CCR9
gene geneOn this page
Also known as GPR-9-6CDw199
Summary
CCR9 (C-C motif chemokine receptor 9, HGNC:1610) is a protein-coding gene on chromosome 3p21.31, encoding C-C chemokine receptor type 9 (P51686). Receptor for chemokine SCYA25/TECK.
The protein encoded by this gene is a G protein-coupled receptor with seven transmembrane domains that belongs to the beta chemokine receptor family. Chemokines and their receptors are key regulators of thymocyte migration and maturation in normal and inflammation conditions. This gene is differentially expressed in T lymphocytes of the small intestine and colon, and its interaction with chemokine 25 contributes to intestinal intra-epithelial lymphocyte homing to the small intestine. This suggests a role for this gene in directing immune responses to different segments of the gastrointestinal tract. This gene and its exclusive ligand, chemokine 25, are overexpressed in a variety of malignant tumors and are closely associated with tumor proliferation, apoptosis, invasion, migration and drug resistance. This gene maps to the chemokine receptor gene cluster. Multiple transcript variants encoding different isoforms have been found for this gene.
Source: NCBI Gene 10803 — RefSeq curated summary.
At a glance
- Clinical variants (ClinVar): 60 total
- GTEx eGene: eQTL in 6 tissues, sQTL in 0 (q < 0.05)
- Drug target: yes — 2 curated mechanism-of-action drugs; 1 molecules with ChEMBL bioactivity
- Constraint (gnomAD): pLI 0.26 (intermediate), LOEUF 0.99 (unconstrained)
- MANE Select transcript:
NM_031200 - Notable: 60 clinical variants but no curated precision-oncology (CIViC) evidence yet
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:1610 |
| Approved symbol | CCR9 |
| Name | C-C motif chemokine receptor 9 |
| Location | 3p21.31 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | GPR-9-6, CDw199 |
| Ensembl gene | ENSG00000173585 |
| Ensembl biotype | protein_coding |
| OMIM | 604738 |
| Entrez | 10803 |
Gene structure
Transcript identifiers
Ensembl transcripts: 8 — 7 protein_coding, 1 retained_intron
MANE Select: ENST00000357632
Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 3, TSL 4: 1
ENST00000357632, ENST00000395963, ENST00000422395, ENST00000463197, ENST00000706789, ENST00000902118, ENST00000959606, ENST00001145197
RefSeq mRNA: 5 — MANE Select: NM_031200
NM_001256369, NM_001386447, NM_001386448, NM_006641, NM_031200
CCDS: CCDS2732, CCDS2733
Canonical transcript exons
ENST00000357632 — 3 exons
| Exon | Start | End |
|---|---|---|
| ENSE00003587279 | 45900810 | 45903174 |
| ENSE00003627693 | 45894906 | 45894954 |
| ENSE00003841903 | 45886543 | 45886655 |
Expression profiles
Bgee: expression breadth ubiquitous, 106 present calls, max score 93.19.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.6415 / max 427.3848, expressed in 67 samples.
Highest expression (Bgee): thymus, duodenum, small intestine Peyer’s patch, small intestine, granulocyte.
Genetic regulation across tissues (GTEx eQTL / sQTL)
CCR9 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 6 tissues and its splicing (sQTL) in 0 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.
6 significant tissue × QTL associations:
| Tissue | QTL | q-value | Slope | Lead variant |
|---|---|---|---|---|
| Thyroid | eqtl | 3.6e-06 | -0.30 | 3:45921260:T:C |
| Nerve Tibial | eqtl | 1.4e-04 | -0.20 | 3:46054546:C:T |
| Colon Transverse | eqtl | 1.8e-04 | +0.32 | 3:46137047:A:G |
| Skin Sun Exposed Lower leg | eqtl | 4.3e-03 | -0.23 | 3:45996955:G:A |
| Breast Mammary Tissue | eqtl | 1.7e-02 | +0.91 | 3:46103671:G:A |
| Adipose Visceral Omentum | eqtl | 4.6e-02 | +0.84 | 3:46498475:G:A |
FANTOM5 promoters
4 alternative TSS:
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 36395 | 0.4140 | 59 |
| 36394 | 0.1409 | 26 |
| 36396 | 0.0579 | 18 |
| 202741 | 0.0287 | 4 |
Top tissues by expression
showing 100 of 141 tissues by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| thymus | UBERON:0002370 | 93.19 | gold quality |
| duodenum | UBERON:0002114 | 72.52 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 67.95 | gold quality |
| small intestine | UBERON:0002108 | 67.69 | gold quality |
| granulocyte | CL:0000094 | 66.31 | gold quality |
| sural nerve | UBERON:0015488 | 64.60 | gold quality |
| vermiform appendix | UBERON:0001154 | 62.25 | gold quality |
| vastus lateralis | UBERON:0001379 | 60.30 | gold quality |
| quadriceps femoris | UBERON:0001377 | 60.14 | gold quality |
| bone marrow cell | CL:0002092 | 59.89 | silver quality |
| blood | UBERON:0000178 | 59.14 | gold quality |
| trachea | UBERON:0003126 | 59.07 | gold quality |
| dorsal plus ventral thalamus | UBERON:0001897 | 59.03 | gold quality |
| dorsal root ganglion | UBERON:0000044 | 58.67 | gold quality |
| bone marrow | UBERON:0002371 | 58.30 | gold quality |
| epithelium of bronchus | UBERON:0002031 | 58.19 | gold quality |
| layer of synovial tissue | UBERON:0007616 | 57.91 | gold quality |
| spleen | UBERON:0002106 | 57.85 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 57.82 | gold quality |
| cerebellar vermis | UBERON:0004720 | 57.59 | gold quality |
| leukocyte | CL:0000738 | 57.27 | gold quality |
| monocyte | CL:0000576 | 56.06 | gold quality |
| metanephric glomerulus | UBERON:0004736 | 55.97 | gold quality |
| colonic epithelium | UBERON:0000397 | 54.33 | silver quality |
| lymph node | UBERON:0000029 | 53.84 | gold quality |
| skeletal muscle tissue | UBERON:0001134 | 53.09 | gold quality |
| mucosa of stomach | UBERON:0001199 | 52.46 | gold quality |
| muscle tissue | UBERON:0002385 | 51.90 | gold quality |
| gall bladder | UBERON:0002110 | 51.76 | gold quality |
| apex of heart | UBERON:0002098 | 51.62 | gold quality |
| frontal pole | UBERON:0002795 | 50.41 | gold quality |
| middle frontal gyrus | UBERON:0002702 | 50.30 | gold quality |
| paraflocculus | UBERON:0005351 | 50.18 | gold quality |
| Brodmann (1909) area 10 | UBERON:0013541 | 50.18 | gold quality |
| rectum | UBERON:0001052 | 49.67 | gold quality |
| calcaneal tendon | UBERON:0003701 | 49.67 | silver quality |
| intestine | UBERON:0000160 | 49.47 | gold quality |
| islet of Langerhans | UBERON:0000006 | 49.18 | gold quality |
| tonsil | UBERON:0002372 | 49.08 | gold quality |
| smooth muscle tissue | UBERON:0001135 | 47.11 | gold quality |
