C3AR1

Summary

C3AR1 (complement C3a receptor 1, HGNC:1319) is a protein-coding gene on chromosome 12p13.31, encoding C3a anaphylatoxin chemotactic receptor (Q16581). Receptor for the chemotactic and inflammatory peptide anaphylatoxin C3a, stimulating chemotaxis, granule enzyme release and superoxide anion production.

C3a is an anaphylatoxin released during activation of the complement system. The protein encoded by this gene is an orphan G protein-coupled receptor for C3a. Binding of C3a by the encoded receptor activates chemotaxis, granule enzyme release, superoxide anion production, and bacterial opsonization.

Source: NCBI Gene 719 — RefSeq curated summary.

At a glance

• GWAS associations: 5
• Clinical variants (ClinVar): 85 total — 1 likely-pathogenic
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_004054

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:1319
Approved symbol	C3AR1
Name	complement C3a receptor 1
Location	12p13.31
Locus type	gene with protein product
Status	Approved
Aliases	C3AR, AZ3B
Ensembl gene	ENSG00000171860
Ensembl biotype	protein_coding
OMIM	605246
Entrez	719

Gene structure

Transcript identifiers

Ensembl transcripts: 5 — 5 protein_coding

ENST00000307637, ENST00000546241, ENST00000904894, ENST00000904895, ENST00000962850

RefSeq mRNA: 3 — MANE Select: NM_004054 NM_001326475, NM_001326477, NM_004054

CCDS: CCDS8588

Canonical transcript exons

ENST00000307637 — 2 exons

Exon	Start	End
ENSE00001163543	8056844	8060195
ENSE00001252999	8066278	8066359

Expression profiles

Bgee: expression breadth ubiquitous, 262 present calls, max score 93.48.

FANTOM5 (CAGE): breadth broad, TPM avg 16.5146 / max 634.8944, expressed in 562 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
129315	14.1155	521
129316	2.2014	323
129317	0.1977	103

Top tissues by expression

290 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
monocyte	CL:0000576	93.48	gold quality
mononuclear cell	CL:0000842	93.25	gold quality
leukocyte	CL:0000738	93.03	gold quality
trabecular bone tissue	UBERON:0002483	92.54	gold quality
decidua	UBERON:0002450	91.61	gold quality
amniotic fluid	UBERON:0000173	91.36	gold quality
bone marrow	UBERON:0002371	91.15	gold quality
blood	UBERON:0000178	90.35	gold quality
bone element	UBERON:0001474	90.27	gold quality
vermiform appendix	UBERON:0001154	89.37	gold quality
lower lobe of lung	UBERON:0008949	89.36	gold quality
bone marrow cell	CL:0002092	87.68	gold quality
superficial temporal artery	UBERON:0001614	87.62	gold quality
placenta	UBERON:0001987	87.53	gold quality
heart right ventricle	UBERON:0002080	87.37	gold quality
layer of synovial tissue	UBERON:0007616	87.15	gold quality
myocardium	UBERON:0002349	86.15	silver quality
germinal epithelium of ovary	UBERON:0001304	86.10	gold quality
caecum	UBERON:0001153	85.87	gold quality
synovial joint	UBERON:0002217	85.83	gold quality
parietal pleura	UBERON:0002400	85.76	gold quality
pleura	UBERON:0000977	85.33	gold quality
gall bladder	UBERON:0002110	84.84	gold quality
granulocyte	CL:0000094	83.98	gold quality
visceral pleura	UBERON:0002401	83.85	gold quality
dorsal motor nucleus of vagus nerve	UBERON:0002870	83.62	gold quality
mammary duct	UBERON:0001765	83.50	gold quality
endothelial cell	CL:0000115	83.27	silver quality
right coronary artery	UBERON:0001625	83.19	gold quality
CA1 field of hippocampus	UBERON:0003881	83.18	silver quality

Single-cell (SCXA)

Detected in 6 experiment(s), a significant marker in 5.

Experiment	Marker?	Max mean expression
E-MTAB-6678	yes	38.58
E-GEOD-134144	yes	29.49
E-ANND-3	yes	26.09
E-MTAB-8498	yes	10.01
E-GEOD-137537	yes	5.41
E-MTAB-7606	no	909.98

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AP1, ETS1, TAL1

miRNA regulators (miRDB)

24 targeting C3AR1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-6740-5P	100.00	65.64	932
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-4534	99.99	66.58	1907
HSA-MIR-5696	99.98	72.36	4487
HSA-MIR-8075	99.97	67.20	962
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-651-3P	99.94	73.48	5177
HSA-MIR-10523-5P	99.91	69.22	2038
HSA-MIR-10395-5P	99.86	67.35	676
HSA-MIR-4639-5P	99.81	67.37	1028
HSA-MIR-33A-3P	99.70	70.27	3362
HSA-MIR-580-3P	99.67	69.23	1841
HSA-MIR-4728-3P	99.47	68.94	981
HSA-MIR-6513-5P	99.43	67.81	1071
HSA-MIR-942-5P	99.41	68.40	1977
HSA-MIR-361-3P	99.19	66.45	1381
HSA-MIR-6506-5P	99.04	65.66	1386
HSA-MIR-4272	98.76	68.74	1810
HSA-MIR-619-5P	98.57	64.97	1988
HSA-MIR-6801-3P	98.04	64.64	805
HSA-MIR-6881-3P	98.04	68.24	1777
HSA-MIR-6810-3P	97.96	64.57	1023
HSA-MIR-5196-3P	97.57	65.98	979
HSA-MIR-3192-5P	96.98	65.76	1926

Literature-anchored findings (GeneRIF, showing 40)

