed as inhibition of CCL27-induced beta-arrestin recruitment pre-incubated for 30 mins before CCL27 stimulation for 90 or 180 mins by chemiluminescence method | ic50 | 3.1400 | uM |
| 4-(2-cyanopyrrol-1-yl)-2-(1H-indol-4-ylsulfonylamino)-N,N-dimethylbutanamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 3.9811 | uM |
| 4-amino-3,5-dichloro-N-[1-(4-methylpiperidin-1-yl)-1-oxo-4-pyrrol-1-ylbutan-2-yl]benzenesulfonamide | 1323903: Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ic50 | 3.9811 | uM |
CTD chemical–gene interactions
12 total (human), top 12 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| S-(1,2-dichlorovinyl)cysteine | affects cotreatment, increases expression | 1 |
| entinostat | increases expression | 1 |
| abrine | increases expression | 1 |
| bisphenol S | decreases methylation | 1 |
| Benzo(a)pyrene | decreases methylation | 1 |
| Calcium | affects abundance | 1 |
| Cisplatin | decreases expression | 1 |
| Lipopolysaccharides | increases expression, affects cotreatment | 1 |
| Niclosamide | increases expression | 1 |
| Smoke | decreases expression | 1 |
| Aflatoxin B1 | decreases methylation | 1 |
| Acrylamide | increases expression | 1 |
ChEMBL screening assays
25 unique, capped per target: 16 functional, 9 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL2328027 | Binding | Antagonist activity at CCR10 (unknown origin) assessed as inhibition of chemotaxis at 10 uM | 1-(4-Phenylpiperazin-1-yl)-2-(1H-pyrazol-1-yl)ethanones as novel CCR1 antagonists. — Bioorg Med Chem Lett |
| CHEMBL2328619 | Functional | Antagonist activity at CCR10 (unknown origin) assessed as inhibition of calcium flux at 10 uM | 1-(4-Phenylpiperazin-1-yl)-2-(1H-pyrazol-1-yl)ethanones as novel CCR1 antagonists. — Bioorg Med Chem Lett |
Cellosaurus cell lines
3 cell lines: 2 cancer cell line, 1 spontaneously immortalized cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_KU88 | cAMP Hunter CHO-K1 CCR10 Gi | Spontaneously immortalized cell line | Female |
| CVCL_KZ92 | PathHunter U2OS CCR10 Activated GPCR Internalization | Cancer cell line | Female |
| CVCL_KZ93 | PathHunter U2OS CCR10 beta-arrestin | 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.