| endometrium epithelium | UBERON:0004811 | 46.85 | gold quality |
| prefrontal cortex | UBERON:0000451 | 45.88 | gold quality |
| tibial nerve | UBERON:0001323 | 45.86 | gold quality |
| superior frontal gyrus | UBERON:0002661 | 45.07 | silver quality |
| muscle of leg | UBERON:0001383 | 44.97 | gold quality |
| left uterine tube | UBERON:0001303 | 44.91 | gold quality |
| transverse colon | UBERON:0001157 | 44.50 | gold quality |
| adult mammalian kidney | UBERON:0000082 | 44.38 | gold quality |
| gastrocnemius | UBERON:0001388 | 44.35 | gold quality |
| liver | UBERON:0002107 | 44.05 | silver quality |
| corpus callosum | UBERON:0002336 | 43.89 | silver quality |
| fallopian tube | UBERON:0003889 | 43.83 | gold quality |
| kidney | UBERON:0002113 | 43.52 | gold quality |
| frontal cortex | UBERON:0001870 | 43.44 | gold quality |
| olfactory segment of nasal mucosa | UBERON:0005386 | 43.37 | gold quality |
| colon | UBERON:0001155 | 42.73 | gold quality |
| ectocervix | UBERON:0012249 | 42.41 | gold quality |
| lung | UBERON:0002048 | 41.73 | gold quality |
| pancreas | UBERON:0001264 | 41.43 | gold quality |
| right lung | UBERON:0002167 | 41.03 | silver quality |
| stomach | UBERON:0000945 | 40.70 | gold quality |
| metanephros cortex | UBERON:0010533 | 40.50 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 40.38 | silver quality |
| urinary bladder | UBERON:0001255 | 40.25 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 40.19 | gold quality |
| right lobe of liver | UBERON:0001114 | 40.16 | silver quality |
| ventricular zone | UBERON:0003053 | 39.98 | gold quality |
| fundus of stomach | UBERON:0001160 | 39.67 | gold quality |
| body of stomach | UBERON:0001161 | 39.56 | gold quality |
| uterine cervix | UBERON:0000002 | 39.51 | gold quality |
| placenta | UBERON:0001987 | 38.49 | gold quality |
| multicellular organism | UBERON:0000468 | 38.47 | gold quality |
| cortex of kidney | UBERON:0001225 | 38.39 | gold quality |
| cerebral cortex | UBERON:0000956 | 38.20 | gold quality |
| Brodmann (1909) area 9 | UBERON:0013540 | 37.85 | silver quality |
| primary visual cortex | UBERON:0002436 | 37.84 | gold quality |
| endometrium | UBERON:0001295 | 37.71 | gold quality |
| skin of abdomen | UBERON:0001416 | 37.62 | gold quality |
| uterus | UBERON:0000995 | 36.83 | silver quality |
| zone of skin | UBERON:0000014 | 36.59 | gold quality |
| body of pancreas | UBERON:0001150 | 36.52 | silver quality |
| cortical plate | UBERON:0005343 | 36.47 | gold quality |
| omental fat pad | UBERON:0010414 | 36.40 | gold quality |
| sigmoid colon | UBERON:0001159 | 36.36 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 36.23 | gold quality |
| body of uterus | UBERON:0009853 | 35.94 | silver quality |
| esophagus mucosa | UBERON:0002469 | 35.88 | silver quality |
| skin of leg | UBERON:0001511 | 35.84 | gold quality |
| prostate gland | UBERON:0002367 | 35.77 | gold quality |
| right frontal lobe | UBERON:0002810 | 35.59 | gold quality |
| ganglionic eminence | UBERON:0004023 | 35.49 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 35.42 | gold quality |
| thoracic mammary gland | UBERON:0005200 | 35.23 | gold quality |
| myometrium | UBERON:0001296 | 35.02 | silver quality |
| adipose tissue | UBERON:0001013 | 35.00 | gold quality |
| adrenal tissue | UBERON:0018303 | 34.36 | gold quality |
| esophagus | UBERON:0001043 | 34.33 | silver quality |
| descending thoracic aorta | UBERON:0002345 | 34.32 | gold quality |
| spinal cord | UBERON:0002240 | 34.12 | gold quality |
| saliva-secreting gland | UBERON:0001044 | 34.05 | silver quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 3.42 |
HPA expression
RNA tissue specificity: Tissue enhanced
showing 60 of 209 HPA tissues / cells by nTPM:
| Tissue / cell | Axis | nTPM | Protein (IHC) |
|---|---|---|---|
| Thymus | tissue | 120.8 | |
| Locus coeruleus | tissue | 20.2 | |
| Pituitary gland | tissue | 19.6 | |
| Placenta | tissue | 15.0 | high |
| Liver | tissue | 8.8 | not detected |
| Postcentral gyrus | tissue | 8.3 | |
| Caudate putamen | tissue | 7.9 | |
| Choroid plexus | tissue | 7.2 | |
| Postcentral gyrus | tissue | 6.9 | |
| Hippocampus | tissue | 6.7 | not detected |
| Nucleus accumbens | tissue | 6.4 | |
| Cerebral cortex | tissue | 6.4 | low |
| Somatosensory cortex | tissue | 6.4 | |
| Locus coeruleus | tissue | 6.1 | |
| Hippocampus | tissue | 6.1 | low |
| Nucleus accumbens | tissue | 5.9 | |
| Occipital cortex | tissue | 5.6 | |
| Small intestine | tissue | 5.3 | not detected |
| Motor cortex | tissue | 5.3 | |
| Putamen | tissue | 5.0 | |
| Frontal cortex | tissue | 4.8 | |
| Temporal cortex | tissue | 4.4 | |
| Superior colliculi | tissue | 4.3 | |
| Hippocampal formation | tissue | 4.3 | |
| Entorhinal cortex | tissue | 4.3 | |
| Substantia nigra | tissue | 4.2 | |
| Prefrontal cortex | tissue | 4.2 | |
| Retrosplenial and cingulate cortex | tissue | 4.2 | |
| Adipose tissue | tissue | 4.1 | low |
| Thalamus | tissue | 3.8 | |
| Duodenum | tissue | 3.7 | not detected |
| Adipose tissue | tissue | 3.7 | not detected |
| Basal ganglia | tissue | 3.7 | not detected |
| Retrosplenial cortex | tissue | 3.7 | |
| Pons | tissue | 3.6 | |
| Skeletal muscle | tissue | 3.5 | medium |
| Insular cortex | tissue | 3.4 | |
| Superior colliculi | tissue | 3.1 | |
| Medulla oblongata | tissue | 3.1 | |
| Cerebellum | tissue | 3.1 | medium |
| Vagina | tissue | 3.0 | low |
| Midbrain | tissue | 3.0 | |
| Superior colliculi | tissue | 2.9 | |
| Spinal cord | tissue | 2.9 | |
| Medulla oblongata | tissue | 2.8 | |
| Spinal cord | tissue | 2.7 | |
| Epididymis | tissue | 2.6 | not detected |
| Substantia nigra | tissue | 2.6 | |
| Hypothalamus | tissue | 2.5 | |
| Periaqueductal gray | tissue | 2.5 | |
| Breast | tissue | 2.3 | low |
| Hippocampal formation | tissue | 2.3 | |
| Entorhinal cortex | tissue | 2.3 | |
| Amygdala | tissue | 2.3 | |
| Ventral forebrain | tissue | 2.3 | |
| Vagina | tissue | 2.2 | not detected |
| Fallopian tube | tissue | 2.2 | high |
| Corpus callosum | tissue | 2.2 | |
| Olfactory bulb | tissue | 2.2 | |
| Septum | tissue | 2.2 |
Brain sub-regions (HPA Brain Atlas): detected in 569; highest nTPM — Arcuate nucleus (19.3), Median raphe nucleus (15.7), Nucleus ambiguus (14.1), Ventromedial nucleus (14.1), Piriform cortex (12.5).
