CCR5

Summary

CCR5 (C-C motif chemokine receptor 5, HGNC:1606) is a protein-coding gene on chromosome 3p21.31, encoding C-C chemokine receptor type 5 (P51681). Receptor for a number of inflammatory CC-chemokines including CCL3/MIP-1-alpha, CCL4/MIP-1-beta and RANTES and subsequently transduces a signal by increasing the intracellular calcium ion level.

This gene encodes a member of the beta chemokine receptor family, which is predicted to be a seven transmembrane protein similar to G protein-coupled receptors. This protein is expressed by T cells and macrophages, and is known to be an important co-receptor for macrophage-tropic virus, including HIV, to enter host cells. Defective alleles of this gene have been associated with the HIV infection resistance. The ligands of this receptor include monocyte chemoattractant protein 2 (MCP-2), macrophage inflammatory protein 1 alpha (MIP-1 alpha), macrophage inflammatory protein 1 beta (MIP-1 beta) and regulated on activation normal T expressed and secreted protein (RANTES). Expression of this gene was also detected in a promyeloblastic cell line, suggesting that this protein may play a role in granulocyte lineage proliferation and differentiation. This gene is located at the chemokine receptor gene cluster region. An allelic polymorphism in this gene results in both functional and non-functional alleles; the reference genome represents the functional allele. Two transcript variants encoding the same protein have been found for this gene.

Source: NCBI Gene 1234 — RefSeq curated summary.

At a glance

• GWAS associations: 9
• Clinical variants (ClinVar): 46 total
• GTEx eGene: eQTL in 16 tissues, sQTL in 0 (q < 0.05)
• Drug target: yes — 12 curated mechanism-of-action drugs; 15 molecules with ChEMBL bioactivity (top 2% of genes corpus-wide)
• Approved drugs (ChEMBL mechanism of action): 1 — Maraviroc
• Constraint (gnomAD): pLI 0.18 (intermediate), LOEUF 1.59 (unconstrained)
• MANE Select transcript: NM_001394783
• Interaction hub: 3,150 STRING partners (top 2% of genes corpus-wide)

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:1606
Approved symbol	CCR5
Name	C-C motif chemokine receptor 5
Location	3p21.31
Locus type	gene with protein product
Status	Approved
Aliases	CKR-5, CC-CKR-5, CKR5, CD195, IDDM22
Ensembl gene	ENSG00000160791
Ensembl biotype	protein_coding
OMIM	601373
Entrez	1234

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 3 protein_coding

MANE Select: ENST00000292303

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 1

ENST00000292303, ENST00000445772, ENST00001142998

RefSeq mRNA: 3 — MANE Select: NM_001394783 NM_000579, NM_001100168, NM_001394783

CCDS: CCDS2739

Canonical transcript exons

ENST00000292303 — 2 exons

Exon	Start	End
ENSE00001054508	46372892	46376206
ENSE00001078626	46370946	46370988

Expression profiles

Bgee: expression breadth ubiquitous, 194 present calls, max score 89.38.

FANTOM5 (CAGE): breadth broad, TPM avg 6.3603 / max 277.3082, expressed in 355 samples.

Highest expression (Bgee): type B pancreatic cell, olfactory bulb, epithelium of nasopharynx, nasopharynx, diaphragm.

Genetic regulation across tissues (GTEx eQTL / sQTL)

CCR5 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 16 tissues and its splicing (sQTL) in 0 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

16 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Whole Blood	eqtl	2.0e-08	-0.24	3:46318831:T:C
Colon Sigmoid	eqtl	5.8e-04	-0.40	3:46154389:A:G
Skin Sun Exposed Lower leg	eqtl	8.4e-04	+0.17	3:46235387:T:A
Lung	eqtl	9.1e-04	-0.15	3:46439310:A:G
Brain Hippocampus	eqtl	3.4e-03	-0.26	3:46369003:A:C
Adipose Visceral Omentum	eqtl	6.4e-03	-0.17	3:46304382:C:G
Prostate	eqtl	1.4e-02	+0.23	3:46309225:T:C
Stomach	eqtl	1.5e-02	-0.24	3:46098510:A:G
Nerve Tibial	eqtl	1.7e-02	-0.12	3:46406413:G:A
Adipose Subcutaneous	eqtl	2.4e-02	-0.20	3:46220620:C:T
Brain Nucleus accumbens basal ganglia	eqtl	2.6e-02	+0.20	3:46418602:C:T
Brain Substantia nigra	eqtl	2.8e-02	-0.23	3:46408579:T:A
Breast Mammary Tissue	eqtl	2.9e-02	-0.16	3:46417999:C:T
Skin Not Sun Exposed Suprapubic	eqtl	3.7e-02	+0.15	3:46247622:G:A
Esophagus Muscularis	eqtl	3.9e-02	-0.21	3:46175405:G:C
Esophagus Mucosa	eqtl	4.2e-02	-0.29	3:46747140:A:C

FANTOM5 promoters

2 alternative TSS:

Promoter ID	TPM avg	Samples expressed
36451	4.6010	327
36450	1.7592	253

Top tissues by expression

showing 100 of 282 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
type B pancreatic cell	CL:0000169	89.38	gold quality
olfactory bulb	UBERON:0002264	89.07	gold quality
epithelium of nasopharynx	UBERON:0001951	87.90	gold quality
nasopharynx	UBERON:0001728	87.89	gold quality
diaphragm	UBERON:0001103	87.25	gold quality
parietal pleura	UBERON:0002400	85.81	gold quality
pleura	UBERON:0000977	85.74	gold quality
visceral pleura	UBERON:0002401	85.28	gold quality
palpebral conjunctiva	UBERON:0001812	84.50	gold quality
granulocyte	CL:0000094	84.48	gold quality
germinal epithelium of ovary	UBERON:0001304	83.66	gold quality
mucosa of urinary bladder	UBERON:0001259	83.58	silver quality
vermiform appendix	UBERON:0001154	83.43	gold quality
superficial temporal artery	UBERON:0001614	82.00	gold quality
jejunal mucosa	UBERON:0000399	81.66	gold quality
lymph node	UBERON:0000029	81.43	gold quality
leukocyte	CL:0000738	80.23	gold quality
left ventricle myocardium	UBERON:0006566	80.17	gold quality
caecum	UBERON:0001153	79.85	gold quality
decidua	UBERON:0002450	79.82	gold quality
mononuclear cell	CL:0000842	79.54	gold quality
monocyte	CL:0000576	79.25	gold quality
epithelial cell of pancreas	CL:0000083	78.61	silver quality
amniotic fluid	UBERON:0000173	78.58	gold quality
oral cavity	UBERON:0000167	78.45	gold quality
cardiac muscle of right atrium	UBERON:0003379	78.31	gold quality
blood	UBERON:0000178	78.19	gold quality
eye	UBERON:0000970	77.96	gold quality
myocardium	UBERON:0002349	77.27	gold quality
colonic epithelium	UBERON:0000397	76.61	gold quality
gall bladder	UBERON:0002110	75.21	gold quality
esophagus squamous epithelium	UBERON:0006920	74.96	gold quality
spleen	UBERON:0002106	74.38	gold quality
ileal mucosa	UBERON:0000331	74.07	silver quality
thymus	UBERON:0002370	73.93	silver quality
squamous epithelium	UBERON:0006914	73.58	silver quality
mucosa of sigmoid colon	UBERON:0004993	73.14	gold quality
smooth muscle tissue	UBERON:0001135	72.95	gold quality
duodenum	UBERON:0002114	72.73	gold quality
rectum	UBERON:0001052	72.61	gold quality
mucosa of paranasal sinus	UBERON:0005030	72.03	silver quality
jejunum	UBERON:0002115	71.81	gold quality
colonic mucosa	UBERON:0000317	71.71	gold quality
epithelium of esophagus	UBERON:0001976	71.44	silver quality
bone marrow cell	CL:0002092	71.29	silver quality
gingiva	UBERON:0001828	70.91	silver quality
gingival epithelium	UBERON:0001949	70.75	gold quality
cervix squamous epithelium	UBERON:0006922	70.18	gold quality
tonsil	UBERON:0002372	70.00	gold quality
bone marrow	UBERON:0002371	69.82	gold quality
nasal cavity epithelium	UBERON:0005384	69.50	silver quality
cardia of stomach	UBERON:0001162	69.48	gold quality
vastus lateralis	UBERON:0001379	69.20	gold quality
lung	UBERON:0002048	69.07	gold quality
mammary duct	UBERON:0001765	68.90	silver quality
quadriceps femoris	UBERON:0001377	68.74	gold quality
epithelium of bronchus	UBERON:0002031	68.62	silver quality
bronchus	UBERON:0002185	68.46	silver quality
epithelium of mammary gland	UBERON:0003244	68.46	silver quality
mammalian vulva	UBERON:0000997	67.81	gold quality
tibia	UBERON:0000979	67.69	silver quality
cervix epithelium	UBERON:0004801	67.69	silver quality
right coronary artery	UBERON:0001625	67.52	gold quality
tongue squamous epithelium	UBERON:0006919	67.36	gold quality
urinary bladder	UBERON:0001255	67.07	gold quality
bronchial epithelial cell	CL:0002328	66.48	silver quality
small intestine	UBERON:0002108	66.24	gold quality
upper lobe of lung	UBERON:0008948	65.78	gold quality
trachea	UBERON:0003126	65.74	gold quality
upper lobe of left lung	UBERON:0008952	65.73	gold quality
skin of hip	UBERON:0001554	65.43	silver quality
small intestine Peyer’s patch	UBERON:0003454	65.35	gold quality
endometrium	UBERON:0001295	65.24	gold quality
layer of synovial tissue	UBERON:0007616	65.04	silver quality
pylorus	UBERON:0001166	64.98	gold quality
thoracic mammary gland	UBERON:0005200	64.96	gold quality
mammary gland	UBERON:0001911	64.88	gold quality
nephron tubule	UBERON:0001231	64.58	gold quality
caput epididymis	UBERON:0004358	64.39	gold quality
dorsal plus ventral thalamus	UBERON:0001897	64.31	gold quality
cauda epididymis	UBERON:0004360	64.24	silver quality
CA1 field of hippocampus	UBERON:0003881	64.12	gold quality
corpus epididymis	UBERON:0004359	64.12	silver quality
trabecular bone tissue	UBERON:0002483	63.81	silver quality
tongue	UBERON:0001723	63.53	silver quality
hair follicle	UBERON:0002073	63.49	gold quality
metanephric glomerulus	UBERON:0004736	63.44	gold quality
trigeminal ganglion	UBERON:0001675	63.37	silver quality
body of tongue	UBERON:0011876	63.37	gold quality
superior surface of tongue	UBERON:0007371	63.35	silver quality
cranial nerve II	UBERON:0000941	63.32	silver quality
nasal cavity mucosa	UBERON:0001826	63.31	gold quality
kidney epithelium	UBERON:0004819	63.21	gold quality
mucosa of transverse colon	UBERON:0004991	63.20	gold quality
placenta	UBERON:0001987	63.08	gold quality
saphenous vein	UBERON:0007318	62.97	gold quality
fallopian tube	UBERON:0003889	62.78	gold quality
ventral tegmental area	UBERON:0002691	62.74	gold quality
pharyngeal mucosa	UBERON:0000355	62.54	gold quality
gluteal muscle	UBERON:0002000	62.48	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	4.72