• results indicate that normal human hematopoietic stem and progenitor cells express functional C3aR and that the C3aR-C3a axis sensitizes the responses of these cells to SDF-1 (PMID:12511407)
• Sulfation of tyrosine 174 in the human C3a receptor is essential for binding of C3a anaphylatoxin. (PMID:12871936)
• determination of whether the levels of complement factors C3a, C4a, and C5a are elevated at the site of inflammation in chronic obstructive pulmonary disease and in asthma (PMID:15039137)
• Complement receptor 3 (CR3) is involved in the binding of Leishmania promastigote surface antigen-2 leucine-rich repeat motifs to macrophages, an interaction which can be blocked by anti-CR3 antibodies. (PMID:15067069)
• C3a receptor is highly expressed in primary renal proximal tubular epithelial cells in studies that define a new pathway by which complement activation may directly modulate the renal response to immunologic injury. (PMID:15356170)
• C3aR is expressed on plasmacytoid dendritic cells. (PMID:16778800)
• endothelial cells and subendothelial smooth muscle cells express both C3aR and C5aR (PMID:17234193)
• C3a receptor may be used as a unique biomarker of diagnosis and disease activity in patients with lupus nephritis. (PMID:17472841)
• In stenotic valves, expression of C3aR mRNA was upregulated (PMID:17498719)
• on the basis of the location of C3aR and C5aR, C5aR may play a role in activation of inflammatory cells, whereas C3aR may mediate mucus secretion and mucosal swelling in allergic nasal mucosa, especially severe persistent allergic nasal mucosa (PMID:18538384)
• Significantly more transcripts encoding alternative pathway components factor B, C3 and properdin, and C3a receptor and C5a receptor were detected in grade 3 versus grade 0 or 1 biopsies of human cardiac allografts. (PMID:19005416)
• Mutant gonococci lacking the pilin glycan did not bind to the I-domain when it is in a closed, low-affinity conformation and cannot induce an active conformation to complement receptor 3 during pex cell challenge. (PMID:21371235)
• shows that both beta-arrestin-1 and beta-arrestin-2 play a novel and shared role in inhibiting G protein-dependent ERK1/2 phosphorylation. These findings reveal a new level of complexity for C3aR regulation by beta-arrestins in human mast cells (PMID:21589858)
• a new level of complexity for C3aR regulation (PMID:21799898)
• Complement C3a receptor activation contributes to the pathogenesis of preeclampsia. (PMID:22868393)
• significantly decreased expression of C3aR mRNA and protein expression in placentas with preeclampsia compared to controls (PMID:22901903)
• study demonstrates that although C3a causes phosphorylation of its receptor at multiple sites, Ser459, Thr463, Ser465, Thr466 and Ser470 participate in C3aR desensitization (PMID:23077507)
• functional regulation of C3aR by NHERFs in human mast cells (PMID:23284683)
• C3aR and CD46 activation via intrinsic generation of their respective ligands is an integral part of human Th1 (but not Th2) immunity. (PMID:24321396)
• In patients with IgAN, urinary and renal C3a and C5a and renal expression of C3aR and C5aR are significantly correlated with the activity and severity of renal injury. (PMID:24327134)
• The obesity-induced down-regulation of complement C3 and C3aR which is specific to subcutaneous adipose tissue. (PMID:24743347)
• High C3aR1 expression is associated with acute myeloid leukemia-M2. (PMID:25426664)
• these findings suggest a critical role for C3a through autocrine/paracrine induction of C3aR in the pathogenesis of cigarette smoke-induced sterile inflammation and provide new therapeutic targets for the treatment of emphysema. (PMID:25465103)
• Observed a positive correlation between the expression of anaphylatoxin-receptors C3aR and C5aR with platelet activation in patients with coronary artery disease. (PMID:25544179)
• Medulloblastoma cells express C3aR, and siRNA-mediated knockdown of C3aR inhibits proliferation of these cells in vitro. (PMID:25603857)
• Studies indicate that the complement response lie the active fragments, C3a and C5a, acting through their specific receptors, C3aR, C5aR1 and C5aR2 to direct the cellular response to inflammation. (PMID:28576324)
• This study aimed to investigate the role of C3aR and C5aR in these two diseases…Our data indicates that increased C3aR expression may lead to over activation of the Th17 cell response and may therefore contribute to the pathogenesis of Behcet’s disease (BD) and Vogt-Koyanagi-Harada disease (VKH). (PMID:29138505)
• Anaphylatoxin C3a has novel roles involved in regulating platelet function and thrombus formation. (PMID:29802205)
• this study shows that C3AR1 expression on M2 macrophages is down-regulated by stimulating the histamine H4 receptor and the IL-4 receptor (PMID:30032131)
• C3aR-positive cells are found more often in patients with inflammatory cardiomyopathy. The relevance of C3aR-positive cells in patients with non-ischaemic cardiomyopathy should be further evaluated as potential predictors or modulators of adverse cardiac remodelling, the substrate of progressive heart failure. (PMID:30168657)
• This study demonstrate a crucial role for activation of the C3-C3aR network in mediating neuroinflammation and tau pathology. (PMID:30415998)
• C3aR has roles in platelet function, thrombus formation and in vivo hemostasis (PMID:30597512)
• The Role of Complement C3a Receptor in Stroke. (PMID:31102134)
• Peptide/Receptor Co-evolution Explains the Lipolytic Function of the Neuropeptide TLQP-21. (PMID:31484069)
• Deficiency of C3a receptor attenuates the development of diabetic nephropathy. (PMID:31798904)
• Results found that C3a-C3aR signaling in carcinoma associated fibroblasts (CAFs) facilitates the metastasis of breast cancer. Mechanically, C3a-C3aR signaling augments pro-metastatic cytokine secretion and extracellular matrix components expression of CAFs via the activation of PI3K-AKT signaling. (PMID:31931851)
• The validation experiments showed that those variants in CCR5 and C3AR1 significantly increased the rise of intracellular calcium and the variant in CCR5 profoundly enhanced proliferative capacity of human pulmonary artery smooth muscle cells. (PMID:32159364)
• Down-Regulation of C3aR/C5aR Inhibits Cell Proliferation and EMT in Hepatocellular Carcinoma. (PMID:33176600)
• Changes in VGF and C3aR1 gene expression in human adipose tissue in obesity. (PMID:33306149)
• Autoantibodies against C5aR1, C3aR1, CXCR3, and CXCR4 are decreased in primary Sjogren’s syndrome. (PMID:33446393)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	c3ar1	ENSDARG00000031749
mus_musculus	C3ar1	ENSMUSG00000040552
rattus_norvegicus	C3ar1	ENSRNOG00000009211

Paralogs (8): C5AR2 (ENSG00000134830), GPR32 (ENSG00000142511), FPR2 (ENSG00000171049), FPR1 (ENSG00000171051), CMKLR1 (ENSG00000174600), FPR3 (ENSG00000187474), C5AR1 (ENSG00000197405), GPR33 (ENSG00000214943)

Protein

Protein identifiers

C3a anaphylatoxin chemotactic receptor — Q16581 (reviewed: Q16581)

All UniProt accessions (3): Q16581, A8K2H7, F5GZE6

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for the chemotactic and inflammatory peptide anaphylatoxin C3a, stimulating chemotaxis, granule enzyme release and superoxide anion production. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors, such as adenylate cyclase. C3AR1 is coupled to G(i)/G(o) (GNAI1 or GNAO1) G alpha proteins and mediates inhibition of adenylate cyclase.