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
Targeting CCR9 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).
showing 30 of 65 miRNAs:
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-4455 | 100.00 | 65.48 | 1587 |
| HSA-MIR-1252-5P | 100.00 | 69.80 | 2774 |
| HSA-MIR-4682 | 100.00 | 68.89 | 1258 |
| HSA-MIR-6077 | 99.99 | 68.04 | 2299 |
| HSA-MIR-223-3P | 99.99 | 70.14 | 1140 |
| HSA-MIR-4789-5P | 99.98 | 70.76 | 2721 |
| HSA-MIR-433-3P | 99.98 | 69.37 | 1203 |
| HSA-MIR-27A-3P | 99.98 | 72.13 | 2955 |
| HSA-MIR-27B-3P | 99.98 | 72.13 | 2955 |
| HSA-MIR-9985 | 99.98 | 72.11 | 2939 |
| HSA-MIR-25-3P | 99.98 | 74.60 | 1817 |
| HSA-MIR-32-5P | 99.98 | 75.21 | 1964 |
| HSA-MIR-363-3P | 99.98 | 74.72 | 1821 |
| HSA-MIR-367-3P | 99.98 | 74.83 | 1819 |
| HSA-MIR-92A-3P | 99.98 | 75.21 | 1960 |
| HSA-MIR-92B-3P | 99.98 | 75.25 | 1955 |
| HSA-MIR-146A-5P | 99.96 | 68.93 | 988 |
| HSA-MIR-146B-5P | 99.96 | 69.13 | 977 |
| HSA-MIR-128-3P | 99.95 | 71.17 | 2484 |
| HSA-MIR-216A-3P | 99.95 | 71.19 | 2505 |
| HSA-MIR-7153-5P | 99.94 | 68.89 | 1006 |
| HSA-MIR-589-3P | 99.91 | 69.62 | 2088 |
| HSA-MIR-8063 | 99.91 | 69.76 | 3146 |
| HSA-MIR-3681-3P | 99.88 | 70.46 | 2254 |
| HSA-MIR-182-5P | 99.87 | 74.03 | 2589 |
| HSA-MIR-6875-3P | 99.82 | 70.26 | 2983 |
| HSA-MIR-204-5P | 99.79 | 71.62 | 2439 |
| HSA-MIR-211-5P | 99.79 | 71.65 | 2440 |
| HSA-MIR-4524A-3P | 99.72 | 66.85 | 2406 |
| HSA-MIR-466 | 99.67 | 70.85 | 2863 |
Functional genomics
gnomAD constraint: pLI 0.262, LOEUF 0.987, missense Z 1.41 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD
Regional missense constraint (gnomAD RMC): no regional variation along ENST00000357632 — one region, missense o/e 0.87.
Literature-anchored findings (GeneRIF, showing 40)
- A subset of CCR9+ T cells from normal donors has characteristics of mucosal T cells in terms of activated phenotype, proliferative response to anti-CD2 stimulation, a Th1 or Tr1 cytokine profile, and support for Ig production by cocultured B cells. (PMID:12816994)
- CCR9 selectively induced T-ALL CD4+ T-cell chemotaxis and adhesion. (PMID:14559839)
- High Expression of CCR9 is associated with prostate cancer cell migration and invasion (PMID:15623660)
- involved in the pathogenesis of lymphatic filarial disease (PMID:15717282)
- CCR9 overexpression is associated with Adult T-cell leukemia cells infiltrating gastrointestinal tract (PMID:17205512)
- CCR9 expression is reduced on epithelial and lamina propria T cells in untreated celiac disease. Down-regulation of CCR9 persists in intraepithelial T cells from well-treated patients. Possible ongoing immune activation preferentially within epithelium. (PMID:17570212)
- CCR9 is expressed on human melanoma cells and participates in the enhanced motility of melanoma cells and is likely a “homing receptor” for melanoma to the small bowel. (PMID:18245518)
- Functionally active CCR9 on melanoma cells facilitates metastasis to the small intestine which may explain high incidence of metastis to the small intestine. (PMID:18245522)
- more active homing of CCR9-926AG T cells to Peyer’s patches may produce changes in Ag presentation and result in increased incidence of skin graft vs. host disease. (PMID:19525985)
- Results demonstrate enhanced pancreatic intraepithelial neoplasia and pancreatic cancer cell proliferation with activation of CCR9 by its selective ligand CCL25 (PMID:19756884)
- Studies indicate that D6 chemokine receptor(CCR-9) may act as scavenging decoys and are involved in clearance of chemokines. (PMID:20036838)
- over-expressed TECK interacts with CCR9 on the endometrial stromal cells in the endometriotic milieu, which may contribute to the onset and progression of endometriosis. (PMID:20081876)
- CCR9 expression by monocytes is increased in rheumatoid arthritis (PMID:20738854)
- 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)
- CCL25 enhanced the expression of MMP-1, -9, -11 and -13 active proteins by BrCa cells in a CCR9-dependent fashion. (PMID:21344163)
- CCR9+ Th cells are a subset of IL-21-producing T helper cells that influence regional specification of autoimmune diseases that affect accessory organs of the digestive system (PMID:21511186)
- We provide the first evidence that CCR9 and its natural ligand CCL25 are highly expressed by ovarian cancer tissue and their expression correlates with histological subtypes. (PMID:21637913)
- Notch1 regulates chemotaxis and proliferation by controlling the CC-chemokine receptors 5 and 9 in T cell acute lymphoblastic leukaemia. (PMID:21984373)
- Data suggest that P-glycoprotein associate with the F-actin cytoskeleton through ezrin/radixin/moesin (ERM) in CCR9/CCL25 induced multidrug resistance of acute T-lymphocytic leukemia (T-ALL) cells. (PMID:23326330)
- results suggest that CCR9 can act as a novel prognostic marker and therapeutic target for hepatocellular carcinoma (PMID:24481516)
- Only rotavirus specific CD4 T cells expressed intestinal homing receptors alpha4beta7 and CCR9. (PMID:24606696)
- CCR9 expression is elevated in the nodal lymphomas of patients with GI involvement (PMID:24828696)
- The results show the potential of the 91R monoclonal antibody as a therapeutic agent for treatment of CCR9-expressing tumors. (PMID:24870448)
- High CCR9 expression is associated with the pathogenesis of ulcerative colitis. (PMID:24936795)
- Expression of CCR9 and CCL25, the only natural ligand of CCR9, was significantly higher (p<0.0001) in NSCLC tissues and serum respectively, compared to their respective controls. (PMID:25296976)
- CCR9-CCL25 interaction promoted proliferation and suppressed apoptosis of non-small cell lung cancer cells by activating the PI3K/Akt pathway. (PMID:25691296)
- activation of Notch1 has a dominant-negative effect on Ccr9 transcription and that Notch1 and E proteins control the dynamic expression of Ccr9 during T cell development. (PMID:25710912)
- We also show that primary tumors can be modeled in immunocompetent mice by microinjecting CCR9-expressing cancer cell lines into early-stage mouse blastocysts, which induces central immune tolerance (PMID:26006007)
- CCR9 could be beneficial in predicting lymph node metastasis, and it might act as a novel prognostic biomarker for lung adenocarcinoma. (PMID:26168791)
- CCR9 mRNA and protein levels were significantly increased in the nasopharyngeal carcinoma group compared with the control group. (PMID:26279399)
- CCR9 and Integrin-beta7 expression has a differential effect on graft fate during acute graft-versus-host disease (GVHD) of the liver depending on the GVHD target tissue. (PMID:26348893)
- Results indicated that the expression levels of CCR9 in lesional skin may be a useful biologic marker of the clinical efficacy of infliximab therapy in psoriasis patients. (PMID:26507968)
- this study showed that CCR7 are overexpressed in CD4(-) CD8(-) thymocytes of myasthenia gravis patients. (PMID:26616645)
- Studies indicate important roles played by chemokine ligand 25 (CCL25)/chemokine receptor 9 (CCR9) in tumorigenesis, tumor chemoresistance and metastasis. (PMID:26879872)
- that CCL25/CCR9 signal may provide cancer cells with chemotactic abilities through influencing several epithelial-mesenchymal transitionmarkers (PMID:27008282)
- There were significantly increased CCR9 protein levels in failing human hearts. (PMID:27146447)
- It plays a pathogenic role in liver diseases and it will be a therapeutic target of the diseases. (PMID:27795503)
- Xray crystal structure of the CCR9 receptor in complex with vercirnon at 2.8 A resolution (PMID:27926729)
- our observations of increased circulating CCR9+ IL-17+ Treg cells and its inverse correlation with the severity of intestinal tissue injury in NEC are novel (PMID:31129099)
Cross-species orthologs
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | ccr9a | ENSDARG00000055186 |
| danio_rerio | ccr9b | ENSDARG00000099738 |
| mus_musculus | Ccr9 | ENSMUSG00000029530 |
| rattus_norvegicus | Ccr9 | ENSRNOG00000006311 |
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), CCR8 (ENSG00000179934), CXCR2 (ENSG00000180871), GALR2 (ENSG00000182687), CCR3 (ENSG00000183625), CCR4 (ENSG00000183813), CCR10 (ENSG00000184451), CXCR3 (ENSG00000186810)
Mouse-model phenotypes
Observed phenotypes of the mouse ortholog (MGI:1341902) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 17 distinct phenotype terms.