HPA expression

RNA tissue specificity: Tissue enhanced

showing 60 of 73 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM
Appendix	tissue	14.5
Lymph node	tissue	13.8
Spinal cord	tissue	13.4
Substantia nigra	tissue	12.5
Hypothalamus	tissue	11.6
Medulla oblongata	tissue	11.1
Periaqueductal gray	tissue	11.1
Corpus callosum	tissue	11.0
Midbrain	tissue	10.0
Pons	tissue	9.7
Septum	tissue	9.4
Spleen	tissue	9.1
Tonsil	tissue	9.1
Thalamus	tissue	8.3
Putamen	tissue	7.8
Superior colliculi	tissue	7.6
Lung	tissue	7.1
Ventral pallidum	tissue	6.9
Stomach 1	tissue	6.6
Amygdala	tissue	6.5
Hippocampal formation	tissue	6.5
Small intestine	tissue	5.7
Basal ganglia	tissue	5.2
Gallbladder	tissue	4.8
Urinary bladder	tissue	4.6
Entorhinal cortex	tissue	4.4
Olfactory bulb	tissue	4.2
Cerebral cortex	tissue	4.0
Motor cortex	tissue	4.0
Duodenum	tissue	4.0
Thymus	tissue	4.0
Temporal cortex	tissue	3.9
Prefrontal cortex	tissue	3.8
Rectum	tissue	3.8
Insular cortex	tissue	3.7
Retrosplenial cortex	tissue	3.6
Colon	tissue	3.2
Liver	tissue	3.2
Smooth muscle	tissue	3.1
Cingulate cortex	tissue	3.1
Somatosensory cortex	tissue	3.0
Occipital cortex	tissue	2.9
Salivary gland	tissue	2.8
Breast	tissue	2.4
Cervix	tissue	2.0
Adrenal gland	tissue	1.9
Choroid plexus	tissue	1.8
Prostate	tissue	1.8
Adipose tissue	tissue	1.7
Fallopian tube	tissue	1.6
Esophagus	tissue	1.4
Endometrium 1	tissue	1.4
Bone marrow	tissue	1.3
Cerebellum	tissue	1.2
Skin 1	tissue	1.1
Heart muscle	tissue	1.0
Seminal vesicle	tissue	1.0
Kidney	tissue	1.0
Ovary	tissue	0.9
Epididymis	tissue	0.9

Brain sub-regions (HPA Brain Atlas): detected in 183; highest nTPM — Dorsal spinal cord (13.4), Ventral spinal cord (12.4), White matter (11.0), Dorsal hippocampus (6.5), Subiculum (5.9).

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AP1, CEBPB, CREB1, EGR1, FOS, GATA1, GATA3, HAND1, IRF1, JUN, KLF2, MYC, NFKB1, NR3C2, POU2F2, RELA, STAT1, STAT3, TRERF1, YY1

miRNA regulators (miRDB)

Targeting CCR5 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-5193	100.00	67.26	1744
HSA-MIR-7110-3P	100.00	73.18	2486
HSA-MIR-6759-5P	99.99	66.54	785
HSA-MIR-6793-5P	99.97	65.95	758
HSA-MIR-1229-3P	99.97	66.49	906
HSA-MIR-493-5P	99.96	72.47	2382
HSA-MIR-4778-3P	99.93	70.40	1818
HSA-MIR-335-3P	99.93	73.36	4958
HSA-MIR-345-3P	99.89	70.23	1421
HSA-MIR-629-3P	99.85	67.99	1875
HSA-MIR-636	99.80	69.58	1500
HSA-MIR-6817-3P	99.79	68.35	2126
HSA-MIR-4694-3P	99.79	69.53	2640
HSA-MIR-4713-5P	99.78	67.80	1794
HSA-MIR-498-5P	99.76	69.64	1807
HSA-MIR-4319	99.76	69.83	2586
HSA-MIR-8084	99.73	69.57	1760
HSA-MIR-4524A-3P	99.72	66.85	2406
HSA-MIR-670-5P	99.67	69.94	1565
HSA-MIR-3175	99.65	66.30	2031
HSA-MIR-182-3P	99.57	67.57	825
HSA-MIR-4276	99.56	67.66	2514
HSA-MIR-12123	99.52	71.79	2990
HSA-MIR-5007-3P	99.51	68.14	1242
HSA-MIR-203A-3P	99.49	70.56	2806
HSA-MIR-125B-5P	99.36	70.36	1662
HSA-MIR-125A-5P	99.36	70.59	1640
HSA-MIR-4312	99.34	67.30	511
HSA-MIR-7515	99.31	68.22	1795
HSA-MIR-6731-5P	99.28	67.42	2375

Functional genomics

gnomAD constraint: pLI 0.181, LOEUF 1.59, missense Z -0.388 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000292303 — one region, missense o/e 1.10.

Literature-anchored findings (GeneRIF, showing 40)

• Biological characterization and chemokine receptor usage of HIV type 1 isolates prevalent in Brazil. (PMID:11559423)
• differences in primary structural requirements for RANTES, MIP-1 alpha, and vMIP-II binding (PMID:11700073)
• Association of CCR5 genotype with disease progression of HIV infection (PMID:11709782)
• Effect of cocaine on chemokine and CCR-5 gene expression by mononuclear cells from normal donors and HIV-1 infected patients. (PMID:11727771)
• Up-regulation on distinct subpopulations of antigen-activated CD4+ T lymphocytes (PMID:11751947)
• genotypes and their relative contribution to human immunodeficiency virus type 1 (HIV-1) seroconversion, early HIV-1 RNA concentration in plasma, and later disease progression (PMID:11752157)
• CC chemokine receptor 5 (CCR5) mRNA expression in pulmonary sarcoidosis (PMID:11803051)
• results support the conclusion that the CCR5-Delta32/Delta32 genotype mediated resistance is incomplete and is associated with acquisition of exclusively-X4 variants of HIV-1 (PMID:11873082)
• CXCR-4 was constitutively expressed by thymocytes and it mediated polarization, migration and intercellular CA2+ increase in response to SDF-1. (PMID:11876757)
• the role of CD4, CXCR4, and CCR5 in HIV envelope-mediated apoptosis was examined in peripheral blood mononuclear cells (PMID:11878912)
• cytokine regulation of CCR5 expression on monocytes, monocyte-derived macrophages (MDMs), and microglia was investigated (PMID:11920312)
• Lipopolysaccharide,lipoarabinomannan and lipoteichoic acid down-regulated the expression of CXCR4 and CCR5 on monocytes (PMID:11920324)
• Results identified specific regions in CCR5 that confer HIV-1 coreceptor function, structural rearrangements in the transmembrane region that may modulate this activity, and a role for the extracellular surface in folding and assembly. (PMID:11937056)
• Graves’ disease is associated with an altered CCR5 expression in thyroid-derived compared to peripheral blood t lymphocytes (PMID:11966764)
• Elevated expression of CCR5 by myeloid (CD11c+) blood dendritic cells in multiple sclerosis and acute optic neuritis (PMID:11966770)
• High level expression of CCR5 is a characteristic and selective feature of circulating V delta 2 gamma delta T cells, which is in line with their suspected function as Th1 effector T cells. (PMID:11994442)
• CCR5 and CXCR4 are present on the resident testicular macrophages in the interstitial space but not in the germ cell line (PMID:11994538)
• Cholesterol is essential for macrophage inflammatory protein 1 beta binding and signaling and conformational integrity of CC chemokine receptor 5. (PMID:12036855)
• Frequency of the HIV-protective CC chemokine receptor 5-Delta32/Delta32 genotype is increased in hepatitis C. (PMID:12055576)
• decreased density of the CCR5 receptor on the surface of CD4+ lymphocytes and monocytes/macrophages is associated with the CCR5-59653T transition in the promoter region (PMID:12056598)
• Most Natural killer t-cells express receptors for extralymphoid tissue or inflammation-related chemokines (CCR2, CCR5, and CXCR3), while few NKT cells express lymphoid tissue-homing chemokine receptors (CCR7 and CXCR5). (PMID:12070001)
• chronic hepatitis C, but not hepatitis B, infection alters surface expression of CCR1 and CCR5 in T cells, resulting in lower CC chemokine responsiveness. (PMID:12085329)
• Caco-2 and M cells do not express CCR5, but transfection of these cells with CCR5 cDNA restores transport of R5 virus, which demonstrates that HIV-1 transport across M cells is receptor-mediated. (PMID:12093918)
• CCR5 mediates Fas- and caspase-8 dependent apoptosis of both uninfected and HIV infected primary human CD4 T cells (PMID:12131184)
• Data show that two distinct forms of CCR5 protein, 62 and 42k Da, are present in lymphocytic cells. (PMID:12163044)
• tyrosine sulfastion of n-terminal peptide follows a discrete pattern and temporal sequence (PMID:12169668)
• expression detected in a stromal cell line, a myeloma cell line, and primary multiple myeloma cells and may be target for MIP1A and MIP1B. (PMID:12200385)
• prevalence of CCR5-Delta32 allele frequency in a large Pakistani population sample representing 10 ethnic groups (PMID:12215252)
• Binding chemokines modulate CXCL12 (SDF-1)-induced responses of progenitor B cells in human bone marrow through heterologous desensitization of the CXCR4 chemokine receptor (PMID:12239139)
• P. falciparum antigens (PF-Ags) variably regulate the expression of HIV-1 coreceptors and modulate the infectability of CD4 cells by HIV-1 (PMID:12355376)
• Significant increase in surface CCR5 in CD4+, CD8+, CD19+ and CD14+ cells as well as an increased percentage of CXCR3 and CXCR4 in CD14+ cells in MS patients. (PMID:12356205)
• role of IL-12 and IFN-gamma on inducing inflammatory chemokine secretion and down-regulating CCR5 expression in human T cells (PMID:12377943)
• influence of the major CCR5 promoter or coding region variants as haplotypes and genotypes in a cohort of 250 chronically infected HCV patients (PMID:12403355)
• CCR5 is phosphorylated at specific sites by protein kinase C and GPCR kinase (PMID:12403770)
• These results suggest that oligomerization of chemokine receptor CCR5 and opioid receptors mu, delta and kappa on the cell membrane of human or monkey lymphocytes may modulate receptor functions. (PMID:12413885)
• chemokine receptor CCR5 deletion mutation is associated with multiple sclerosis in HLA-DR4-positive Russians (PMID:12451219)
• META-ANALYSIS: Effect of CCR5-delta32 heterozygosity on the risk of perinatal HIV-1 infection (PMID:12514416)
• An increase in the numbers of CCR5(+) cells in H. pylori-infected stomach mucosa suggests that this molecule may play an important role in gastric immune responses. (PMID:12522035)
• physical association of CD4 and CCR5 results in receptor cross-talk with allosteric CD4-dependent regulation of the binding and signaling properties of CCR5 (PMID:12531905)
• Limited protective effect of the CCR5Delta32/CCR5Delta32 genotype on human immunodeficiency virus infection incidence in a cohort of patients with hemophilia and selection for genotypic X4 virus (PMID:12552446)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	ccr11.1	ENSDARG00000070755
danio_rerio	ccr2	ENSDARG00000079829
danio_rerio	si:ch211-207g17.3	ENSDARG00000105363
mus_musculus	Ccr5	ENSMUSG00000079227
rattus_norvegicus	Ccr5	ENSRNOG00000049115