Subunit / interactions. Interacts with VGF-derived peptide TLQP-21. Interacts (when phosphorylated) with ARRB1; the interaction is associated with internalization of the receptor and short-term desensitization to the ligand.

Subcellular location. Cell membrane.

Tissue specificity. Widely expressed in several differentiated hematopoietic cell lines, in the lung, spleen, ovary, placenta, small intestine, throughout the brain, heart, and endothelial cells (PubMed:8605247, PubMed:8765043, Ref.3). Mostly expressed in lymphoid tissues (PubMed:8605247, PubMed:8765043, Ref.3).

Post-translational modifications. Phosphorylation of the C-terminus by GRK2 or GRK3 promotes association with beta-arrestin (ARRB1), leading to receptor desensitization and negative regulation of G-protein coupled receptor signaling. Among the sulfation sites Tyr-174 is essential for binding of C3a anaphylatoxin. O-glycosylated.

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

RefSeq proteins (3): NP_001313404, NP_001313406, NP_004045* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000826	Formyl_rcpt-rel	Family
IPR001644	Anaphtx_C3AR1	Family
IPR002234	Anphylx_rcpt_C3a/C5a1-2	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (63 total): helix 18, topological domain 8, transmembrane region 7, modified residue 7, strand 7, turn 6, glycosylation site 3, disulfide bond 2, sequence conflict 2, chain 1, sequence variant 1, mutagenesis site 1

Structure

Experimental structures (PDB)

18 structures.

PDB	Method	Resolution (Å)
9IPV	ELECTRON MICROSCOPY	2.53
9KVP	ELECTRON MICROSCOPY	2.79
8IA8	ELECTRON MICROSCOPY	2.86
8ZWG	ELECTRON MICROSCOPY	2.87
8I95	ELECTRON MICROSCOPY	2.88
8HK2	ELECTRON MICROSCOPY	2.9
8ZWF	ELECTRON MICROSCOPY	3
8J6D	ELECTRON MICROSCOPY	3.1
8I9L	ELECTRON MICROSCOPY	3.18
8I97	ELECTRON MICROSCOPY	3.19
8HK3	ELECTRON MICROSCOPY	3.2
8I9S	ELECTRON MICROSCOPY	3.26
9KUT	ELECTRON MICROSCOPY	3.29
9KZ2	ELECTRON MICROSCOPY	3.43
9IPY	ELECTRON MICROSCOPY	3.5
9ISI	ELECTRON MICROSCOPY	3.56
8I9A	ELECTRON MICROSCOPY	3.57
8JA3	ELECTRON MICROSCOPY	3.94

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q16581-F1	68.68	0.36

Antibody-complex structures (SAbDab): 11 — 8HK2, 8HK3, 8I95, 8I97, 8I9A, 8I9L, 8I9S, 8IA8, 8J6D, 8JA3, 9KZ2

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 (7): 174, 184, 318, 459, 463, 465, 466

Disulfide bonds (2): 95–172, 121–355

Glycosylation sites (3): 9, 194, 266

Mutagenesis-validated functional residues (1):

Position	Phenotype
449–481	abolished ability to promote degranulation of leukocytes.

Function

Pathways and Gene Ontology

Reactome pathways

18 pathways

ID	Pathway
R-HSA-375276	Peptide ligand-binding receptors
R-HSA-418594	G alpha (i) signalling events
R-HSA-6798695	Neutrophil degranulation
R-HSA-9660826	Purinergic signaling in leishmaniasis infection
R-HSA-977606	Regulation of Complement cascade
R-HSA-162582	Signal Transduction
R-HSA-1643685	Disease
R-HSA-166658	Complement cascade
R-HSA-168249	Innate Immune System
R-HSA-168256	Immune System
R-HSA-372790	Signaling by GPCR
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)
R-HSA-388396	GPCR downstream signalling
R-HSA-500792	GPCR ligand binding
R-HSA-5663205	Infectious disease
R-HSA-9658195	Leishmania infection
R-HSA-9664424	Cell recruitment (pro-inflammatory response)
R-HSA-9824443	Parasitic Infection Pathways

MSigDB gene sets: 366 (showing top): GSE18804_SPLEEN_MACROPHAGE_VS_COLON_TUMORAL_MACROPHAGE_UP, REACTOME_INNATE_IMMUNE_SYSTEM, MCLACHLAN_DENTAL_CARIES_UP, GOBP_MYELOID_LEUKOCYTE_MIGRATION, GOBP_CIRCULATORY_SYSTEM_PROCESS, GOBP_CELL_CHEMOTAXIS, GOBP_INFLAMMATORY_RESPONSE, GOCC_VACUOLAR_MEMBRANE, GOCC_SECRETORY_GRANULE, MODULE_64, GOBP_POSITIVE_REGULATION_OF_VASCULATURE_DEVELOPMENT, GAUSSMANN_MLL_AF4_FUSION_TARGETS_A_UP, MODULE_128, GOBP_POSITIVE_REGULATION_OF_CYTOKINE_PRODUCTION, GAURNIER_PSMD4_TARGETS

GO Biological Process (16): complement receptor mediated signaling pathway (GO:0002430), chemotaxis (GO:0006935), inflammatory response (GO:0006954), G protein-coupled receptor signaling pathway (GO:0007186), adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway (GO:0007193), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), positive regulation of cytosolic calcium ion concentration (GO:0007204), blood circulation (GO:0008015), positive regulation of vascular endothelial growth factor production (GO:0010575), positive regulation of macrophage chemotaxis (GO:0010759), calcium-mediated signaling (GO:0019722), positive regulation of angiogenesis (GO:0045766), positive regulation of neutrophil chemotaxis (GO:0090023), positive regulation of immune system process (GO:0002684), signal transduction (GO:0007165), complement component C5a signaling pathway (GO:0038178)