| Mouse phenotype (MP) | Records |
|---|---|
| abnormal T cell differentiation | 2 |
| abnormal leukocyte cell number | 1 |
| decreased thymocyte number | 1 |
| impaired coordination | 1 |
| abnormal T cell subpopulation ratio | 1 |
| increased T cell number | 1 |
| decreased lymphocyte cell number | 1 |
| decreased T cell number | 1 |
| decreased double-positive T cell number | 1 |
| abnormal mesenteric lymph node morphology | 1 |
| impaired glucose tolerance | 1 |
| decreased pro-B cell number | 1 |
| abnormal gamma-delta T cell number | 1 |
| increased gamma-delta T cell number | 1 |
| abnormal gamma-delta intraepithelial T cell morphology | 1 |
| decreased gamma-delta intraepithelial T cell number | 1 |
| decreased CD8-positive, gamma-delta intraepithelial T cell number | 1 |
Additional cross-species homologs
Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.
| Organism | UniProt | Identity | Method |
|---|---|---|---|
| Trachypithecus phayrei | O97879 | 100.0% | Diamond |
| Pongo pygmaeus | O97881 | 100.0% | Diamond |
| Pan troglodytes | P56440 | 100.0% | Diamond |
| Pan paniscus | P60574 | 100.0% | Diamond |
| Lophocebus aterrimus | P61755 | 100.0% | Diamond |
| Pongo abelii | P61756 | 100.0% | Diamond |
| Semnopithecus entellus | P61757 | 100.0% | Diamond |
| Macaca mulatta | P61813 | 100.0% | Diamond |
| Macaca fascicularis | P61814 | 100.0% | Diamond |
| Macaca nemestrina | P61815 | 100.0% | Diamond |
| Papio anubis | P68269 | 100.0% | Diamond |
| Papio hamadryas | P68270 | 100.0% | Diamond |
| Cercocebus atys | O62743 | 99.7% | Diamond |
| Trachypithecus francoisi | O97878 | 99.7% | Diamond |
| Rhinopithecus bieti | O97880 | 99.7% | Diamond |
| Rhinopithecus avunculus | O97962 | 99.7% | Diamond |
| Macaca arctoides | O97975 | 99.7% | Diamond |
| Meleagris gallopavo | P33396 | 99.7% | Diamond |
| Gorilla gorilla gorilla | P56439 | 99.7% | Diamond |
| Gallus gallus | P79785 | 99.7% | Diamond |
| Saimiri sciureus | Q8HZU0 | 99.7% | Diamond |
| Callithrix jacchus | Q8HZU1 | 99.7% | Diamond |
| Hylobates moloch | Q95NC0 | 99.7% | Diamond |
| Theropithecus gelada | Q95NC1 | 99.7% | Diamond |
| Symphalangus syndactylus | Q95NC5 | 99.7% | Diamond |
| Nasalis larvatus | Q95NC7 | 99.7% | Diamond |
| Colobus polykomos | Q95NC8 | 99.7% | Diamond |
| Chlorocebus aethiops | Q9TSQ8 | 99.7% | Diamond |
| Cercocebus galeritus | Q9TV49 | 99.7% | Diamond |
| Pygathrix nemaeus | O97882 | 99.4% | Diamond |
| Nomascus leucogenys | O97883 | 99.4% | Diamond |
| Trachypithecus johnii | Q95NC6 | 99.4% | Diamond |
| Mandrillus sphinx | Q95ND1 | 99.4% | Diamond |
| Mandrillus leucophaeus | Q95ND2 | 99.4% | Diamond |
| Chlorocebus tantalus | Q95NE8 | 99.4% | Diamond |
| Allochrocebus solatus | Q9BGN6 | 99.4% | Diamond |
| Chlorocebus pygerythrus | Q9TV42 | 99.4% | Diamond |
| Allochrocebus lhoesti | Q9XT76 | 99.4% | Diamond |
| Miopithecus talapoin | Q95NC3 | 99.1% | Diamond |
| Erythrocebus patas | Q95ND0 | 99.1% | Diamond |
Genomic neighbors (locus context)
Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).
| Symbol | Type | Entrez |
|---|---|---|
| CXCR6 | protein-coding | 10663 |
| XCR1 | protein-coding | 2829 |
| LZTFL1 | protein-coding | 54585 |
| FYCO1 | protein-coding | 79443 |
| SACM1L | protein-coding | 22908 |
| SLC6A20 | protein-coding | 54716 |
Protein
Protein identifiers
C-C chemokine receptor type 9 — P51686 (reviewed: P51686)
Alternative names: G protein-coupled receptor 28, GPR-9-6
All UniProt accessions (2): C9JWC0, P51686
UniProt curated annotations — full annotation on UniProt →
Function. Receptor for chemokine SCYA25/TECK. Subsequently transduces a signal by increasing the intracellular calcium ions level. (Microbial infection) Alternative coreceptor with CD4 for HIV-1 infection.
Subcellular location. Cell membrane.
Tissue specificity. Highly expressed in the thymus and low in lymph nodes and spleen.
Miscellaneous. EC50 of SCYA25/TECK for isoform 1 is lower than for isoform 2.
Similarity. Belongs to the G protein-coupled receptor 1 family.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P51686-1 | 1, CCR9A | yes |
| P51686-2 | 2, CCR9B |
RefSeq proteins (5): NP_001243298, NP_001373376, NP_001373377, NP_006632, NP_112477* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000276 | GPCR_Rhodpsn | Family |
| IPR000355 | Chemokine_rcpt | Family |
| IPR004069 | Chemokine_CCR9 | Family |
| IPR017452 | GPCR_Rhodpsn_7TM | Domain |
| IPR050119 | CCR1-9-like | Family |
Pfam: PF00001
UniProt features (41 total): helix 19, topological domain 8, transmembrane region 7, disulfide bond 2, sequence variant 2, chain 1, glycosylation site 1, splice variant 1
Structure
Experimental structures (PDB)
1 structures by resolution:
| PDB | Title | Method | Resolution (Å) |
|---|---|---|---|
| 5LWE | Crystal structure of the human CC chemokine receptor type 9 (CCR9) in complex with … | X-RAY DIFFRACTION | 2.8 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P51686-F1 | 83.69 | 0.45 |
Human Protein Atlas
Protein class: Transporters, G-protein coupled receptors, GPCRs excl olfactory receptors, Chemokines and chemotactic factors receptors, Predicted membrane proteins, GPCRHMM predicted membrane proteins
Protein evidence: Evidence at protein level
Subcellular location (HPA, imaging): cytosol; vesicles; nucleoplasm
Antibody reliability (HPA): IH enhanced · IF supported
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)
| Type | Positions |
|---|---|
| Disulfide bond | 38–289, 119–198 |
Glycosylation sites (1)
| Type | Positions |
|---|---|
| N-linked (glcnac…) asparagine | 32 |
Function
Pathways and Gene Ontology
Reactome pathways
2 curated (TAS) of 8; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).