Paralogs (23): CCR6 (ENSG00000112486), CCRL2 (ENSG00000121797), CCR2 (ENSG00000121807), CXCR4 (ENSG00000121966), CCR7 (ENSG00000126353), ACKR4 (ENSG00000129048), ACKR3 (ENSG00000144476), ACKR2 (ENSG00000144648), RGR (ENSG00000148604), CXCR5 (ENSG00000160683), CXCR1 (ENSG00000163464), CCR1 (ENSG00000163823), CX3CR1 (ENSG00000168329), CXCR6 (ENSG00000172215), XCR1 (ENSG00000173578), CCR9 (ENSG00000173585), CCR8 (ENSG00000179934), CXCR2 (ENSG00000180871), GALR2 (ENSG00000182687), CCR3 (ENSG00000183625), CCR4 (ENSG00000183813), CCR10 (ENSG00000184451), CXCR3 (ENSG00000186810)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:107182) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 50 distinct phenotype terms.

Mouse phenotype (MP)	Records
impaired macrophage chemotaxis	3
abnormal response to cardiac infarction	1
decreased metastatic potential	1
abnormal locomotor behavior	1
abnormal spatial learning	1
abnormal cardiovascular system physiology	1
decreased inflammatory response	1
increased susceptibility to bacterial infection	1
abnormal CD4-positive, alpha beta T cell morphology	1
abnormal leukocyte physiology	1
abnormal conditioned taste aversion behavior	1
abnormal cytokine secretion	1
liver failure	1
increased alcohol consumption	1
abnormal leukocyte adhesion	1
abnormal nervous system physiology	1
abnormal glial cell physiology	1
increased length of allograft survival	1
abnormal CD8-positive, alpha beta T cell morphology	1
decreased T cell proliferation	1
decreased susceptibility to injury	1
increased susceptibility to fungal infection	1
abnormal heart size	1
cornea vascularization	1
increased susceptibility to type IV hypersensitivity reaction	1

+25 more (showing top 25).

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
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
Cercocebus galeritus	Q9TV49	99.7%	Diamond
Pygathrix nemaeus	O97882	99.4%	Diamond
Nomascus leucogenys	O97883	99.4%	Diamond
Chlorocebus aethiops	P56493	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
Chlorocebus sabaeus	Q9TV43	99.1%	Diamond
Cercopithecus cephus	Q9TV47	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
CCR5AS	ncRNA	102724297
CCR1	protein-coding	1230
CCR3	protein-coding	1232
CCR2	protein-coding	729230
LINC02009	ncRNA	105377068
CCRL2	protein-coding	9034
LTF	protein-coding	4057
RTP3	protein-coding	83597

Protein

Protein identifiers

C-C chemokine receptor type 5 — P51681 (reviewed: P51681)

Alternative names: CHEMR13, HIV-1 fusion coreceptor

All UniProt accessions (2): P51681, Q38L21

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for a number of inflammatory CC-chemokines including CCL3/MIP-1-alpha, CCL4/MIP-1-beta and RANTES and subsequently transduces a signal by increasing the intracellular calcium ion level. May play a role in the control of granulocytic lineage proliferation or differentiation. Participates in T-lymphocyte migration to the infection site by acting as a chemotactic receptor. (Microbial infection) Acts as a coreceptor (CD4 being the primary receptor) of human immunodeficiency virus-1/HIV-1.

Subunit / interactions. Interacts with PRAF2. Efficient ligand binding to CCL3/MIP-1alpha and CCL4/MIP-1beta requires sulfation, O-glycosylation and sialic acid modifications. Glycosylation on Ser-6 is required for efficient binding of CCL4. Interacts with GRK2. Interacts with ARRB1 and ARRB2. Interacts with CNIH4. Interacts with S100A4; this interaction stimulates T-lymphocyte chemotaxis. (Microbial infection) Interacts with HIV-1 surface protein gp120. (Microbial infection) May interact with human cytomegalovirus/HHV-5 protein UL78. (Microbial infection) Interacts with Kaposi virus protein vCCL2.

Subcellular location. Cell membrane.

Tissue specificity. Highly expressed in spleen, thymus, in the myeloid cell line THP-1, in the promyeloblastic cell line KG-1a and on CD4+ and CD8+ T-cells. Medium levels in peripheral blood leukocytes and in small intestine. Low levels in ovary and lung.

Post-translational modifications. Sulfated on at least 2 of the N-terminal tyrosines. Sulfation contributes to the efficiency of HIV-1 entry and is required for efficient binding of the chemokines, CCL3 and CCL4. O-glycosylated, but not N-glycosylated. Ser-6 appears to be the major site even if Ser-7 may be also O-glycosylated. Also sialylated glycans present which contribute to chemokine binding. Thr-16 and Ser-17 may also be glycosylated and, if so, with small moieties such as a T-antigen. Palmitoylation in the C-terminal is important for cell surface expression, and to a lesser extent, for HIV entry. Phosphorylation on serine residues in the C-terminal is stimulated by binding CC chemokines especially by APO-RANTES.

Disease relevance. Type 1 diabetes mellitus 22 (T1D22) [MIM:612522] A multifactorial disorder of glucose homeostasis that is characterized by susceptibility to ketoacidosis in the absence of insulin therapy. Clinical features are polydipsia, polyphagia and polyuria which result from hyperglycemia-induced osmotic diuresis and secondary thirst. These derangements result in long-term complications that affect the eyes, kidneys, nerves, and blood vessels. Disease susceptibility is associated with variants affecting the gene represented in this entry.

Induction. (Microbial infection) May be down-regulated by human cytomegalovirus/HHV-5 protein UL78.

Polymorphism. Variations in CCR5 are associated with resistance or susceptibility to immunodeficiency virus type 1 (resistance or susceptibility to HIV-1) [MIM:609423]. Variations in CCR5 gene also influence the rate of progression to AIDS after infection. Variations in CCR5 are associated with susceptibility to West Nile virus (WNV) infection [MIM:610379].

Similarity. Belongs to the G protein-coupled receptor 1 family.

RefSeq proteins (3): NP_000570, NP_001093638, NP_001381712* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000355	Chemokine_rcpt	Family
IPR002240	Chemokine_CCR5	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain
IPR050119	CCR1-9-like	Family

Pfam: PF00001

UniProt features (113 total): sequence variant 38, mutagenesis site 22, helix 16, topological domain 8, modified residue 8, transmembrane region 7, strand 3, turn 3, lipid moiety-binding region 3, glycosylation site 2, disulfide bond 2, chain 1

Structure

Experimental structures (PDB)

26 structures by resolution:

PDB	Title	Method	Resolution (Å)
5YD3	Crystal structure of the scFv antibody 4B08 with epitope peptide	X-RAY DIFFRACTION	1.35
5YD4	Crystal structure of the scFv antibody 4B08 with epitope peptide (mutation T6A)	X-RAY DIFFRACTION	1.35
5YY4	Crystal structure of the scFv antibody 4B08 with sulfated epitope peptide	X-RAY DIFFRACTION	1.59
9J8A	Structure of antibody BA8 in complex with sulfated peptide from CCR5	X-RAY DIFFRACTION	1.75
5YD5	Crystal structure of the scFv antibody 4B08 with epitope peptide (mutation N3A)	X-RAY DIFFRACTION	1.96
5UIW	Crystal Structure of CC Chemokine Receptor 5 (CCR5) in complex with high potency HIV …	X-RAY DIFFRACTION	2.2
7F1T	Crystal structure of the human chemokine receptor CCR5 in complex with MIP-1a	X-RAY DIFFRACTION	2.6
4MBS	Crystal Structure of the CCR5 Chemokine Receptor	X-RAY DIFFRACTION	2.71
6AKX	The Crystal structure of Human Chemokine Receptor CCR5 in complex with compound 21	X-RAY DIFFRACTION	2.8
6AKY	The Crystal structure of Human Chemokine Receptor CCR5 in complex with compound 34	X-RAY DIFFRACTION	2.8
7F1S	Cryo-EM structure of the apo chemokine receptor CCR5 in complex with Gi	ELECTRON MICROSCOPY	2.8
7F1Q	Cryo-EM structure of the chemokine receptor CCR5 in complex with MIP-1a and Gi	ELECTRON MICROSCOPY	2.9
7F1R	Cryo-EM structure of the chemokine receptor CCR5 in complex with RANTES and Gi	ELECTRON MICROSCOPY	3
7O7F	Structural basis of the activation of the CC chemokine receptor 5 by a chemokine agonist	ELECTRON MICROSCOPY	3.15
7NJZ	X-ray crystallography study of RoAb13 which binds to PIYDIN, a part of the CCR5 N …	X-RAY DIFFRACTION	3.2
8AS2	Structure of arrestin2 in complex with 4P CCR5 phosphopeptide and Fab30	X-RAY DIFFRACTION	3.2
9WP1	Structural insights into tyrosine sulfation of CCR5 by human tyrosylprotein …	X-RAY DIFFRACTION	3.2
7NW3	X-ray crystallographic study of PIYDIN, which contains the truncation determinants of …	X-RAY DIFFRACTION	3.2
8AS3	Structure of arrestin2 in complex with 6P CCR5 phosphopeptide and Fab30	X-RAY DIFFRACTION	3.5
6MEO	Structural basis of coreceptor recognition by HIV-1 envelope spike	ELECTRON MICROSCOPY	3.9
6MET	Structural basis of coreceptor recognition by HIV-1 envelope spike	ELECTRON MICROSCOPY	4.5
2L87	The 27-residue N-terminus CCR5-peptide in a ternary complex with HIV-1 gp120 and a …	SOLUTION NMR
2MZX	CCR5-ECL2 helical structure, residues Q186-T195	SOLUTION NMR
2RLL	CCR5 Nt(7-15)	SOLUTION NMR
2RRS	NMR Structure of LC4 transmembrane segment of CCR5	SOLUTION NMR
6FGP	NMR solution structure of monomeric CCL5 in complex with a doubly-sulfated N-terminal …	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P51681-F1	85.41	0.66