GO Molecular Function (4): complement component C3a receptor activity (GO:0004876), complement component C5a receptor activity (GO:0004878), G protein-coupled receptor activity (GO:0004930), complement receptor activity (GO:0004875)

GO Cellular Component (4): plasma membrane (GO:0005886), azurophil granule membrane (GO:0035577), specific granule membrane (GO:0035579), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-13 pathways:

Category	Pathways
Innate Immune System	2
Signaling by GPCR	2
Class A/1 (Rhodopsin-like receptors)	1
GPCR downstream signalling	1
Cell recruitment (pro-inflammatory response)	1
Complement cascade	1
Immune System	1
Signal Transduction	1
GPCR ligand binding	1
Disease	1
Parasitic Infection Pathways	1
Leishmania infection	1
Infectious disease	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor signaling pathway	3
complement receptor mediated signaling pathway	2
complement receptor activity	2
transmembrane signaling receptor activity	2
secretory granule membrane	2
immune response-activating cell surface receptor signaling pathway	1
response to chemical	1
taxis	1
defense response	1
G protein-coupled receptor activity	1
signal transduction	1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase inhibitor activity	1
phospholipase C activator activity	1
regulation of biological quality	1
circulatory system process	1
positive regulation of cytokine production	1
vascular endothelial growth factor production	1
regulation of vascular endothelial growth factor production	1
positive regulation of leukocyte chemotaxis	1
regulation of macrophage chemotaxis	1
macrophage chemotaxis	1
regulation of granulocyte chemotaxis	1
positive regulation of macrophage migration	1
intracellular signaling cassette	1
angiogenesis	1
regulation of angiogenesis	1
positive regulation of vasculature development	1
neutrophil chemotaxis	1
positive regulation of granulocyte chemotaxis	1
regulation of neutrophil chemotaxis	1
positive regulation of neutrophil migration	1
immune system process	1
regulation of immune system process	1
positive regulation of biological process	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1

Protein interactions and networks

STRING

1988 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
C3AR1	C4A	P01028	987
C3AR1	C3	P01024	983
C3AR1	C5AR1	P21730	970
C3AR1	C4A	P01028	770
C3AR1	CFH	P08603	770
C3AR1	C5	P01031	758
C3AR1	C1QA	P02745	753
C3AR1	ITGB2	P05107	690
C3AR1	IL1B	P01584	683
C3AR1	FCER1G	P30273	683
C3AR1	VSIG4	Q9Y279	679
C3AR1	C1QBP	Q07021	678
C3AR1	CD46	P15529	667
C3AR1	CD55	P08174	663
C3AR1	CR1	P17927	655

IntAct

120 interactions, top by confidence:

A	B	Type	Score
C3AR1	TMEM120B	psi-mi:“MI:0914”(association)	0.530
C3AR1	MAST2	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	LNX2	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	MAGI3	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	DLG1	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	SYNJ2BP	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	DLG4	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	SNX27	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	PDZD2	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	MAGI2	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	DLG2	psi-mi:“MI:0407”(direct interaction)	0.440
ARHGEF11	C3AR1	psi-mi:“MI:0407”(direct interaction)	0.440
DLG3	C3AR1	psi-mi:“MI:0407”(direct interaction)	0.440
PDZD7	C3AR1	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	MAGI1	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	TAMALIN	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	ARHGEF12	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	HTRA1	psi-mi:“MI:0407”(direct interaction)	0.440
RHPN1	C3AR1	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	HTRA4	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	RADIL	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	DLG3	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	PTPN3	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	ARHGAP21	psi-mi:“MI:0407”(direct interaction)	0.440
C3AR1	GOPC	psi-mi:“MI:0407”(direct interaction)	0.440
APBA3	C3AR1	psi-mi:“MI:0407”(direct interaction)	0.440

BioGRID (170): RDH14 (Affinity Capture-MS), PTPN2 (Affinity Capture-MS), PEX13 (Affinity Capture-MS), VEZT (Affinity Capture-MS), GOLGA5 (Affinity Capture-MS), ELOVL2 (Affinity Capture-MS), DGAT1 (Affinity Capture-MS), PTPLB (Affinity Capture-MS), ATP2B3 (Affinity Capture-MS), ZDHHC17 (Affinity Capture-MS), ZDHHC21 (Affinity Capture-MS), UBE2Q1 (Affinity Capture-MS), ZFPL1 (Affinity Capture-MS), CERS5 (Affinity Capture-MS), TMEM56 (Affinity Capture-MS)

ESM2 similar proteins: O00421, O02824, O09047, O15218, O18982, O55193, O55197, O70342, O88416, O88680, O89039, O97663, O97664, O97969, P0C7U4, P11613, P18130, P25089, P25106, P31389, P31392, P33766, P35348, P35351, P35374, P41597, P43142, P46091, P49685, P50052, P51683, P56412, P56485, P97718, Q05394, Q0II78, Q0VDU3, Q16581, Q28929, Q2WED0

Diamond homologs: A1A5S3, E9QJ73, O08707, P29755, P32248, P33396, P49220, P79785, P97266, Q14330, Q149R9, Q16581, Q28553, Q3T0E9, Q3ZC80, Q4R613, Q58D85, Q5REI5, Q6IYF8, Q6TAC8, Q6Y1R5, Q8K1Z6, Q8NGA4, Q8VIH9, Q920E1, Q924T8, Q95N02, Q96P68, Q99PE3, Q9H1C0, A4FUQ5, B1PHQ8, B9VR26, O08565, O08790, O35210, O35786, O62747, O70129, O75388

SIGNOR signaling

6 interactions.

A	Effect	B	Mechanism
C3	“up-regulates activity”	C3AR1	binding
C3AR1	up-regulates	Chemotaxis
C3AR1	up-regulates	Inflammation
GRK2	“down-regulates activity”	C3AR1	phosphorylation
GRK3	“down-regulates activity”	C3AR1	phosphorylation
C3AR1	up-regulates	Vascular_Permeability

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 80 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.