8 pathways:
| ID | Pathway | Evidence |
|---|---|---|
| R-HSA-380108 | Chemokine receptors bind chemokines | curated |
| R-HSA-418594 | G alpha (i) signalling events | curated |
| R-HSA-373076 | Class A/1 (Rhodopsin-like receptors) | — |
| R-HSA-388396 | GPCR downstream signalling | — |
| R-HSA-500792 | GPCR ligand binding | — |
| R-HSA-375276 | Peptide ligand-binding receptors | — |
| R-HSA-162582 | Signal Transduction | — |
| R-HSA-372790 | Signaling by GPCR | — |
MSigDB gene sets: 242 (showing top):
GOBP_CELL_CHEMOTAXIS, GOBP_RESPONSE_TO_PEPTIDE, MODULE_64, GOCC_CELL_SURFACE, HSIAO_HOUSEKEEPING_GENES, GGGTGGRR_PAX4_03, ACEVEDO_LIVER_CANCER_WITH_H3K27ME3_UP, GCM_PRKCG, GOBP_TAXIS, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, YGACNNYACAR_UNKNOWN, GCM_RING1, OSWALD_HEMATOPOIETIC_STEM_CELL_IN_COLLAGEN_GEL_UP, MODULE_75, SU_THYMUS
GO Biological Process (9): chemotaxis (GO:0006935), immune response (GO:0006955), cellular defense response (GO:0006968), 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), chemokine-mediated signaling pathway (GO:0070098)
GO Molecular Function (4): chemokine receptor activity (GO:0004950), C-C chemokine receptor activity (GO:0016493), C-C chemokine binding (GO:0019957), G protein-coupled receptor activity (GO:0004930)
GO Cellular Component (4): plasma membrane (GO:0005886), external side of plasma membrane (GO:0009897), cell surface (GO:0009986), membrane (GO:0016020)
Reactome top-level categories
6 top-level categories:
| 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
33 GO namespaces:
| Category | Terms |
|---|---|
| G protein-coupled receptor signaling pathway | 2 |
| chemokine binding | 2 |
| cellular anatomical structure | 2 |
| response to chemical | 1 |
| taxis | 1 |
| immune system process | 1 |
| response to stimulus | 1 |
| defense response | 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 |
| 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 |
| G protein-coupled chemoattractant receptor activity | 1 |
| cytokine receptor activity | 1 |
| chemokine-mediated signaling pathway | 1 |
| chemokine receptor activity | 1 |
| C-C chemokine binding | 1 |
| transmembrane signaling receptor activity | 1 |
| membrane | 1 |
| cell periphery | 1 |
| plasma membrane | 1 |
| cell surface | 1 |
| side of membrane | 1 |
Experimentally-supported GO annotations
GO terms backed by direct experimental evidence (ECO experimental codes) — 1 of 17 annotations. The rest are phylogenetic / computational / electronic (IEA).
1 experimentally-supported GO terms:
| GO term | NS | Evidence |
|---|---|---|
| cell surface | CC | direct assay |
Protein interactions and networks
STRING
showing 15 of 1,242 interactions by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CCR9 | CCL25 | O15444 | 972 |
| CCR9 | MADCAM1 | Q13477 | 896 |
| CCR9 | CD8A | P01732 | 812 |
| CCR9 | ITGB7 | P26010 | 757 |
| CCR9 | ITGA4 | P13612 | 723 |
| CCR9 | CD4 | P01730 | 719 |
| CCR9 | ITGAE | P38570 | 702 |
| CCR9 | CCL28 | Q9NRJ3 | 698 |
| CCR9 | LZTFL1 | Q9NQ48 | 692 |
| CCR9 | SELPLG | Q14242 | 688 |
| CCR9 | SLC6A20 | Q9NP91 | 679 |
| CCR9 | IGBP1 | P78318 | 663 |
| CCR9 | CD19 | P15391 | 641 |
| CCR9 | FYCO1 | Q9BQS8 | 627 |
| CCR9 | FOXP3 | Q9BZS1 | 611 |
IntAct
Human interaction partners of CCR9 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).
19 partners by confidence:
| Partner | Interaction type | MIscore | Records |
|---|---|---|---|
| DGAT1 | physical association | 0.550 | 1 |
| ADGRG1 | physical association | 0.370 | 1 |
| AIG1 | physical association | 0.370 | 1 |
| CD81 | physical association | 0.370 | 1 |
| G6PC3 | physical association | 0.370 | 1 |
| HLA-A | physical association | 0.370 | 1 |
| KDELR1 | physical association | 0.370 | 1 |
| NEU1 | physical association | 0.370 | 1 |
| OSTC | physical association | 0.370 | 1 |
| RHBDD2 | physical association | 0.370 | 1 |
| SAP130 | physical association | 0.370 | 1 |
| SCAMP4 | physical association | 0.370 | 1 |
| SPNS1 | physical association | 0.370 | 1 |
| TMC6 | physical association | 0.370 | 1 |
| TRPM4 | physical association | 0.370 | 1 |
| TSPAN7 | physical association | 0.370 | 1 |
| TTYH1 | physical association | 0.370 | 1 |
| YWHAE | physical association | 0.370 | 1 |
| ABCC4 | association | 0.350 | 1 |
BioGRID (19 interactions; top human partners by supporting records): AIG1 (Two-hybrid), CD81 (Two-hybrid), DGAT1 (Two-hybrid), G6PC3 (Two-hybrid), GATAD2B (Cross-Linking-MS (XL-MS)), GPR56 (Two-hybrid), HLA-A (Two-hybrid), KDELR1 (Two-hybrid), NEU1 (Two-hybrid), OSTC (Two-hybrid), RHBDD2 (Two-hybrid), SAP130 (Two-hybrid), SCAMP4 (Two-hybrid), SPNS1 (Two-hybrid), TMC6 (Two-hybrid)
SIGNOR signaling
1 signaling interactions:
| A | Effect | B | Mechanism |
|---|---|---|---|
| CCL25 | up-regulates | CCR9 | binding |
Disease & clinical
Genetic variants
Variant evidence for CCR9: 60 ClinVar records (0 pathogenic / likely pathogenic).
ClinVar
60 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 53 |
| Likely benign | 1 |
| Benign | 2 |
AlphaMissense
692 missense substitutions predicted likely pathogenic (of 2,467 scored), across 208 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:
| Residue | Likely-pathogenic substitutions | Mean am_pathogenicity | Max am_pathogenicity |
|---|---|---|---|
| D94 | 8 | 0.973 | 0.991 |
| N66 | 8 | 0.968 | 0.991 |
| F324 | 8 | 0.947 | 0.992 |
| F263 | 8 | 0.918 | 0.990 |
| N313 | 8 | 0.917 | 0.982 |
| D143 | 8 | 0.909 | 0.968 |
| F97 | 8 | 0.881 | 0.962 |
| D84 | 8 | 0.842 | 0.907 |
| H309 | 8 | 0.834 | 0.967 |
| F319 | 8 | 0.769 | 0.939 |
| C198 | 7 | 0.984 | 0.992 |
| C119 | 7 | 0.980 | 0.993 |
| W112 | 7 | 0.968 | 0.996 |
| C289 | 7 | 0.959 | 0.975 |
| C38 | 7 | 0.947 | 0.975 |
| R144 | 7 | 0.911 | 0.977 |
| W173 | 7 | 0.896 | 0.987 |
| F86 | 7 | 0.880 | 0.951 |
| F46 | 7 | 0.864 | 0.963 |
| N129 | 7 | 0.852 | 0.986 |
HPA cancer prognostics
RNA cancer specificity: Low cancer specificity
Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.
1 prognostic cancer types:
| Cancer | Prognostic | p-value |
|---|---|---|
| Kidney Renal Clear Cell Carcinoma (TCGA) | unfavorable | 0.00023 |
Disease associations
OMIM: gene MIM:604738 | disease phenotypes:
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL5815 (SINGLE PROTEIN)
Drugs by curated mechanism of action (ChEMBL)
Drugs whose curated ChEMBL mechanism of action targets the CCR9 protein itself — single-protein targets only (drugs acting on a protein family or complex that merely includes it are excluded). Includes antibodies and oligonucleotides that bioactivity screening does not capture.