Antibody-complex structures (SAbDab)

10 antibodies co-crystallized with this protein: 5YD3, 5YD4, 5YD5, 5YY4, 7NJZ, 7NW3, 7O7F, 8AS2, 8AS3, 9J8A

Human Protein Atlas

Protein class: CD markers, G-protein coupled receptors, GPCRs excl olfactory receptors, Chemokines and chemotactic factors receptors, Predicted membrane proteins, GPCRHMM predicted membrane proteins, Disease related genes, FDA approved drug targets, Small molecule drugs, Human disease related genes, Diabetes

Protein evidence: Evidence at protein level

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Post-translational modifications (11)

Type	Positions
Sulfotyrosine	3, 10, 14, 15
Phosphoserine	336, 337, 342, 349
S-palmitoyl cysteine	321, 323, 324

Disulfide bonds (2)

Type	Positions
Disulfide bond	20–269, 101–178

Glycosylation sites (2)

Type	Positions
O-linked (galnac…) serine	6, 7

Mutagenesis-validated functional residues (22)

Position	Phenotype
3	no sulfation and strongly decreases binding with ccl4 and ccl5; when associated with d-10; d-14 and d-15. restores most ccl4 binding; when …
3	no sulfation and strongly decreases binding with ccl4 and ccl5; when associated with f-10; f-14 and f-15.
6–7	loss of molecular mass of 2 kda compared to wild type when treated with o-glycosidase. dramatically reduces binding with ccl4. loss of …
6	strongly decreases ccl4 binding. no change in glycosylation status.
7	no change in glycosylation status and binds ccl4 as efficiently as wild type.
10	no sulfation and greatly decreases binding of ccl4 and ccl5; when associated with f-3; f-14 and f-15. small loss of sulfation; when …
14	no sulfation and greatly decreased binding of ccl4 and ccl5; when associated with d-3; d-10 and d-14. no restoration of ccl4 binding; when …
14	no sulfation and greatly decreases binding of ccl4 and ccl5; when associated with f-3; f-10; and f-15. small loss of sulfation; when …
15	no sulfation and greatly decreased binding of ccl4 and ccl5; when associated with d-3; d-10 and d-14. restored most ccl4 binding; when …
15	no sulfation and greatly decreases binding of ccl4 and ccl5; when associated with f-3; f-10 and f-14. small loss of sulfation; when …
16–17	similar decrease in molecular mass when treated with o-glycosidase as for wild type. loss of molecular mass of about 2 kda as compared to …
20	decreases to 40% surface expression. no effect on conformational integrity. disrupts binding of ccl4. decreases cell hiv infection.
101	decreases to 40% surface expression. disrupts conformational integrity. disrupts binding of ccl4. decreases hiv cell infection.
178	decreases to 40% surface expression. disrupts conformational integrity. disrupts binding of ccl4. decreases hiv cell infection.
269	decreases to 40% surface expression. no effect on conformational integrity. disrupts binding of ccl4. decreases cell hiv infection.
321	small reduction in palmitoylation. cell surface expression reduced by 50%. greatly reduced palmitoylation. cell surface expression greatly …
323	small reduction in palmitoylation. cell surface expression reduced by 50%. greatly reduced palmitoylation. cell surface expression greatly …
324	small reduction in palmitoylation. cell surface expression reduced by 50%. greatly reduced palmitoylation. cell surface expression greatly …
336	apo-rantes-stimulated phosphorylation reduced by 15%; apo-rantes-stimulated phosphorylation reduced by 30-50%; when associated with a-337 …
337	apo-rantes-stimulated phosphorylation reduced by 18%; apo-rantes-stimulated phosphorylation reduced by 30-50% on apo-rantes stimulation …
342	apo-rantes-stimulated phosphorylation reduced by 42%. phosphorylation reduced by 50% on apo-rantes stimulation; when associated with a-336 …
349	apo-rantes-stimulated phosphorylation reduced by 43%; apo-rantes-stimulated phosphorylation reduced by 30-50%; when associated with a-336 …

Function

Pathways and Gene Ontology

Reactome pathways

5 curated (TAS) of 20; 7 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

20 pathways:

ID	Pathway	Evidence
R-HSA-173107	Binding and entry of HIV virion ⚕	curated
R-HSA-380108	Chemokine receptors bind chemokines	curated
R-HSA-9968734	Differentiation of Circulating Monocytes	curated
R-HSA-418594	G alpha (i) signalling events	curated
R-HSA-6783783	Interleukin-10 signaling	curated
R-HSA-1643685	Disease ⚕	—
R-HSA-162594	Early Phase of HIV Life Cycle ⚕	—
R-HSA-162906	HIV Infection ⚕	—
R-HSA-162587	HIV Life Cycle ⚕	—
R-HSA-5663205	Infectious disease ⚕	—
R-HSA-9824446	Viral Infection Pathways ⚕	—
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)	—
R-HSA-1280215	Cytokine Signaling in Immune system	—
R-HSA-388396	GPCR downstream signalling	—
R-HSA-500792	GPCR ligand binding	—
R-HSA-168256	Immune System	—
R-HSA-375276	Peptide ligand-binding receptors	—
R-HSA-162582	Signal Transduction	—
R-HSA-372790	Signaling by GPCR	—
R-HSA-449147	Signaling by Interleukins	—

MSigDB gene sets: 383 (showing top): MODULE_92, LIANG_HEMATOPOIESIS_STEM_CELL_NUMBER_SMALL_VS_HUGE_UP, WALLACE_PROSTATE_CANCER_RACE_UP, GOBP_DENDRITIC_CELL_MIGRATION, GOBP_CELL_CHEMOTAXIS, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, GOBP_INFLAMMATORY_RESPONSE, GOBP_RESPONSE_TO_PEPTIDE, GOBP_REGULATION_OF_LEUKOCYTE_APOPTOTIC_PROCESS, GOBP_CELLULAR_RESPONSE_TO_LIPID, GOBP_CELLULAR_RESPONSE_TO_BIOTIC_STIMULUS, MODULE_64, KENNY_CTNNB1_TARGETS_UP, GOCC_CELL_SURFACE, MODULE_128

GO Biological Process (22): MAPK cascade (GO:0000165), dendritic cell chemotaxis (GO:0002407), calcium ion transport (GO:0006816), chemotaxis (GO:0006935), inflammatory response (GO:0006954), immune response (GO:0006955), cellular defense response (GO:0006968), cell surface receptor signaling pathway (GO:0007166), G protein-coupled receptor signaling pathway (GO:0007186), positive regulation of cytosolic calcium ion concentration (GO:0007204), cell-cell signaling (GO:0007267), release of sequestered calcium ion into cytosol by sarcoplasmic reticulum (GO:0014808), calcium-mediated signaling (GO:0019722), signaling (GO:0023052), cell chemotaxis (GO:0060326), response to cholesterol (GO:0070723), cellular response to lipopolysaccharide (GO:0071222), negative regulation of macrophage apoptotic process (GO:2000110), signal transduction (GO:0007165), symbiont entry into host cell (GO:0046718), chemokine-mediated signaling pathway (GO:0070098), cellular response to cytokine stimulus (GO:0071345)

GO Molecular Function (11): virus receptor activity (GO:0001618), actin binding (GO:0003779), phosphatidylinositol-4,5-bisphosphate phospholipase C activity (GO:0004435), chemokine receptor activity (GO:0004950), coreceptor activity (GO:0015026), C-C chemokine receptor activity (GO:0016493), C-C chemokine binding (GO:0019957), identical protein binding (GO:0042802), chemokine (C-C motif) ligand 5 binding (GO:0071791), G protein-coupled receptor activity (GO:0004930), protein binding (GO:0005515)

GO Cellular Component (6): cytoplasm (GO:0005737), endosome (GO:0005768), plasma membrane (GO:0005886), external side of plasma membrane (GO:0009897), cell surface (GO:0009986), membrane (GO:0016020)

Reactome top-level categories

16 top-level categories:

Category	Pathways
Signaling by GPCR	2
Early Phase of HIV Life Cycle	1
Peptide ligand-binding receptors	1
GPCR downstream signalling	1
Signaling by Interleukins	1
Developmental Cell Lineages	1
Immune System	1
HIV Infection	1
HIV Life Cycle	1
Viral Infection Pathways	1
Signal Transduction	1
GPCR ligand binding	1
Class A/1 (Rhodopsin-like receptors)	1
Cytokine Signaling in Immune system	1
Disease	1
Infectious disease	1

GO top-level categories

59 GO namespaces:

Category	Terms
cellular anatomical structure	3
intracellular signaling cassette	2
defense response	2
signal transduction	2
cell communication	2
signaling	2
chemokine binding	2
C-C chemokine binding	2
leukocyte chemotaxis	1
dendritic cell migration	1
metal ion transport	1
response to chemical	1
taxis	1
immune system process	1
response to stimulus	1
G protein-coupled receptor activity	1
regulation of biological quality	1
sarcoplasmic reticulum calcium ion transport	1
release of sequestered calcium ion into cytosol by endoplasmic reticulum	1
regulation of biological process	1
chemotaxis	1
cell migration	1
cellular response to chemical stimulus	1
response to sterol	1
response to alcohol	1
response to lipopolysaccharide	1
cellular response to molecule of bacterial origin	1
cellular response to lipid	1
cellular response to oxygen-containing compound	1
negative regulation of myeloid cell apoptotic process	1
macrophage apoptotic process	1
negative regulation of leukocyte apoptotic process	1
regulation of macrophage apoptotic process	1
cellular process	1
regulation of cellular process	1
cellular response to stimulus	1
viral life cycle	1
symbiont entry into host	1
symbiont entry into host cell	1
exogenous protein binding	1
cytoskeletal protein binding	1
C-type glycerophospholipase activity	1
G protein-coupled chemoattractant receptor activity	1
cytokine receptor activity	1
chemokine-mediated signaling pathway	1
signaling receptor activity	1
chemokine receptor activity	1
protein binding	1
transmembrane signaling receptor activity	1
G protein-coupled receptor signaling pathway	1
binding	1
intracellular anatomical structure	1
endomembrane system	1
cytoplasmic vesicle	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) — 17 of 39 annotations. The rest are phylogenetic / computational / electronic (IEA).