Reactome pathways:

Pathway	Partners	Fold	FDR
Ras activation upon Ca2+ influx through NMDA receptor	5	54.9×	1e-06
Unblocking of NMDA receptors, glutamate binding and activation	5	52.3×	1e-06
Negative regulation of NMDA receptor-mediated neuronal transmission	5	52.3×	1e-06
Assembly and cell surface presentation of NMDA receptors	10	48.8×	8e-13
Dopamine Neurotransmitter Release Cycle	5	47.7×	1e-06
Long-term potentiation	5	45.8×	2e-06
Neurexins and neuroligins	10	37.9×	7e-12
Protein-protein interactions at synapses	6	30.6×	1e-06

GO biological processes:

GO term	Partners	Fold	FDR
establishment or maintenance of epithelial cell apical/basal polarity	10	74.5×	2e-14
protein localization to synapse	5	49.1×	5e-06
receptor clustering	6	48.0×	4e-07
regulation of postsynaptic membrane neurotransmitter receptor levels	7	44.5×	4e-08
bicellular tight junction assembly	5	21.2×	2e-04
cell-cell adhesion	9	11.7×	6e-06
protein-containing complex assembly	7	10.2×	2e-04
protein localization to plasma membrane	7	9.8×	3e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	1
Uncertain significance	72
Likely benign	7
Benign	2

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
222958	NM_004054.4(C3AR1):c.355_356dup (p.Asp119fs)	Likely pathogenic

SpliceAI

163 predictions. Top by Δscore:

Variant	Effect	Δscore
12:8060193:CTT:C	acceptor_gain	1.0000
12:8060194:TT:T	acceptor_gain	1.0000
12:8060196:C:CC	acceptor_gain	1.0000
12:8060191:AACTT:A	acceptor_gain	0.9900
12:8060195:TC:T	acceptor_loss	0.9800
12:8060196:C:A	acceptor_loss	0.9800
12:8066276:A:AC	donor_gain	0.9800
12:8066277:C:CC	donor_gain	0.9800
12:8066296:G:C	donor_gain	0.9800
12:8060192:ACTTC:A	acceptor_gain	0.9700
12:8066272:TCTTA:T	donor_loss	0.9700
12:8066273:CTTAC:C	donor_loss	0.9700
12:8066274:TTAC:T	donor_loss	0.9700
12:8066275:TACCA:T	donor_loss	0.9700
12:8066276:A:G	donor_loss	0.9700
12:8060193:CTTCT:C	acceptor_gain	0.9600
12:8060198:G:C	acceptor_loss	0.9500
12:8060199:C:CT	acceptor_gain	0.9200
12:8060200:A:T	acceptor_gain	0.8800
12:8066352:G:C	donor_gain	0.8200
12:8066306:TCAGC:T	donor_gain	0.8100
12:8060756:T:C	donor_gain	0.8000
12:8066305:TTCAG:T	donor_gain	0.8000
12:8066351:AG:A	donor_gain	0.7800
12:8066308:A:AC	donor_gain	0.7600
12:8060194:TTCTG:T	acceptor_gain	0.7500
12:8060206:A:AC	acceptor_gain	0.7500
12:8060206:A:C	acceptor_gain	0.7500
12:8060195:TCT:T	acceptor_gain	0.7400
12:8062058:G:C	donor_gain	0.7400

AlphaMissense

3167 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
12:8059835:G:C	S117R	0.997
12:8059835:G:T	S117R	0.997
12:8059837:T:G	S117R	0.997
12:8059859:A:C	S109R	0.995
12:8059859:A:T	S109R	0.995
12:8059861:T:G	S109R	0.995
12:8059922:C:A	W88C	0.993
12:8059922:C:G	W88C	0.993
12:8059747:A:G	W147R	0.992
12:8059747:A:T	W147R	0.992
12:8059865:A:C	F107L	0.992
12:8059865:A:T	F107L	0.992
12:8059867:A:G	F107L	0.992
12:8059924:A:G	W88R	0.992
12:8059924:A:T	W88R	0.992
12:8058902:A:C	S428R	0.991
12:8058902:A:T	S428R	0.991
12:8058904:T:G	S428R	0.991
12:8059018:A:G	W390R	0.991
12:8059018:A:T	W390R	0.991
12:8059151:G:C	F345L	0.990
12:8059151:G:T	F345L	0.990
12:8059153:A:G	F345L	0.990
12:8059827:C:G	R120P	0.988
12:8059902:C:G	C95S	0.988
12:8059903:A:T	C95S	0.988
12:8059995:A:G	L64P	0.988
12:8059028:A:C	F386L	0.987
12:8059028:A:T	F386L	0.987
12:8059030:A:G	F386L	0.987

dbSNP variants (sampled 300 via entrez): RS1000027217 (12:8063593 C>A,T), RS1000233626 (12:8057874 T>A), RS1001438024 (12:8064351 C>T), RS1001699412 (12:8067175 A>G), RS1001731278 (12:8066806 T>C), RS1001821141 (12:8062860 G>A), RS1002252473 (12:8064903 A>G), RS1002344240 (12:8056831 T>G), RS1002440872 (12:8063107 A>C,G), RS1002805214 (12:8056562 C>T), RS1002932711 (12:8065358 C>T), RS1003032720 (12:8059597 G>A,C,T), RS1003380487 (12:8061726 G>A,T), RS1003545821 (12:8063984 A>C,G), RS1003938570 (12:8066058 G>A)

Disease associations

OMIM: gene MIM:605246 | disease phenotypes: MIM:235400, MIM:615833

GenCC curated gene-disease

Mondo (3): prostate cancer (MONDO:0008315), hemolytic uremic syndrome, atypical, susceptibility to, 1 (MONDO:0009335), developmental and epileptic encephalopathy, 21 (MONDO:0014360)

Orphanet (4): Familial prostate cancer (Orphanet:1331), Atypical hemolytic uremic syndrome (Orphanet:2134), Shiga toxin-associated hemolytic uremic syndrome (Orphanet:90038), Non-specific early-onset epileptic encephalopathy (Orphanet:442835)

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

5 associations (top):

Study	Trait	p-value
GCST004608_175	Granulocyte percentage of myeloid white cells	4.000000e-09
GCST004633_22	Neutrophil percentage of white cells	4.000000e-09
GCST90002394_361	Monocyte percentage of white cells	1.000000e-12
GCST90002398_138	Neutrophil count	7.000000e-11
GCST90002399_328	Neutrophil percentage of white cells	2.000000e-11