2 curated-mechanism drugs:
| Drug | Modality | Max phase |
|---|---|---|
| VERCIRNON | Small molecule | 3 |
| MLN3126 | Unknown | 1 |
Molecules with ChEMBL bioactivity
Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 352 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
1 molecules by phase:
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL2178578 | VERCIRNON | 3 | 352 |
PharmGKB: 1 entry (CPIC guideline: no)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: gpcr — Chemokine receptors
Most potent curated ligand interactions (2 total), top 2:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| vercirnon | Antagonist | 8.22 | pIC50 |
| compound 24 [PMID: 26987013 ] | Antagonist | 8.22 | pKi |
Binding affinities (BindingDB)
187 measured of 190 human assays (190 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| CHEMBL3604484 | IC50 | 0.3 nM | |
| CHEMBL6170963 | KI | 0.53 nM | |
| CHEMBL3814804 | IC50 | 1.5 nM | |
| 4-tert-butyl-N-[7-chloro-2-(4-methoxy-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 2 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-(2-methoxy-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 3 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-(2-cyanothiophen-3-yl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 3 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-(3-methyl-4-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 3 nM | US-9969687: Compounds useful as CCR9 modulators |
| CHEMBL3604485 | IC50 | 3.2 nM | |
| 4-tert-butyl-N-[7-chloro-1,3-dioxo-2-(2-oxo-3H-pyridin-3-yl)isoindol-4-yl]benzenesulfonamide | KI | 4 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-(2,6-dimethyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 5 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-(2,6-dimethoxy-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 6 nM | US-9969687: Compounds useful as CCR9 modulators |
| CHEMBL3604496 | IC50 | 6 nM | |
| 4-tert-butyl-N-[7-chloro-2-[(3-fluoro-1-oxidopyridin-1-ium-2-yl)methyl]-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 7 nM | US-9969687: Compounds useful as CCR9 modulators |
| CHEMBL3814136 | IC50 | 8 nM | |
| 4-tert-butyl-N-[7-chloro-2-[(1-oxidopyridin-1-ium-2-yl)methyl]-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 10 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-(5-fluoro-2-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 10 nM | US-9969687: Compounds useful as CCR9 modulators |
| 3-[4-[(4-tert-butylphenyl)sulfonylamino]-7-chloro-1,3-dioxoisoindol-2-yl]pyridine-2-carboxylic acid | KI | 10 nM | US-9969687: Compounds useful as CCR9 modulators |
| CHEMBL2178578 | IC50 | 10 nM | |
| 4-tert-butyl-N-[7-chloro-2-(2-methoxy-5-methyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 11 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-(2,5-dimethyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 11 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-(7-chloro-1,3-dioxo-2-pyridin-4-ylisoindol-4-yl)benzenesulfonamide | KI | 11 nM | US-9969687: Compounds useful as CCR9 modulators |
| CHEMBL3604488 | IC50 | 11 nM | |
| CHEMBL3604495 | IC50 | 11 nM | |
| 4-tert-butyl-N-[7-chloro-2-(2-methyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 12 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-(3-methylimidazol-4-yl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 12 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-[(4-methyl-1-oxidopyridin-1-ium-3-yl)methyl]-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 12 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-(7-chloro-1,3-dioxo-2-pyridin-2-ylisoindol-4-yl)benzenesulfonamide | KI | 12 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-1,3-dioxo-2-[(2-oxo-3H-pyridin-3-yl)methyl]isoindol-4-yl]benzenesulfonamide | KI | 12 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-[(1-oxidopyridin-1-ium-3-yl)methyl]-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 13 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-(2-methyl-1-oxidopyridin-1-ium-3-yl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 13 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-(6-methoxy-2-methyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 13 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-[(3-fluoro-2-pyridinyl)methyl]-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 13 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-[(5-methyl-1-oxidopyridin-1-ium-2-yl)methyl]-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 13 nM | US-9969687: Compounds useful as CCR9 modulators |
| ethyl 3-[4-[(4-tert-butylphenyl)sulfonylamino]-7-chloro-1,3-dioxoisoindol-2-yl]pyridine-2-carboxylate | KI | 14 nM | US-9969687: Compounds useful as CCR9 modulators |
| ethyl 3-[4-[(4-tert-butylphenyl)sulfonylamino]-7-chloro-1,3-dioxoisoindol-2-yl]-1-oxidopyridin-1-ium-2-carboxylate | KI | 14 nM | US-9969687: Compounds useful as CCR9 modulators |
| CHEMBL3604492 | IC50 | 14 nM | |
| methyl 5-[4-[(4-tert-butylphenyl)sulfonylamino]-7-chloro-1,3-dioxoisoindol-2-yl]-1-methylpyrazole-3-carboxylate | KI | 15 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-(1-oxidopyridin-1-ium-3-yl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 16 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-[(4-methyl-3-pyridinyl)methyl]-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 16 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-(5-methoxy-6-methyl-2-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 16 nM | US-9969687: Compounds useful as CCR9 modulators |
| methyl 3-[4-[(4-tert-butylphenyl)sulfonylamino]-7-chloro-1,3-dioxoisoindol-2-yl]-1-methylpyrazole-5-carboxylate | KI | 16 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-1,3-dioxo-2-(pyridin-4-ylmethyl)isoindol-4-yl]benzenesulfonamide | KI | 17 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-cyano-2-(5-methoxy-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 17 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-cyano-1,3-dioxo-2-(pyridin-2-ylmethyl)isoindol-4-yl]benzenesulfonamide | KI | 17 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-(5-methoxy-4-methyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 18 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-(2-cyano-5-methyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 18 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-cyano-1,3-dioxo-2-(pyridin-3-ylmethyl)isoindol-4-yl]benzenesulfonamide | KI | 19 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-(6-methyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 19 nM | US-9969687: Compounds useful as CCR9 modulators |
| 4-tert-butyl-N-[7-chloro-2-(6-methyl-2-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | KI | 19 nM | US-9969687: Compounds useful as CCR9 modulators |
| CHEMBL3800073 | KI | 19 nM |
ChEMBL bioactivities
399 potent at pChembl≥5 of 400 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
180 with measured affinity, of 197 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 |
|---|---|---|---|---|
| 4-tert-butyl-N-(4-chloro-2-pyrimidin-2-ylphenyl)benzenesulfonamide | 1239784: Antagonist activity at CCR9 receptor (unknown origin) assessed as inhibition of TECK-induced calcium mobilization incubated for 10 mins prior to TECK induction | ic50 | 0.0003 | uM |
| N-[2-(4-aminopyrimidin-5-yl)-4-chlorophenyl]-4-tert-butylbenzenesulfonamide | 2269471: Binding affinity to CCR9 (unknown origin) expressed in HEK293T cells harbouring Nlu tagged CCR9 assessed as inhibition constant | ki | 0.0005 | uM |
| 4-tert-butyl-N-[4-chloro-2-(1-oxidopyridin-1-ium-4-carbonyl)phenyl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0011 | uM |
| 1-[(4-tert-butylphenyl)methyl]-6-chloropyrrolo[3,2-c]pyridine-2-carboxylic acid | 1306155: Antagonist activity at CCR9 (unknown origin) assessed as inhibition of TECK-stimulated calcium mobilization preincubated for 10 mins followed by agonist addition measured for 90 sec by fluo-8 dye-based FLIPR assay | ic50 | 0.0015 | uM |
| 4-tert-butyl-N-[7-chloro-2-(4-methoxy-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0020 | uM |
| 4-tert-butyl-N-[7-chloro-2-(2-methyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0030 | uM |
| 4-tert-butyl-N-[7-chloro-2-(2-methoxy-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0030 | uM |
| N-[2-(5-aminopyrimidin-4-yl)-4-chlorophenyl]-4-tert-butylbenzenesulfonamide | 1239784: Antagonist activity at CCR9 receptor (unknown origin) assessed as inhibition of TECK-induced calcium mobilization incubated for 10 mins prior to TECK induction | ic50 | 0.0032 | uM |