17 experimentally-supported GO terms:

GO term	NS	Evidence
G protein-coupled receptor signaling pathway	BP	mutant phenotype
MAPK cascade	BP	expression pattern
calcium ion transport	BP	direct assay
calcium-mediated signaling	BP	direct assay
cell-cell signaling	BP	direct assay
cellular response to lipopolysaccharide	BP	expression pattern
release of sequestered calcium ion into cytosol by sarcoplasmic reticulum	BP	direct assay
response to cholesterol	BP	mutant phenotype
signaling	BP	expression pattern
cell surface	CC	direct assay
endosome	CC	direct assay
external side of plasma membrane	CC	direct assay
C-C chemokine binding	MF	physical interaction
C-C chemokine receptor activity	MF	direct assay
actin binding	MF	direct assay
chemokine (C-C motif) ligand 5 binding	MF	physical interaction
identical protein binding	MF	physical interaction

Protein interactions and networks

STRING

showing 15 of 3,150 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CCR5	CCL5	P13501	958
CCR5	CD4	P01730	946
CCR5	CCL3	P10147	941
CCR5	ITIH4	Q14624	938
CCR5	CCL4	P13236	929
CCR5	CCL2	P13500	896
CCR5	CD8A	P01732	890
CCR5	IL6	P05231	856
CCR5	IFNG	P01579	854
CCR5	CXCL12	P48061	830
CCR5	CCL3L1	P16619	823
CCR5	CX3CL1	P78423	816
CCR5	TNF	P01375	809
CCR5	IL10	P22301	809
CCR5	ERVW-1	Q9UQF0	792

IntAct

Human interaction partners of CCR5 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

20 partners by confidence:

Partner	Interaction type	MIscore	Records
CD4	physical association	0.670	3
CXCR4	physical association	0.670	3
CCL5	physical association	0.660	5
EMP1	physical association	0.560	3
PRAF2	physical association	0.520	3
CCL17	physical association	0.500	2
ACKR1	physical association	0.470	3
CCL4	physical association	0.400	2
ARL6IP5	physical association	0.400	1
MYH9	physical association	0.400	1
RAMP1	physical association	0.400	1
RAMP2	physical association	0.400	1
RAMP3	physical association	0.400	1
C	physical association	0.370	1
CREB3	physical association	0.370	1
CST9L	physical association	0.370	1
CTBP2	physical association	0.370	1
ETV5	physical association	0.370	1
IL24	physical association	0.370	1
SLC20A2	physical association	0.370	1

BioGRID (25 interactions; top human partners by supporting records): CCL5 (Affinity Capture-Western; 3 records), CCL3L1 (Reconstituted Complex; 2 records), PSMA5 (Two-hybrid; 2 records), AFP (Affinity Capture-Western), ARRB1 (Reconstituted Complex), CCL3 (Reconstituted Complex), CD4 (Affinity Capture-Western), CST9L (Two-hybrid), CTBP2 (Two-hybrid), CXCR4 (Reconstituted Complex), EMP1 (Two-hybrid), ETV5 (Two-hybrid), IL24 (Two-hybrid), JAK2 (Affinity Capture-Western), PIK3R2 (Affinity Capture-Western)

SIGNOR signaling

showing 12 of 16 signaling interactions:

A	Effect	B	Mechanism
maraviroc	down-regulates	CCR5	“chemical inhibition”
“Vicriviroc Malate”	down-regulates	CCR5	“chemical inhibition”
CCL5	“up-regulates activity”	CCR5	binding
CCR5	“up-regulates activity”	GNAI1	binding
CCR5	“up-regulates activity”	GNAI2	binding
CCR5	“up-regulates activity”	GNAZ	binding
CCR5	“up-regulates activity”	GNAO1	binding
CCR5	“up-regulates activity”	GNA15	binding
CCL3	“up-regulates activity”	CCR5	binding
CCL4	“up-regulates activity”	CCR5	binding
CCR5	“up-regulates activity”	ERK1/2	phosphorylation
GRK3	“down-regulates activity”	CCR5	phosphorylation

Protein complexes (CORUM) (10)

Experimentally-characterized complexes this protein is a subunit of (★ = the complex contains a known drug target).

10 complexes by size:

Complex	Subunits	Members
★ CCR5-CD4-CXCR4 complex	3	CCR5, CD4, CXCR4
★ CCR5-CNIH4 complex	2	CCR5, CNIH4
★ C5AR1-CCR5 complex	2	C5AR1, CCR5
★ CCR5-CXCR4 complex	2	CCR5, CXCR4
★ CCR2-CCR5 complex	2	CCR2, CCR5
★ CCR5-OPRM1 complex	2	CCR5, OPRM1
★ CCR5-OPRD1 complex	2	CCR5, OPRD1
★ CCR5-OPRK1 complex	2	CCR5, OPRK1
★ CCR5-CD4 complex	2	CCR5, CD4
★ C-C chemokine receptor type 5	1	CCR5

Ligand–receptor pairs (CellPhoneDB) (5)

Curated ligand–receptor partners (cell-cell communication), distinct from the protein–protein interactions above.

5 ligand–receptor pairs:

Partner	This gene’s role	Signaling class
CCL7	receptor	Signaling by Chemokines
CCL5	receptor	Signaling by Chemokines
CCL3	receptor	Signaling by Chemokines
CCL8	receptor	Signaling by Chemokines
CCL4	receptor	Signaling by Chemokines

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 20 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

GO biological processes:

GO term	Partners	Fold	FDR
protein transport	6	13.9×	3e-04
immune response	5	12.4×	7e-04
inflammatory response	5	9.9×	2e-03
G protein-coupled receptor signaling pathway	5	9.5×	2e-03

Disease & clinical

Genetic variants

Variant evidence for CCR5: 46 ClinVar records (0 pathogenic / likely pathogenic); 9 GWAS associations.

ClinVar

46 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	29
Likely benign	4
Benign	5

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 17 predictions of 23):

Position(s)	Effect	Δscore	Sites
3:46370989–46370990	donor_loss	0.9900	3
3:46370989	donor_loss	0.9800
3:46372890–46372891	acceptor_loss	0.9800	3
3:46370990	donor_loss	0.9700
3:46372889–46372891	acceptor_loss	0.9700	4
3:46372885	acceptor_gain	0.9200
3:46372885	acceptor_gain	0.8100
3:46373040	acceptor_gain	0.7500
3:46372881	acceptor_loss	0.7400
3:46373645	acceptor_gain	0.5400

AlphaMissense

682 missense substitutions predicted likely pathogenic (of 2,321 scored), across 197 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
D76	8	0.946	0.980
N48	8	0.936	0.980
D125	8	0.936	0.974
F304	8	0.892	0.987
D66	8	0.853	0.906
H289	8	0.826	0.951
F118	8	0.820	0.923
D276	8	0.709	0.811
C178	7	0.971	0.986
C101	7	0.967	0.986
W94	7	0.952	0.993
C20	7	0.943	0.969
C269	7	0.930	0.957
F166	7	0.919	0.967
W248	7	0.897	0.975
W153	7	0.895	0.994
R126	7	0.891	0.961
N293	7	0.889	0.978
F182	7	0.851	0.946
F113	7	0.806	0.943

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
Head and Neck Squamous Cell Carcinoma (TCGA)	favorable	0.000332

Disease associations

OMIM: gene MIM:601373 | disease phenotypes:

GWAS associations

9 associations:

Study	Trait	p-value
GCST009731_29	Blood protein levels in cardiovascular risk	8e-83
GCST000612_32	Celiac disease	3e-17
GCST002665_3	Cerebrospinal fluid levels of Alzheimer’s disease-related proteins	2e-13
GCST003045_6	Ulcerative colitis	9e-10
GCST004608_74	Granulocyte percentage of myeloid white cells	1e-9
GCST003045_39	Ulcerative colitis	1e-8
GCST003043_190	Inflammatory bowel disease	4e-8
GCST005536_41	Type 1 diabetes	5e-8
GCST004133_14	Ulcerative colitis	2e-6

EFO canonical traits (from GWAS)

2 canonical traits:

EFO ID	Trait name
EFO:0006514	Alzheimer’s disease biomarker measurement
EFO:0007997	granulocyte percentage of myeloid white cells

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL274 (SINGLE PROTEIN), CHEMBL3301384 (PROTEIN COMPLEX)

Drugs by curated mechanism of action (ChEMBL)

Drugs whose curated ChEMBL mechanism of action targets the CCR5 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.

12 curated-mechanism drugs:

Drug	Modality	Max phase
MARAVIROC	Small molecule	4
APLAVIROC HYDROCHLORIDE	Small molecule	3
CENICRIVIROC	Small molecule	3
LERONLIMAB	Antibody	3
VICRIVIROC MALEATE	Small molecule	3
AZD5672	Small molecule	2
BMS-813160	Small molecule	2
INCB-9471	Small molecule	2
PF-04634817	Small molecule	2
PF-232798	Small molecule	2
CCR5MAB004	Unknown	1
HGS-1025	Unknown	1

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 78,757 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

15 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL256907	MARAVIROC	4	6
CHEMBL2205807	ABAMETAPIR	4	761
CHEMBL964	DISULFIRAM	4	39,061
CHEMBL17157	TERFENADINE	4	25,528
CHEMBL1255794	APLAVIROC	3	957
CHEMBL1668019	APLAVIROC HYDROCHLORIDE	3	41
CHEMBL2110727	CENICRIVIROC	3	2,245
CHEMBL82301	VICRIVIROC	3	8,805
CHEMBL1951914	AZD5672	2	226
CHEMBL4594419	BMS-813160	2	60
CHEMBL1688243	INCB-9471	2	152
CHEMBL78535	ANCRIVIROC	2	790
CHEMBL4457723	BMS-741672	2	2
CHEMBL397647	JNJ-17166864 CATION	2	36
CHEMBL2105686	CENICRIVIROC MESYLATE	1	87

PharmGKB: 1 entry (CPIC guideline: no)

PharmGKB variant annotations

Per-publication pharmacogenomic findings for this gene (significant associations).