EFO canonical traits (4, from GWAS)

EFO ID	Trait name
EFO:0007997	granulocyte percentage of myeloid white cells
EFO:0007990	neutrophil percentage of leukocytes
EFO:0007989	monocyte percentage of leukocytes
EFO:0004833	neutrophil count

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
D011471	Prostatic Neoplasms	C04.588.945.440.770; C12.100.500.260.750; C12.100.500.565.625; C12.200.294.260.750; C12.200.294.565.625; C12.200.758.409.750; C12.900.619.750

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4761 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 59,532 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1707	LOPERAMIDE HYDROCHLORIDE	4	59,532

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Complement peptide receptors

Most potent curated ligand interactions (18 total), top 18:

Ligand	Action	Affinity	Parameter
C3a	Agonist	9.62	pEC50
E7	Full agonist	8.7	pEC50
[125I]C3a (human)	Full agonist	8.4	pKd
compound 17 [PMID: 24257095]	Agonist	8.1	pEC50
Eu-DTPA-hC3a	Agonist	8.06	pKd
JR14a	Agonist	8.0	pIC50
compound 21 [PMID: 25259874]	Full agonist	7.7	pEC50
SB290157	Antagonist	7.6	pIC50
TLQP-21	Agonist	6.94	pIC50
YSFKPMPLaR	Full agonist	6.7	pEC50
SQ007-5	Partial agonist	6.65	pEC50
FLTChaAR	Antagonist	6.6	pIC50
FLPLAR	Full agonist	6.4	pEC50
C3a receptor agonist	Agonist	6.1	pIC50
Ac-RHYPLWR	Full agonist	5.96	pEC50
WWGKKYRASKLGLAR	Full agonist	5.9	pEC50
compound 4 [PMID: 25259874]	Antagonist	5.89	pIC50
casoxin C	Agonist	4.4	pIC50

ChEMBL bioactivities

420 potent at pChembl≥5 of 463 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.74	IC50	0.18	nM	CHEMBL1170042
9.10	IC50	0.8	nM	CHEMBL3342676
8.73	IC50	1.862	nM	CHEMBL2064013
8.70	IC50	2	nM	CHEMBL4470864
8.70	IC50	1.995	nM	CHEMBL4470864
8.70	IC50	2	nM	CHEMBL1170024
8.70	IC50	1.995	nM	CHEMBL1170024
8.52	IC50	3	nM	CHEMBL4445758
8.50	IC50	3.162	nM	CHEMBL4445758
8.40	IC50	4	nM	CHEMBL3342678
8.40	IC50	4	nM	CHEMBL4559976
8.40	IC50	4	nM	CHEMBL4576800
8.40	IC50	3.981	nM	CHEMBL4576800
8.40	IC50	3.981	nM	CHEMBL4559976
8.34	IC50	4.571	nM	CHEMBL2064017
8.30	IC50	5.012	nM	CHEMBL2064014
8.30	IC50	5.012	nM	CHEMBL3735507
8.30	IC50	5	nM	CHEMBL3735507
8.22	IC50	6	nM	CHEMBL3342677
8.22	IC50	6	nM	CHEMBL4459830
8.20	IC50	6.31	nM	CHEMBL3342688
8.20	IC50	6.31	nM	CHEMBL4459830
8.20	IC50	6.31	nM	CHEMBL4470864
8.15	IC50	7	nM	CHEMBL3342688
8.15	EC50	7	nM	CHEMBL3736108
8.15	EC50	7.079	nM	CHEMBL3736108
8.15	IC50	7	nM	CHEMBL4470864
8.12	EC50	7.586	nM	CHEMBL3736125
8.11	IC50	7.762	nM	CHEMBL2064015
8.10	IC50	7.943	nM	CHEMBL3342676
8.10	IC50	8	nM	CHEMBL3342676
8.10	EC50	8	nM	CHEMBL3736125
8.10	IC50	8	nM	CHEMBL4459627
8.10	IC50	7.943	nM	CHEMBL4459627
8.05	IC50	9	nM	CHEMBL3736108
8.04	IC50	9.12	nM	CHEMBL2064016
8.04	EC50	9.036	nM	CHEMBL5076900
8.03	IC50	9.333	nM	CHEMBL3736108
8.00	IC50	10	nM	CHEMBL389348
8.00	IC50	10	nM	CHEMBL3342686
8.00	IC50	10	nM	CHEMBL3342689
8.00	IC50	10	nM	CHEMBL3735614
8.00	IC50	10	nM	CHEMBL4459627
7.96	IC50	10.96	nM	CHEMBL2064012
7.96	IC50	11	nM	CHEMBL3342686
7.96	EC50	11.04	nM	CHEMBL5081621
7.92	IC50	12	nM	CHEMBL3342680
7.91	IC50	12.3	nM	CHEMBL2064021
7.90	IC50	12.59	nM	CHEMBL3342680
7.90	IC50	12.59	nM	CHEMBL1170026