| N-[2-(3-aminopyrazin-2-yl)-4-chlorophenyl]-4-tert-butylbenzenesulfonamide | 1239784: Antagonist activity at CCR9 receptor (unknown origin) assessed as inhibition of TECK-induced calcium mobilization incubated for 10 mins prior to TECK induction | ic50 | 0.0032 | uM |
| N-[2-(4-aminopyridazin-3-yl)-4-chlorophenyl]-4-tert-butylbenzenesulfonamide | 1239784: Antagonist activity at CCR9 receptor (unknown origin) assessed as inhibition of TECK-induced calcium mobilization incubated for 10 mins prior to TECK induction | ic50 | 0.0038 | uM |
| N-[2-(2-amino-5-hydroxypyrimidin-4-yl)-4-chlorophenyl]-4-tert-butylbenzenesulfonamide | 1239784: Antagonist activity at CCR9 receptor (unknown origin) assessed as inhibition of TECK-induced calcium mobilization incubated for 10 mins prior to TECK induction | ic50 | 0.0040 | uM |
| 4-tert-butyl-N-[7-chloro-2-(2-methoxy-1-oxidopyridin-1-ium-3-yl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0040 | uM |
| 4-tert-butyl-N-[7-chloro-2-(2,6-dimethyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0050 | uM |
| 4-tert-butyl-N-[7-chloro-2-(6-methyl-2-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0050 | uM |
| 4-tert-butyl-N-[7-chloro-2-(2-methyl-1-oxidopyridin-1-ium-3-yl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0060 | uM |
| 4-tert-butyl-N-(7-chloro-1,3-dioxo-2-pyridin-2-ylisoindol-4-yl)benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0060 | uM |
| 4-tert-butyl-N-[7-chloro-2-(3-methyl-4-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0060 | uM |
| 4-tert-butyl-N-[4-chloro-2-(6-ethyl-5-hydroxypyrimidin-4-yl)phenyl]benzenesulfonamide | 1239784: Antagonist activity at CCR9 receptor (unknown origin) assessed as inhibition of TECK-induced calcium mobilization incubated for 10 mins prior to TECK induction | ic50 | 0.0060 | uM |
| 4-tert-butyl-N-[7-chloro-2-[(1-oxidopyridin-1-ium-2-yl)methyl]-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0060 | uM |
| 4-tert-butyl-N-[7-chloro-2-(4-methyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0070 | uM |
| 4-tert-butyl-N-[7-chloro-2-(2-fluoro-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0070 | uM |
| 4-tert-butyl-N-[7-chloro-1,3-dioxo-2-(pyridin-4-ylmethyl)isoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0080 | uM |
| 4-tert-butyl-N-[7-chloro-2-(2,6-dimethoxy-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0080 | uM |
| 1-[(4-tert-butylphenyl)methyl]-6-cyanoindole-2-carboxylic acid | 1306155: Antagonist activity at CCR9 (unknown origin) assessed as inhibition of TECK-stimulated calcium mobilization preincubated for 10 mins followed by agonist addition measured for 90 sec by fluo-8 dye-based FLIPR assay | ic50 | 0.0080 | uM |
| 4-tert-butyl-N-[4-chloro-2-[3-hydroxy-4-(hydroxymethyl)-2-pyridinyl]phenyl]benzenesulfonamide | 1239784: Antagonist activity at CCR9 receptor (unknown origin) assessed as inhibition of TECK-induced calcium mobilization incubated for 10 mins prior to TECK induction | ic50 | 0.0087 | uM |
| 4-tert-butyl-N-[7-chloro-2-(4-ethoxy-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0090 | uM |
| 4-tert-butyl-N-[4-chloro-2-[6-(dimethylamino)-5-hydroxypyrimidin-4-yl]phenyl]benzenesulfonamide | 1239784: Antagonist activity at CCR9 receptor (unknown origin) assessed as inhibition of TECK-induced calcium mobilization incubated for 10 mins prior to TECK induction | ic50 | 0.0090 | uM |
| methyl 3-[(1R)-1-(3,4-difluorophenyl)propyl]-5-(1,2-oxazol-5-yl)-2-sulfanylidene-1H-imidazole-4-carboxylate | 1957049: Inhibition of human CCR9 in recombinant MCP-1-induced calcium mobilization in THP-1 cells | ic50 | 0.0100 | uM |
| 4-tert-butyl-N-[7-chloro-2-(5-fluoro-2-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0100 | uM |
| 4-tert-butyl-N-[7-chloro-2-(2,5-dimethyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0110 | uM |
| 4-tert-butyl-N-(7-chloro-1,3-dioxo-2-pyridin-4-ylisoindol-4-yl)benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0110 | uM |
| 4-tert-butyl-N-[4-chloro-2-(5-hydroxypyrimidin-4-yl)phenyl]benzenesulfonamide | 1239784: Antagonist activity at CCR9 receptor (unknown origin) assessed as inhibition of TECK-induced calcium mobilization incubated for 10 mins prior to TECK induction | ic50 | 0.0110 | uM |
| 4-tert-butyl-N-[4-chloro-2-[5-hydroxy-6-(hydroxymethyl)pyrimidin-4-yl]phenyl]benzenesulfonamide | 1239784: Antagonist activity at CCR9 receptor (unknown origin) assessed as inhibition of TECK-induced calcium mobilization incubated for 10 mins prior to TECK induction | ic50 | 0.0110 | uM |
| 4-tert-butyl-N-[7-chloro-2-[(4-methyl-1-oxidopyridin-1-ium-3-yl)methyl]-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0120 | uM |
| 4-tert-butyl-N-[7-chloro-2-[(1-oxidopyridin-1-ium-3-yl)methyl]-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0130 | uM |
| 4-tert-butyl-N-[7-chloro-2-[(3-fluoro-2-pyridinyl)methyl]-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0130 | uM |
| 4-tert-butyl-N-[7-chloro-2-[(5-methyl-1-oxidopyridin-1-ium-2-yl)methyl]-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0130 | uM |
| 4-tert-butyl-N-[7-chloro-2-(6-methoxy-2-methyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0140 | uM |
| N-[2-(6-amino-5-hydroxypyrimidin-4-yl)-4-chlorophenyl]-4-tert-butylbenzenesulfonamide | 1239784: Antagonist activity at CCR9 receptor (unknown origin) assessed as inhibition of TECK-induced calcium mobilization incubated for 10 mins prior to TECK induction | ic50 | 0.0140 | uM |
| 4-tert-butyl-N-[7-chloro-2-(1-oxidopyridin-1-ium-3-yl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0160 | uM |
| 4-tert-butyl-N-[7-chloro-2-(2-methoxy-5-methyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0160 | uM |
| 4-tert-butyl-N-[7-chloro-2-(5-methoxy-6-methyl-2-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0160 | uM |
| 4-tert-butyl-N-[7-chloro-2-(2-cyano-5-methyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0180 | uM |
| 4-tert-butyl-N-[7-chloro-2-(5-methoxy-4-methyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0180 | uM |
| 4-tert-butyl-N-[7-cyano-1,3-dioxo-2-(pyridin-3-ylmethyl)isoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0190 | uM |
| 4-tert-butyl-N-[7-chloro-2-(6-methyl-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0190 | uM |
| 4-tert-butyl-N-[7-chloro-2-(6-fluoro-3-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0190 | uM |
| 4-tert-butyl-N-[7-chloro-1,3-dioxo-2-(pyridin-2-ylmethyl)isoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0200 | uM |
| 1-[(4-tert-butylphenyl)methyl]-6-chloropyrrolo[3,2-b]pyridine-2-carboxylic acid | 1306155: Antagonist activity at CCR9 (unknown origin) assessed as inhibition of TECK-stimulated calcium mobilization preincubated for 10 mins followed by agonist addition measured for 90 sec by fluo-8 dye-based FLIPR assay | ic50 | 0.0200 | uM |
| 4-tert-butyl-N-[7-chloro-2-(5-methyl-2-pyridinyl)-1,3-dioxoisoindol-4-yl]benzenesulfonamide | 1296738: Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | ki | 0.0210 | uM |
CTD chemical–gene interactions
8 total (human), top 8 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| quercitrin | decreases expression | 1 |
| Amiodarone | increases expression | 1 |
| Benzo(a)pyrene | increases expression | 1 |
| Calcium | affects abundance | 1 |
| Ozone | increases expression | 1 |
| Zinc | increases expression | 1 |
| Aflatoxin B1 | increases methylation | 1 |
| Okadaic Acid | decreases expression | 1 |
ChEMBL screening assays
30 unique, capped per target: 17 binding, 13 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL2184856 | Functional | Antagonist activity at CCR9 assessed as inhibition of CCL25-induced chemotaxis by cell based assay | Chemokine receptor antagonists. — *J Med Chem* |
| CHEMBL2184877 | Binding | Binding affinity to CCR9 | Chemokine receptor antagonists. — *J Med Chem* |
Cellosaurus cell lines
5 cell lines: 3 cancer cell line, 2 spontaneously immortalized cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B8CS | Abcam HCT 116 CCR9 KO | Cancer cell line | Male |
| CVCL_B9F0 | Abcam A-549 CCR9 KO | Cancer cell line | Male |
| CVCL_D2E6 | Abcam MCF-7 CCR9 KO | Cancer cell line | Female |
| CVCL_D2SF | CHO/hCCR9 | Spontaneously immortalized cell line | Female |
| CVCL_KW63 | PathHunter CHO-K1 CCR9 beta-arrestin | Spontaneously immortalized cell line | Female |
Clinical trials (associated diseases)
Via MONDO — disease-level, not drug-specific.