1 published findings:

Variant	Drug(s)	Category	Finding	PMID
rs333	glatiramer acetate	Efficacy	Allele del is associated with decreased response to glatiramer acetate in people with Multiple Sclerosis as compared to allele GTCAGTATCAATTCTGGAAGAATTTCCAGACA.	PMID:22111603

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: gpcr — Chemokine receptors

Most potent curated ligand interactions (31 total), top 25:

Ligand	Action	Affinity	Parameter
CCL5	Full agonist	9.7	pKi
CCL4	Full agonist	9.6	pKi
[125I]CCL4 (human)	Full agonist	9.6	pKd
AZD5672	Antagonist	9.59	pIC50
CCL8	Full agonist	9.3	pKi
vicriviroc	Antagonist	9.1	pKi
CCL13	Full agonist	9.1	pKi
[3H]maraviroc	Antagonist	9.1	pKd
CCL3	Full agonist	8.9	pKi
[3H]ancriviroc	Antagonist	8.9	pKd
E913	Antagonist	8.7	pIC50
ancriviroc	Antagonist	8.7	pKi
BMS-681	Antagonist	8.62	pIC50
cenicriviroc	Antagonist	8.6	pIC50
CCR5 antagonist 34	Antagonist	8.52	pIC50
TAK-220	Antagonist	8.5	pIC50
aplaviroc	Antagonist	8.5	pKi
vMIP-II	Antagonist	8.3	pIC50
maraviroc	Antagonist	8.1	pIC50
BP-CCL3	Full agonist	7.7	pKi
CCL11	Full agonist	7.7	pIC50
Flu-CCL3	Full agonist	7.6	pKi
CCL7	Antagonist	7.5	pKi
CCL2	Full agonist	7.5	pKi
TAK-779	Antagonist	7.5	pKi

Binding affinities (BindingDB)

2226 measured of 2381 human assays (2381 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
N-((1S)-3-(4-(3-(3,4-dichlorobenzyl)-1-ethylureido)piperidin-1-yl)-1-phenylbutyl)cyclobutanecarboxamide	IC50	0.003 nM
(4,6-Dimethyl-pyrimidin-5-yl)-(4-methyl-4-{(S)-3-methyl-4-[(S)-1-(4-trifluoromethyl-phenyl)-ethyl]-piperazin-1-yl}-piperidin-1-yl)-methanone	IC50	0.01 nM
N-((1S)-3-(4-(2-(3,4-dichlorophenyl)-N-ethylacetamido)piperidin-1-yl)-1-phenylbutyl)cyclobutanecarboxamide	IC50	0.05 nM
3-(R)-Cyclopropyl-2-[(S)-3-{4-[3,3-difluoro-3-(4-fluoro-phenyl)-propyl]-piperidin-1-ylmethyl}-4-(3-fluoro-phenyl)-pyrrolidin-1-yl]-propionic acid	IC50	0.06 nM
CHEMBL181276	IC50	0.06 nM
N-((1S)-3-(4-(N-ethyl-2-(4-(methylsulfonyl)phenyl)acetamido)piperidin-1-yl)-1-phenylbutyl)cyclobutanecarboxamide	IC50	0.07 nM
CHEMBL2164207	IC50	0.08 nM
CHEMBL1926899	IC50	0.09 nM
Allyl-{1-[(S)-4-(benzenesulfonyl-methyl-amino)-3-methyl-3-phenyl-butyl]-piperidin-4-yl}-carbamic acid 4-nitro-benzyl ester	IC50	0.1 nM
Allyl-[1-((3S,4S)-1-benzyl-4-phenyl-pyrrolidin-3-ylmethyl)-piperidin-4-yl]-carbamic acid 4-nitro-benzyl ester	IC50	0.1 nM
Cyclohexyl-{3-phenyl-4-[4-(3-phenyl-propyl)-piperidin-1-ylmethyl]-pyrrolidin-1-yl}-acetic acid	IC50	0.1 nM
(R)-3-Cyclobutyl-2-{(S)-3-phenyl-4-[4-(3-phenyl-propyl)-piperidin-1-ylmethyl]-pyrrolidin-1-yl}-propionic acid	IC50	0.1 nM
(R)-3-cyclopropyl-2-((3S,4S)-3-phenyl-4-((4-(3-phenylpropyl)piperidin-1-yl)methyl)pyrrolidin-1-yl)propanoic acid	IC50	0.1 nM
2-cyclobutyl-2-{3-phenyl-4-[4-(3-phenylpropyl)hexahydro-1-pyridinylmethyl]tetrahydro-1H-1-pyrrolyl}acetic acid	IC50	0.1 nM
(R)-3-cyclobutyl-2-((3S,4S)-3-(3-fluorophenyl)-4-((4-(2-(4-fluorophenylthio)ethyl)piperidin-1-yl)methyl)pyrrolidin-1-yl)propanoic acid	IC50	0.1 nM
(4-{(4-Bromo-phenyl)-[(E)-ethoxyimino]-methyl}-4’-methyl-[1,4’]bipiperidinyl-1’-yl)-(2,6-dimethyl-4-pyridin-4-yl-phenyl)-methanone	KI	0.1 nM
endo-methyl 3-(8-((S)-3-acetamido-3-(3-fluorophenyl)propyl)-8-azabicyclo[3.2.1]octan-3-yl)-2-methyl-6,7-dihydro-3H-imidazo[4,5-c]pyridine-5(4H)-carboxylate	IC50	0.1 nM
CHEMBL2164210	IC50	0.1 nM
CHEMBL2164202	IC50	0.1 nM
CHEMBL2164217	IC50	0.11 nM
4N-allyl-4N-[4-nitrobenzyloxycarboyl]-1-[4’-phenyl-(3a’S,4’S,5’S)-spiro[cyclohexane-1,2’-perhydropyrrolo[1,2-b]isoxazole]-5-ylmethyl]hexahydro-4-pyridinamine	IC50	0.13 nM
(+/-)-N-((1S)-3-(4-(3-isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)piperidin-1-yl)-1-phenylbutyl)cyclopentanecarboxamide	IC50	0.137 nM
N-((1S)-3-(4-(3-benzyl-1-ethylureido)piperidin-1-yl)-1-phenylbutyl)cyclobutanecarboxamide	IC50	0.16 nM
CHEMBL2178577	IC50	0.17 nM
Compound T140	EC50	0.18 nM
(S)-(-)-8-{4-[2-(butoxy)ethoxy]phenyl}-1-isobutyl-N-(4-{[(4-propyl-4H-1,2,4-triazol-3-yl)methyl]sulfinyl}phenyl)-1,2,3,4-tetrahydro-1-benzazocine-5-carboxamide	IC50	0.19 nM
Allyl-[1-((3S,4S)-1-benzoyl-4-phenyl-pyrrolidin-3-ylmethyl)-piperidin-4-yl]-carbamic acid 4-nitro-benzyl ester	IC50	0.2 nM
Allyl-[1-((3S,4S)-1-cyclopentanecarbonyl-4-phenyl-pyrrolidin-3-ylmethyl)-piperidin-4-yl]-carbamic acid 4-nitro-benzyl ester	IC50	0.2 nM
1-(1-Cyclohexylmethyl-4-phenyl-pyrrolidin-3-ylmethyl)-4-{3-[4-(1-methyl-1H-tetrazol-5-yl)-phenyl]-propyl}-piperidin-4-ol	IC50	0.2 nM
1-(1-Cyclohexylmethyl-4-phenyl-pyrrolidin-3-ylmethyl)-4-{3-[4-(1H-tetrazol-5-yl)-phenyl]-propyl}-piperidin-4-ol	IC50	0.2 nM
2-cyclopentyl-2-{3-phenyl-4-[4-(3-phenylpropyl)hexahydro-1-pyridinylmethyl]tetrahydro-1H-1-pyrrolyl}acetic acid	IC50	0.2 nM
(R)-3-Cyclobutyl-2-((S)-3-(3-fluoro-phenyl)-4-{4-[3-(4-trifluoromethyl-phenyl)-propyl]-piperidin-1-ylmethyl}-pyrrolidin-1-yl)-propionic acid	IC50	0.2 nM
3-(R)-Cyclobutyl-2-((S)-3-{4-[3,3-difluoro-3-(4-fluoro-phenyl)-propyl]-piperidin-1-ylmethyl}-4-phenyl-pyrrolidin-1-yl)-propionic acid	IC50	0.2 nM
(R)-2-[(2S,3S)-3-[4-(2-Ethyl-5-naphthalen-2-ylmethyl-2H-pyrazol-3-yl)-piperidin-1-ylmethyl]-4-(3-fluoro-phenyl)-pyrrolidin-1-yl]-3,3-dimethyl-butyric acid	IC50	0.2 nM
(2R,4R)-2-[(2S,3S)-3-[4-(2-Ethyl-5-naphthalen-2-ylmethyl-2H-pyrazol-3-yl)-piperidin-1-ylmethyl]-4-(3-fluoro-phenyl)-pyrrolidin-1-yl]-3-methyl-pentanoic acid	IC50	0.2 nM
(2R,4R)-2-[(2S,3S)-3-[4-(2-Ethyl-5-naphthalen-1-ylmethyl-2H-pyrazol-3-yl)-piperidin-1-ylmethyl]-4-(3-fluoro-phenyl)-pyrrolidin-1-yl]-3-methyl-pentanoic acid	IC50	0.2 nM
(R)-2-[(2S,3S)-3-[4-(2-Ethyl-5-naphthalen-1-ylmethyl-2H-pyrazol-3-yl)-piperidin-1-ylmethyl]-4-(3-fluoro-phenyl)-pyrrolidin-1-yl]-3,3-dimethyl-butyric acid	IC50	0.2 nM
(R)-Cyclohexyl-[(2S,3S)-3-{4-[5-(4-cyclopropoxy-benzyl)-2-ethyl-2H-pyrazol-3-yl]-piperidin-1-ylmethyl}-4-(3-fluoro-phenyl)-pyrrolidin-1-yl]-acetic acid	IC50	0.2 nM
endo-methyl(S)-3-(3-(5-acetyl-2-methyl-4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridin-3-yl)-8-azabicyclo[3.2.1]octan-8-yl)-1-(3-fluorophenyl)propylcarbamate	IC50	0.2 nM
endo-methyl 3-(8-((S)-3-(3-fluorophenyl)-3-(methoxycarbonylamino)propyl)-8-azabicyclo[3.2.1]octan-3-yl)-2-methyl-6,7-dihydro-3H-imidazo[4,5-c]pyridine-5(4H)-carboxylate	IC50	0.2 nM
CHEMBL1926893	IC50	0.2 nM
(S)-(-)-8-{4-[2-(butoxy)ethoxy]phenyl}-1-[(1-methyl-1H-pyrazol-4-yl)methyl]-N-(4-{[(1-propyl-1H-imidazol-5-yl)methyl]-sulfinyl}phenyl)-1,2,3,4-tetrahydro-1-benzazocine-5-carboxamide	IC50	0.21 nM
(R)-N-ethyl-N-(1-(3-(3-fluorophenyl)-3-(4-(methylsulfonyl)phenyl)propyl)piperidin-4-yl)-2-(4-(methylsulfonyl)phenyl)acetamide	IC50	0.22 nM
2-{(S)-3-[4-(2-Benzyl-thiazol-5-yl)-piperidin-1-ylmethyl]-4-phenyl-pyrrolidin-1-yl}-3-cyclobutyl-propionic acid	IC50	0.23 nM
2-{(S)-3-[4-(2-Benzyl-thiazol-5-yl)-piperidin-1-ylmethyl]-4-phenyl-pyrrolidin-1-yl}-3-cyclopropyl-propionic acid	IC50	0.23 nM
(R)-2-((3S,4S)-3-((4-(2-benzylthiazol-5-yl)piperidin-1-yl)methyl)-4-phenylpyrrolidin-1-yl)-3-cyclobutylpropanoic acid	IC50	0.23 nM
(R)-2-((3S,4S)-3-((4-(2-benzylthiazol-5-yl)piperidin-1-yl)methyl)-4-phenylpyrrolidin-1-yl)-3-cyclopropylpropanoic acid	IC50	0.23 nM
CHEMBL3577945	IC50	0.24 nM
(S)-(-)-8-{4-[2-(butoxy)ethoxy]phenyl}-1-propyl-N-(4-{[(1-propyl-1H-imidazol-5-yl)methyl]sulfinyl}phenyl)-1,2,3,4-tetrahydro-1-benzazocine-5-carboxamide	IC50	0.24 nM
CHEMBL1951914	IC50	0.26 nM