PubChem BioAssay actives

419 with measured affinity, of 755 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
(2S)-2-[(2-benzhydryl-1,3-oxazole-4-carbonyl)amino]-5-(diaminomethylideneamino)pentanoic acid	1166390: Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a	ec50	<0.0001	uM
(2S)-2-[(2-benzhydryl-5-methyl-1,3-oxazole-4-carbonyl)amino]-5-(diaminomethylideneamino)pentanoic acid	1166390: Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a	ec50	<0.0001	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S,3S)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid	491629: Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting	ic50	0.0002	uM
(2S)-5-(diaminomethylideneamino)-2-[[2-(2,2-diphenylethylsulfanyl)acetyl]amino]pentanoic acid	1166389: Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay	ic50	0.0008	uM
(2S)-5-(diaminomethylideneamino)-2-[[2-(2,2-diphenylethoxy)acetyl]amino]pentanoic acid	1166389: Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay	ic50	0.0013	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-amino-4-oxobutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-[[(2S)-4-amino-1-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(1S)-4-carbamimidamido-1-carboxybutyl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-5-oxopentanoic acid	675744: Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay	ic50	0.0019	uM
(2S)-2-[(5-benzhydryl-3-methylthiophene-2-carbonyl)amino]-5-(diaminomethylideneamino)pentanoic acid	1582636: Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition	ic50	0.0020	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]acetyl]amino]hexanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoic acid	491629: Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting	ic50	0.0020	uM
(2S)-2-[[5-[bis(3-chlorophenyl)methyl]-3-methylthiophene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	1582628: Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay	ic50	0.0030	uM
(2S)-5-(diaminomethylideneamino)-2-[[2-(2,2-diphenylethylamino)acetyl]amino]pentanoic acid	1166389: Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay	ic50	0.0040	uM
(2S)-2-[[5-[cyclohexyl(phenyl)methyl]thiophene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	1582628: Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay	ic50	0.0040	uM
(2S)-2-[(5-benzhydrylthiophene-2-carbonyl)amino]-5-(diaminomethylideneamino)pentanoic acid	1582636: Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition	ic50	0.0040	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-3-carboxypropanoyl]amino]-6-aminohexanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoic acid	675744: Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay	ic50	0.0046	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-6-aminohexanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoic acid	675744: Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay	ic50	0.0050	uM
(2S)-2-[[2-[(1S,2S)-1-[(5-bromopyridine-3-carbonyl)amino]-2-methylbutyl]-1,3-oxazole-4-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	1262222: Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis	ic50	0.0050	uM
(2S)-5-(diaminomethylideneamino)-2-(5,5-diphenylpentanoylamino)pentanoic acid	1166389: Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay	ic50	0.0060	uM
(2S)-2-[[5-[bis(3-chlorophenyl)methyl]thiophene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	1582628: Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay	ic50	0.0060	uM
(2S)-2-[(2-benzhydryl-1H-imidazole-5-carbonyl)amino]-5-(diaminomethylideneamino)pentanoic acid	1166388: Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method	ic50	0.0063	uM
(2S)-5-(diaminomethylideneamino)-2-[[2-[(1S)-1-(1H-indole-3-carbonylamino)-3-methylbutyl]-1,3-oxazole-4-carbonyl]amino]pentanoic acid	1262223: Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay	ec50	0.0070	uM
(2S)-5-(diaminomethylideneamino)-2-[[2-[(1S,2S)-2-methyl-1-[[4-oxo-4-(4-phenylphenyl)butanoyl]amino]butyl]-1,3-oxazole-4-carbonyl]amino]pentanoic acid	1262223: Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay	ec50	0.0076	uM
(4S)-4-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxybutanoyl]amino]-5-[[(2S)-6-amino-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(1S)-4-carbamimidamido-1-carboxybutyl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-oxopentanoic acid	675744: Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay	ic50	0.0078	uM
(2S)-2-[[5-[bis(4-chlorophenyl)methyl]-3-methylthiophene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	1582636: Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition	ic50	0.0079	uM
(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid	1833592: Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay	ec50	0.0090	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-6-aminohexanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoic acid	675744: Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay	ic50	0.0091	uM
(2S)-5-(carbamoylamino)-2-[[2-(2,2-diphenylethoxy)acetyl]amino]pentanoic acid	1262231: Displacement of [125I]-C3a from human C3aR expressed in rat RBL-2H3 cells	ic50	0.0100	uM
(2S)-2-[(2-benzhydryl-5-methyl-1H-imidazole-4-carbonyl)amino]-5-(diaminomethylideneamino)pentanoic acid	1166388: Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method	ic50	0.0100	uM
(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid	1833592: Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay	ec50	0.0110	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]acetyl]amino]-6-aminohexanoyl]amino]-6-aminohexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-3-hydroxypropanoyl]amino]-6-aminohexanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoic acid	675744: Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay	ic50	0.0110	uM
(2S)-2-[(3-benzhydryl-1,2,4-oxadiazole-5-carbonyl)amino]-5-(diaminomethylideneamino)pentanoic acid	1166388: Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method	ic50	0.0120	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoic acid	675744: Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay	ic50	0.0123	uM
(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]-methylamino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid	491629: Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting	ic50	0.0126	uM
(2S)-5-(diaminomethylideneamino)-2-[[5-methyl-2-[(1S)-3-methyl-1-[(2-methylpropan-2-yl)oxycarbonylamino]butyl]-1,3-oxazole-4-carbonyl]amino]pentanoic acid	1262222: Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis	ic50	0.0140	uM
(2S)-2-[(2-benzhydryl-1H-imidazo[4,5-c]pyridin-4-yl)amino]-5-(diaminomethylideneamino)pentanoic acid	1393262: Agonist activity at C3aR in HMDM assessed as induction of Ca2+ release	ec50	0.0150	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-carboxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-3-hydroxypropanoyl]amino]-6-aminohexanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoic acid	675744: Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay	ic50	0.0155	uM
(2R)-2-[[5-[bis(3-chlorophenyl)methyl]furan-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	290701: Inhibition of human C3a receptor expressed on HMC1 cells by SPA assay	ic50	0.0158	uM
(2S)-5-(diaminomethylideneamino)-2-[[2-[(1S)-3-methyl-1-[(2-methylpropan-2-yl)oxycarbonylamino]butyl]-1,3-oxazole-4-carbonyl]amino]pentanoic acid	1262223: Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay	ec50	0.0190	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-3-hydroxypropanoyl]amino]-6-aminohexanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoic acid	675744: Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay	ic50	0.0234	uM
(4S)-4-[[(2S)-2-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(1S)-4-carbamimidamido-1-carboxybutyl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid	675744: Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay	ic50	0.0263	uM
(2S)-2-[[2-[(1S,2S)-1-benzamido-2-methylbutyl]-1,3-oxazole-4-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	1262222: Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis	ic50	0.0263	uM
(2S)-5-(diaminomethylideneamino)-2-[[2-[(1S,2S)-2-methyl-1-[(2-methylpropan-2-yl)oxycarbonylamino]butyl]-1,3-oxazole-4-carbonyl]amino]pentanoic acid	1262223: Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay	ec50	0.0269	uM
(2S)-2-[[5-[bis(4-chlorophenyl)methyl]thiophene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	1582628: Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay	ic50	0.0300	uM
(2S)-2-[(2-benzhydryl-1,5-dimethylimidazole-4-carbonyl)amino]-5-(diaminomethylideneamino)pentanoic acid	1166388: Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method	ic50	0.0310	uM
(2S)-2-[[5-[bis(4-fluorophenyl)methyl]-3-methylthiophene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	1582628: Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay	ic50	0.0316	uM
(2R)-2-[[5-[bis(3-fluorophenyl)methyl]furan-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	290701: Inhibition of human C3a receptor expressed on HMC1 cells by SPA assay	ic50	0.0316	uM
2-cyclohexyl-N-[1-[3-(2-fluoro-3-pyridinyl)propanoyl]piperidin-4-yl]-2-phenylacetamide	296256: Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin	ic50	0.0316	uM
(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid	1833592: Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay	ec50	0.0371	uM
(2S)-5-(diaminomethylideneamino)-2-[[5-[phenyl(pyridin-2-yl)methyl]thiophene-2-carbonyl]amino]pentanoic acid	1582628: Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay	ic50	0.0398	uM
(2S)-5-(diaminomethylideneamino)-2-[[2-[(1S,2S)-2-methyl-1-(quinoline-2-carbonylamino)butyl]-1,3-oxazole-4-carbonyl]amino]pentanoic acid	1262223: Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay	ec50	0.0407	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid	491629: Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting	ic50	0.0417	uM
(2S)-2-[[1-[(2-bromophenyl)methyl]-2-oxopyridine-3-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	1393260: Displacement of 125I-C3a from recombinant human C3aR expressed in HEK293 cell membranes after 3 hrs by scintillation proximity assay	ic50	0.0500	uM