50 trials:
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT02343562 | Phase 4 | UNKNOWN | Probiotics for Prophylaxis of Postoperative Hirschsprungs Associated Enterocolitis |
| NCT07186647 | Phase 4 | COMPLETED | Laparoscopic-Assisted Transanal Pull-Through for Hirschsprung Disease in Pediatric:Short and Intermediate Outcomes of Two Different Techniques |
| NCT04904081 | Phase 3 | UNKNOWN | Feasibility of Use of Indocyanine Green in Pediatric Colorectal Surgery |
| NCT00630838 | Phase 2 | COMPLETED | Probiotic Prophylaxis of Hirschprung’s Disease Associated Enterocolitis (HAEC) |
| NCT01985646 | Early Phase 1 | COMPLETED | A Trial on Conservative Treatment for Infants’ Hirschsprung Disease |
| NCT00478712 | Not specified | RECRUITING | Hirschsprung Disease Genetic Study |
| NCT01515501 | Not specified | COMPLETED | Endoscopic Mucosal Resection for the Diagnosis of a-Ganglionosis, a Controlled Prospective Trial (EDGE Trial) |
| NCT01793168 | Not specified | RECRUITING | Rare Disease Patient Registry & Natural History Study - Coordination of Rare Diseases at Sanford |
| NCT01927809 | Not specified | UNKNOWN | Genetic Mosaicism in Hirschsprung’s Disease |
| NCT02193685 | Not specified | UNKNOWN | Identification Genetic, Immunologic and Microbial Markers of Hirschsprung Associated Enterocolitis in Children With Hirschsprung Disease |
| NCT02216994 | Not specified | UNKNOWN | A New Scoring System Improves Diagnostic Accuracy of Intestinal Dysganglionosis –a Prospective Study |
| NCT02296008 | Not specified | COMPLETED | 3D High Resolution Anorectal Manometry in Children After Surgery for Anorectal Disorders |
| NCT02776176 | Not specified | UNKNOWN | Enhanced Recovery After Surgery In Hirschsprung Disease |
| NCT02857205 | Not specified | COMPLETED | MICROPRUNG : Intestinal Microbiota Analysis in Patients With or Without Hirschsprung’s Associated EnteroColitis |
| NCT03269812 | Not specified | UNKNOWN | Laparoscopic Assisted Pull-through Versus Other Surgical Procedures for Treatment of Hirschsprung Disease |
| NCT03666767 | Not specified | COMPLETED | Management and Outcomes of Congenital Anomalies in Low-, Middle- and High-Income Countries |
| NCT04020939 | Not specified | COMPLETED | The Role of Indocyanine Green Angiography Fluorescence on Intestinal Resections in Pediatric Surgery. |
| NCT04106947 | Not specified | UNKNOWN | Transition of Care for Patients With Hirschsprung Disease and Anorectal Malformations |
| NCT04149093 | Not specified | UNKNOWN | The Association Between Calretinin and the Function of Ganglion Cells in Hirschsprung Disease |
| NCT04150120 | Not specified | COMPLETED | eHealth as an Aid for Facilitating and Supporting Self-management in Families With Long-term Childhood Illness |
| NCT04213976 | Not specified | UNKNOWN | Ostomy in Continuity or Conventional Ileostomy: a Retrospective Multicentric Analysis |
| NCT04476225 | Not specified | COMPLETED | Induced Pluripotent Stem Cells for Disease Research |
| NCT04598841 | Not specified | COMPLETED | Nutrition Support for Hirschsprung Disease |
| NCT04622410 | Not specified | RECRUITING | Registry for Hirschsprung Disease of the BELAPS |
| NCT04624334 | Not specified | TERMINATED | Non-invasive Assessment of Colonic Motility |
| NCT04730128 | Not specified | COMPLETED | Translation and Validation of a Disease-specific Questionnaire for Hirschsprung’s Disease in Danish Patients |
| NCT04837963 | Not specified | COMPLETED | Does Hirschsprung Disease Increase the Risk of Febrile Urinary Tract Infection in Children |
| NCT04957667 | Not specified | COMPLETED | Scintigraphic Defecography for Evaluation of Functional Outcome in an Adult Hirschsprung Population |
| NCT05038345 | Not specified | TERMINATED | Hirschsprung Disease Trends in the United States: Analysis of the National Inpatient Sample |
| NCT05044741 | Not specified | COMPLETED | Risk Factors of Perforated HSCR in Neonates |
| NCT05293353 | Not specified | UNKNOWN | Neokare Safety and Tolerability Assessment in Neonates With GI Problems |
| NCT05307419 | Not specified | UNKNOWN | Full Thickness vs. Rectal Suction Biopsy in the Diagnosis of Hirschsprungs Disease |
| NCT05450991 | Not specified | RECRUITING | Long-term Qualitative and Quantitative Outcomes of Children With Hirschsprung’s Disease and Anorectal Malformations |
| NCT05655845 | Not specified | UNKNOWN | Risk Factors for Bowel Dysfunction at Preschool and Early Childhood Age in Children With Hirschsprung Disease |
| NCT06072976 | Not specified | RECRUITING | The Influence of Feeding Source on the Gut Microbiome and Time to Full Feeds in Neonates With Congenital Gastrointestinal Pathologies |
| NCT06197061 | Not specified | UNKNOWN | Comparison of Robot-assisted With Laparoscopic-assisted Modified Soave Procedure for Classical Hirschsprung Disease |
| NCT06573723 | Not specified | RECRUITING | Institutional Registry of Rare Diseases |
| NCT06590142 | Not specified | RECRUITING | Hirschsprung’s Advances; Working Towards Autologous tIssue therapIes |
| NCT06592534 | Not specified | NOT_YET_RECRUITING | Babies With Enterocolitis - A Study of Faecal Calprotectin in Hirschsprung Disease (The BEACH Study) |
| NCT06650683 | Not specified | RECRUITING | Impact of Providing Nursing Support on Parental Stress Related to Preoperative Care of a Newborn with Hirschsprung’s Disease |
| NCT06874686 | Not specified | COMPLETED | Minimally Invasive Surgical Intervention for Hirschsprung’s Disease in Pediatric Patients |
| NCT06880666 | Not specified | COMPLETED | Minimally Invasive Surgical Intervention for Hirschsprung Disease |
| NCT07098494 | Not specified | COMPLETED | Probiotics and Post-Pullthrough Hirschsprung’s Disease-Associated Enterocolitis |
| NCT07156981 | Not specified | NOT_YET_RECRUITING | Effects of Physiotherapy in Children With Hirschsprung’s Disease |
| NCT07343622 | Not specified | NOT_YET_RECRUITING | Robot/Laparoscopic-Assisted Transanal Transection Duhamel Versus Modified Soave Pull-Through for TCA |
| NCT07468565 | Not specified | NOT_YET_RECRUITING | Surgical Approach for the Treatment of Hirschsprung Disease Using the Swenson Technique (SMILES) |
| NCT07519915 | Not specified | RECRUITING | Improvement of Understanding of Pediatric Sacral Neuromodulation: Therapeutic Strategies and Outcome Variables |
| NCT07526636 | Not specified | NOT_YET_RECRUITING | Pattern And Outcome Of Neonatal Gastrointestinal Emergencies In Assiut University Children Hospital |
| NCT07742436 | Not specified | NOT_YET_RECRUITING | Urinary and Sexual Symptoms in Patients With Hirschsprung Disease |
| NCT07789782 | Not specified | NOT_YET_RECRUITING | Comparison of a New Non-invasive Device With the Invasive Gold-standard Investigation to Assess Function of the Large Bowel in Children |
Predicted chemistry — Sugi Predict
The predicted patent-compound landscape for CCR9 across ~30M SureChEMBL compounds — explore on Sugi Predict.
Related Atlas pages
- Targeted by drugs: Vercirnon
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): Hirschsprung disease, susceptibility to, 1