ChEMBL bioactivities

3034 potent at pChembl≥5 of 3211 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	IC50	0.01	nM	CHEMBL311795
10.30	IC50	0.05	nM	CHEMBL460845
10.22	IC50	0.06	nM	CHEMBL21106
10.22	IC50	0.06	nM	CHEMBL181276
10.22	IC50	0.05998	nM	CHEMBL21106
10.15	IC50	0.07	nM	CHEMBL457043
10.10	IC50	0.08	nM	CHEMBL2164207
10.05	IC50	0.09	nM	CHEMBL1926899
10.00	IC50	0.1	nM	CHEMBL20345
10.00	IC50	0.1	nM	CHEMBL20896
10.00	IC50	0.1	nM	CHEMBL2164210
10.00	IC50	0.1	nM	CHEMBL2164202
10.00	IC50	0.1	nM	CENICRIVIROC MESYLATE
10.00	IC50	0.1	nM	CHEMBL328445
10.00	IC50	0.1	nM	CHEMBL316475
10.00	IC50	0.1	nM	CHEMBL320386
10.00	IC50	0.1	nM	CHEMBL93139
10.00	IC50	0.1	nM	CHEMBL1649924
10.00	Ki	0.1	nM	CHEMBL140484
10.00	IC50	0.1	nM	CHEMBL102826
9.96	IC50	0.11	nM	CHEMBL2164217
9.89	IC50	0.13	nM	CHEMBL157491
9.86	IC50	0.137	nM	CHEMBL473558
9.80	IC50	0.16	nM	CHEMBL461687
9.77	IC50	0.17	nM	AZD-5363
9.74	EC50	0.18	nM	CHEMBL2372983
9.72	IC50	0.19	nM	CHEMBL3085308
9.70	IC50	0.2	nM	CHEMBL171958
9.70	IC50	0.2	nM	CHEMBL369235
9.70	IC50	0.2	nM	CHEMBL21147
9.70	IC50	0.2	nM	CHEMBL366770
9.70	IC50	0.2	nM	CHEMBL173400
9.70	IC50	0.2	nM	CHEMBL20622
9.70	IC50	0.2	nM	CHEMBL174927
9.70	IC50	0.2	nM	CENICRIVIROC MESYLATE
9.70	IC50	0.2	nM	MARAVIROC
9.70	IC50	0.2	nM	CHEMBL319593
9.70	IC50	0.2	nM	CHEMBL99909
9.70	IC50	0.2	nM	CHEMBL329893
9.70	IC50	0.2	nM	CHEMBL431852
9.70	IC50	0.2	nM	CHEMBL1649926
9.70	IC50	0.2	nM	CHEMBL1649927
9.70	IC50	0.2	nM	CHEMBL102826
9.70	IC50	0.2	nM	CHEMBL1926893
9.70	IC50	0.2	nM	CHEMBL322422
9.68	IC50	0.21	nM	CHEMBL3085309
9.66	IC50	0.22	nM	CHEMBL212731
9.64	IC50	0.2301	nM	CHEMBL520091
9.64	IC50	0.2301	nM	CHEMBL511493
9.64	IC50	0.23	nM	CHEMBL520091

PubChem BioAssay actives

2787 with measured affinity, of 3784 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
N-[(1S)-3-[4-[(3,4-dichlorophenyl)methylcarbamoyl-ethylamino]piperidin-1-yl]-1-phenylbutyl]cyclobutanecarboxamide	393050: Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay	ic50	<0.0001	uM
(4,6-dimethylpyrimidin-5-yl)-[4-methyl-4-[(3S)-3-methyl-4-[(1S)-1-[4-(trifluoromethyl)phenyl]ethyl]piperazin-1-yl]piperidin-1-yl]methanone	42493: Inhibition of 0.1 nM of MIP-1beta induced migration of recombinant mouse pro-B cell line BA/F3 expressing human CCR5	ic50	<0.0001	uM
(2R)-3-cyclopropyl-2-[(3S,4S)-3-[[4-[3,3-difluoro-3-(4-fluorophenyl)propyl]piperidin-1-yl]methyl]-4-(3-fluorophenyl)pyrrolidin-1-yl]propanoic acid	352100: Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells	ic50	0.0001	uM
(5E)-8-[4-(2-butoxyethoxy)phenyl]-1-(2-methylpropyl)-N-[4-[(S)-(3-propylimidazol-4-yl)methylsulfinyl]phenyl]-3,4-dihydro-2H-1-benzazocine-5-carboxamide;methanesulfonic acid	261802: Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5	ic50	0.0001	uM
N-[(1S)-1-(3-fluorophenyl)-3-[(1R,5S)-3-(2-methyl-5-propanoyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]octan-8-yl]propyl]acetamide	554132: Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay	ic50	0.0001	uM
N-[(1S)-3-[4-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)piperidin-1-yl]-1-phenylbutyl]cyclopentanecarboxamide	395483: Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay	ic50	0.0001	uM
6-chloro-2,4-dimethyl-N-[(3R)-3-[4-[[2-(2-oxo-1,3-oxazolidin-3-yl)acetyl]-(thiophen-3-ylmethyl)amino]piperidin-1-yl]butyl]pyridine-3-carboxamide	696934: Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay	ic50	0.0001	uM
2-chloro-6-cyano-N-[(3R)-3-[4-[methoxycarbamoyl(thiophen-3-ylmethyl)amino]piperidin-1-yl]butyl]-4-methylpyridine-3-carboxamide	696934: Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay	ic50	0.0001	uM
2,6-dichloro-N-[(3R)-3-[4-[methoxycarbamoyl(thiophen-3-ylmethyl)amino]piperidin-1-yl]butyl]-4-methylpyridine-3-carboxamide	696934: Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay	ic50	0.0001	uM
(2S)-N-[(2S)-1-[[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-2-[[(2S,3R)-2-[[(2S,3R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2R)-2-aminopropanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxybutanoyl]amino]butanediamide	1928524: Antagonist activity at CCR5 (unknown origin) expressed in human HOS cells co-expressing HIV-1 FITC-gp120 Bal assessed inhibition of CD4 dependent gp120 Bal binding to CCR5 by western blot analysis	ic50	0.0001	uM
(4-nitrophenyl)methyl N-[1-[(3S)-4-[benzenesulfonyl(methyl)amino]-3-methyl-3-phenylbutyl]piperidin-4-yl]-N-prop-2-enylcarbamate	42496: Inhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cells	ic50	0.0001	uM
(2R)-3-cyclobutyl-2-[(3S,4S)-3-(3-fluorophenyl)-4-[[4-[2-(4-fluorophenyl)sulfanylethyl]piperidin-1-yl]methyl]pyrrolidin-1-yl]propanoic acid	352100: Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells	ic50	0.0001	uM
(2R)-3-cyclopropyl-2-[(3S,4S)-3-phenyl-4-[[4-(3-phenylpropyl)piperidin-1-yl]methyl]pyrrolidin-1-yl]propanoic acid	352100: Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells	ic50	0.0001	uM
(4-nitrophenyl)methyl N-[1-[[(3aS,4S,5S)-4-phenylspiro[3a,4,5,6-tetrahydro-3H-pyrrolo[1,2-b][1,2]oxazole-2,1’-cyclohexane]-5-yl]methyl]piperidin-4-yl]-N-prop-2-enylcarbamate	42378: Ability to displace [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranes	ic50	0.0001	uM
N-[(1S)-3-[4-[[2-(3,4-dichlorophenyl)acetyl]-ethylamino]piperidin-1-yl]-1-phenylbutyl]cyclobutanecarboxamide	393050: Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay	ic50	0.0001	uM
N-[(1S)-3-[4-[ethyl-[2-(4-methylsulfonylphenyl)acetyl]amino]piperidin-1-yl]-1-phenylbutyl]cyclobutanecarboxamide	393050: Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay	ic50	0.0001	uM
(4-nitrophenyl)methyl N-[1-[[(3S,4S)-1-benzyl-4-phenylpyrrolidin-3-yl]methyl]piperidin-4-yl]-N-prop-2-enylcarbamate	1957048: Inhibition of human CCR5	ic50	0.0001	uM
(2R)-2-cyclohexyl-2-[(3S,4S)-3-phenyl-4-[[4-(3-phenylpropyl)piperidin-1-yl]methyl]pyrrolidin-1-yl]acetic acid	42379: In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.	ic50	0.0001	uM
(2R)-2-cyclobutyl-2-[(3S,4S)-3-phenyl-4-[[4-(3-phenylpropyl)piperidin-1-yl]methyl]pyrrolidin-1-yl]acetic acid	352100: Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells	ic50	0.0001	uM
(2R)-3-cyclobutyl-2-[(3S,4S)-3-phenyl-4-[[4-(3-phenylpropyl)piperidin-1-yl]methyl]pyrrolidin-1-yl]propanoic acid	241856: Displacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranes	ic50	0.0001	uM
methyl 1-[(1R,5S)-8-[(3S)-3-acetamido-3-(3-fluorophenyl)propyl]-8-azabicyclo[3.2.1]octan-3-yl]-2-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridine-5-carboxylate	554132: Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay	ic50	0.0001	uM
propan-2-yl 3-[(1S,5R)-8-[(3S)-3-acetamido-3-phenylpropyl]-8-azabicyclo[3.2.1]octan-3-yl]-2-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridine-5-carboxylate	554132: Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay	ic50	0.0001	uM
N-[(1S)-1-(3-fluorophenyl)-3-[(1R,5S)-3-(2-methyl-5-pyrimidin-4-yl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]octan-8-yl]propyl]acetamide	554132: Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay	ic50	0.0001	uM
N-[(1S)-1-(3-fluorophenyl)-3-[(1R,5S)-3-(2-methyl-5-pyrazin-2-yl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]octan-8-yl]propyl]acetamide	554132: Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay	ic50	0.0001	uM
N-[(1S)-3-[(1R,5S)-3-(5-acetyl-2-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-(3-fluorophenyl)propyl]acetamide	554132: Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay	ic50	0.0001	uM
N-[(1S)-3-[(1R,5S)-3-(5-butanoyl-2-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-(3-fluorophenyl)propyl]acetamide	554132: Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay	ic50	0.0001	uM
N-[(1S)-3-[(1R,5S)-3-[5-(2,2-dimethylpropanoyl)-2-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-1-yl]-8-azabicyclo[3.2.1]octan-8-yl]-1-(3-fluorophenyl)propyl]acetamide	554132: Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay	ic50	0.0001	uM
methyl 3-[(1S,5R)-8-[(3S)-3-acetamido-3-(3-fluorophenyl)propyl]-8-azabicyclo[3.2.1]octan-3-yl]-2-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridine-5-carboxylate	554132: Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay	ic50	0.0001	uM
N-[(1S)-1-(3-fluorophenyl)-3-[(1R,5S)-3-[2-methyl-5-(2-methylpropanoyl)-6,7-dihydro-4H-imidazo[4,5-c]pyridin-1-yl]-8-azabicyclo[3.2.1]octan-8-yl]propyl]acetamide	554132: Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay	ic50	0.0001	uM
N-[1-[(3R)-3-(3,5-dichlorophenyl)-3-(1-methylsulfonylpiperidin-4-yl)propyl]piperidin-4-yl]-N-ethyl-2-(4-methylsulfonylphenyl)acetamide	645643: Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells	ic50	0.0001	uM
N-ethyl-2-(4-methylsulfonylphenyl)-N-[1-[(3R)-3-phenyl-3-[1-(trifluoromethylsulfonyl)piperidin-4-yl]propyl]piperidin-4-yl]acetamide	645643: Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells	ic50	0.0001	uM
N-[1-[(3R)-3-(3,5-dimethylphenyl)-3-(1-methylsulfonylpiperidin-4-yl)propyl]piperidin-4-yl]-N-ethyl-2-(4-methylsulfonylphenyl)acetamide	645643: Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells	ic50	0.0001	uM
5-N-[(3R)-3-[4-[4-methoxy-N-[(4-methyl-3-pyridinyl)methyl]anilino]piperidin-1-yl]butyl]-4,6-dimethyl-2-N-propan-2-ylpyridine-2,5-dicarboxamide	635152: Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay	ic50	0.0001	uM
6-chloro-2,4-dimethyl-N-[(3R)-3-[4-[pyridin-3-ylcarbamoyl(thiophen-3-ylmethyl)amino]piperidin-1-yl]butyl]pyridine-3-carboxamide	696934: Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay	ic50	0.0001	uM
[4-[4-[(E)-C-(4-bromophenyl)-N-ethoxycarbonimidoyl]piperidin-1-yl]-4-methylpiperidin-1-yl]-(2,6-dimethyl-4-pyridin-4-ylphenyl)methanone	42506: Inhibition of RANTES binding to the human C-C chemokine receptor type 5 (CCR5)	ki	0.0001	uM
1-[[(3S,4S)-1-(cyclohexylmethyl)-4-phenylpyrrolidin-3-yl]methyl]-4-[3-[4-(2H-tetrazol-5-yl)phenyl]propyl]piperidin-4-ol	352100: Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells	ic50	0.0002	uM
(5E)-8-[4-(2-butoxyethoxy)phenyl]-1-[(1-methylpyrazol-4-yl)methyl]-N-[4-[(S)-(3-propylimidazol-4-yl)methylsulfinyl]phenyl]-3,4-dihydro-2H-1-benzazocine-5-carboxamide	261802: Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5	ic50	0.0002	uM
(5E)-8-[4-(2-butoxyethoxy)phenyl]-1-(2-methylpropyl)-N-[4-[(S)-(4-propyl-1,2,4-triazol-3-yl)methylsulfinyl]phenyl]-3,4-dihydro-2H-1-benzazocine-5-carboxamide	261802: Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5	ic50	0.0002	uM
6-chloro-N-[(3R)-3-[4-[4-methoxy-N-[(4-methyl-3-pyridinyl)methyl]anilino]piperidin-1-yl]butyl]-2,4-dimethylpyridine-3-carboxamide	635152: Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay	ic50	0.0002	uM
4,4-difluoro-N-[(1S)-3-[(1S,5R)-3-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]cyclohexane-1-carboxamide	1370975: Inhibition of CCR5 in human TZM-bl cells infected with HIV1 Bal R5 assessed as antiviral activity by measuring reduction in viral infection pre-incubated with cells followed by viral infection measured after 3 days by luciferase reporter gene assay	ic50	0.0002	uM
(2R)-2-[(3S,4S)-3-[[4-(2-benzyl-1,3-thiazol-5-yl)piperidin-1-yl]methyl]-4-phenylpyrrolidin-1-yl]-3-cyclopropylpropanoic acid	352100: Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells	ic50	0.0002	uM
(2R)-2-[(3S,4S)-3-[[4-(2-benzyl-1,3-thiazol-5-yl)piperidin-1-yl]methyl]-4-phenylpyrrolidin-1-yl]-3-cyclobutylpropanoic acid	352100: Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells	ic50	0.0002	uM
(2R)-3-cyclobutyl-2-[(3S,4S)-3-(3-fluorophenyl)-4-[[4-[3-[4-(trifluoromethyl)phenyl]propyl]piperidin-1-yl]methyl]pyrrolidin-1-yl]propanoic acid	352100: Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells	ic50	0.0002	uM
(2R)-3-cyclobutyl-2-[(3S,4S)-3-[[4-[3,3-difluoro-3-(4-fluorophenyl)propyl]piperidin-1-yl]methyl]-4-phenylpyrrolidin-1-yl]propanoic acid	352100: Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells	ic50	0.0002	uM
1-[[(3S,4S)-1-(cyclohexylmethyl)-4-phenylpyrrolidin-3-yl]methyl]-4-[3-[4-(1-methyltetrazol-5-yl)phenyl]propyl]piperidin-4-ol	42380: Displacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranes	ic50	0.0002	uM
2-[(3S)-3-[[4-(2-benzyl-1,3-thiazol-5-yl)piperidin-1-yl]methyl]-4-phenylpyrrolidin-1-yl]-3-cyclobutylpropanoic acid	42495: Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand	ic50	0.0002	uM
2-[(3S)-3-[[4-(2-benzyl-1,3-thiazol-5-yl)piperidin-1-yl]methyl]-4-phenylpyrrolidin-1-yl]-3-cyclopropylpropanoic acid	42495: Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand	ic50	0.0002	uM
N-[(1S)-3-[4-[benzylcarbamoyl(ethyl)amino]piperidin-1-yl]-1-phenylbutyl]cyclobutanecarboxamide	393050: Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay	ic50	0.0002	uM
(4-nitrophenyl)methyl N-[1-[[(3S,4S)-1-benzoyl-4-phenylpyrrolidin-3-yl]methyl]piperidin-4-yl]-N-prop-2-enylcarbamate	42496: Inhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cells	ic50	0.0002	uM
(4-nitrophenyl)methyl N-[1-[[(3S,4S)-1-(cyclopentanecarbonyl)-4-phenylpyrrolidin-3-yl]methyl]piperidin-4-yl]-N-prop-2-enylcarbamate	42496: Inhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cells	ic50	0.0002	uM

CTD chemical–gene interactions

59 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Maraviroc	decreases reaction, increases expression, affects binding, decreases activity	3
Benzo(a)pyrene	affects methylation, increases expression	2
Eugenol	increases expression	2
Nickel	affects expression, increases expression, decreases reaction	2
Simvastatin	decreases expression, decreases reaction, increases expression	2
GSK-J4	decreases expression	1
isopentenyl pyrophosphate	decreases expression	1
triphenyl phosphate	affects expression	1
captax	increases expression	1
trichostatin A	affects expression, decreases reaction	1
proanthocyanidin	decreases expression	1
indole-3-carbinol	increases expression	1
3-chlorophenol	decreases expression	1
2,4-dinitrofluorobenzene sulfonic acid	increases expression	1
di-n-butylphosphoric acid	affects expression	1
CGP 52608	affects binding, increases reaction	1
2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one	affects binding, decreases reaction, increases activity, increases expression	1
enniatins	decreases expression	1
cirsimarin	decreases expression	1
TAK 779	affects binding, decreases reaction	1
N-(oxo-5,6-dihydrophenanthridin-2-yl)-N,N-dimethylacetamide hydrochloride	decreases expression, decreases reaction, affects cotreatment	1
Ancriviroc	affects binding, decreases reaction	1
bardoxolone methyl	increases expression, increases reaction	1
vicriviroc	affects binding, decreases reaction	1
aplaviroc	affects binding, decreases reaction	1
PF 232798	affects binding, decreases activity	1
bisphenol S	decreases methylation	1
gardiquimod	increases expression, decreases reaction	1
(+)-JQ1 compound	decreases expression	1
Air Pollutants	increases abundance, increases expression	1

ChEMBL screening assays

409 unique, capped per target: 243 binding, 166 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1000791	Binding	Displacement of [125I]gp-120 from human CCR5 receptor expressed in CHO cells	Isolation and structure of antagonists of chemokine receptor (CCR5). — *J Nat Prod*
CHEMBL1055686	Functional	Inhibition of human CCR5 expressed in mouse B300-19 cells assessed as inhibition of RANTES-induced calcium flux at 10 uM	Synthesis, biological evaluation, and metabolic stability of acrylamide derivatives as novel CCR3 antagonists. — *Bioorg Med Chem*

Cellosaurus cell lines

61 cell lines: 45 cancer cell line, 6 spontaneously immortalized cell line, 5 transformed cell line, 5 induced pluripotent stem cell

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_0C87	MOCHA	Cancer cell line	Male
CVCL_1D98	HOS-CD4-CCR5	Cancer cell line	Female
CVCL_1E08	GHOST(3).R3/X4/R5	Cancer cell line	Female
CVCL_1E10	GHOST(3).X4/R5	Cancer cell line	Female
CVCL_1E15	3T3.T4.CCR5	Transformed cell line	Male
CVCL_1E17	GHOST(3).Hi-5	Cancer cell line	Female
CVCL_1F85	U373-MAGI-CCR5	Cancer cell line	Male
CVCL_1G50	Cf2Th-CCR5	Spontaneously immortalized cell line	Female
CVCL_1H19	HOS-CCR5	Cancer cell line	Female
CVCL_1H21	HeLa-P4-R5 MAGI	Cancer cell line	Female

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for CCR5 across ~30M SureChEMBL compounds — explore on Sugi Predict.