CTD chemical–gene interactions

25 total (human), top 25 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
(+)-JQ1 compound	decreases expression	2
Nickel	increases expression	2
aristolochic acid I	increases expression	1
3-((6-(2-methoxyphenyl)pyrimidin-4-yl)amino)phenyl)methane sulfonamide	decreases expression	1
sulforaphane	increases expression	1
sodium arsenite	decreases expression	1
S-(1,2-dichlorovinyl)cysteine	affects cotreatment, decreases expression	1
3-hydroxy-4-prenyl-5-methoxystilbene-2-carboxylic acid	increases expression	1
Acetaminophen	decreases expression	1
Air Pollutants	affects expression, increases abundance	1
Azacitidine	increases expression	1
Benzo(a)pyrene	affects methylation, decreases methylation, increases methylation	1
Calcitriol	decreases expression	1
Cisplatin	increases expression	1
Cytarabine	increases expression	1
Folic Acid	decreases expression	1
Lipopolysaccharides	decreases expression, affects cotreatment	1
Nicotine	increases expression	1
Ozone	affects expression, increases abundance	1
Silicon Dioxide	decreases expression	1
Tretinoin	increases expression	1
Zidovudine	affects cotreatment, increases expression	1
Antirheumatic Agents	decreases expression	1
Okadaic Acid	increases expression	1
Particulate Matter	decreases expression	1

ChEMBL screening assays

75 unique, capped per target: 45 functional, 28 binding, 2 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1176063	Functional	Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release at 1 mM	Selective hexapeptide agonists and antagonists for human complement C3a receptor. — J Med Chem
CHEMBL1176064	Binding	Displacement of [125I-C3a] from C3a receptor in human PBMC at 1 mM by scintillation counting	Selective hexapeptide agonists and antagonists for human complement C3a receptor. — J Med Chem
CHEMBL4380983	ADMET	Agonist activity at C3a receptor in human MDM cells assessed as induction of intracellular calcium release measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay	Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity. — J Med Chem

Cellosaurus cell lines

7 cell lines: 5 cancer cell line, 2 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B8C8	Abcam HCT 116 C3AR1 KO	Cancer cell line	Male
CVCL_B9EE	Abcam A-549 C3AR1 KO	Cancer cell line	Male
CVCL_D2E1	Abcam MCF-7 C3AR1 KO	Cancer cell line	Female
CVCL_D7C7	Abeomics NIH 3T3 C3aR1	Spontaneously immortalized cell line	Male
CVCL_KU82	cAMP Hunter CHO-K1 C3AR1 Gi	Spontaneously immortalized cell line	Female
CVCL_KZ83	PathHunter U2OS C3AR1 Activated GPCR Internalization	Cancer cell line	Female
CVCL_KZ84	PathHunter U2OS C3AR1 beta-arrestin	Cancer cell line	Female

Clinical trials (associated diseases)

300 trials via MONDO — disease-level, not drug-specific.

Trial	Phase	Status	Title
NCT00029224	PHASE4	COMPLETED	Treatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions
NCT00035997	PHASE4	COMPLETED	Open-label Trial on the Effect of I.V. Zoledronic Acid 4 mg on Bone Density in Hormone Sensitive Prostate Cancer Patients With Bone Metastasis
NCT00063609	PHASE4	COMPLETED	The Effect of Zoledronic Acid on Bone Loss in Prostate Cancer Patients Undergoing Androgen Deprivation Therapy
NCT00103623	PHASE4	SUSPENDED	The Plenaxis® Experience Study
NCT00106392	PHASE4	COMPLETED	A Safety and Efficacy Study of Prograf in the Prevention of Erectile Dysfunction After Radical Prostatectomy
NCT00185029	PHASE4	UNKNOWN	MR-Lymphography and Lymph Node Staging in Prostate Cancer
NCT00199485	PHASE4	COMPLETED	Angelica Sinensis for the Treatment of Hot Flashes in Men Undergoing LHRH Therapy for Prostate Cancer
NCT00219219	PHASE4	COMPLETED	Zoledronic Acid in the Prevention of Skeletal-related Events in Hormone Refractory and Hormone-sensitive Prostate Cancer Patients With Bone Metastases
NCT00219271	PHASE4	COMPLETED	Effect Of Zoledronic Acid On Circulating And Bone Marrow-Residing Prostate Cancer Cells In Patients With Clinically Localized Prostate Cancer
NCT00237146	PHASE4	COMPLETED	Study to Evaluate Zoledronic Acid on Quality of Life and Skeletal-related Events as Adjuvant Treatment in Patients With Hormone-naïve Prostate Cancer and Bone Metastasis Who Have Undergone Orchiectomy
NCT00242554	PHASE4	COMPLETED	Open-label Phase IV Clinical Trial to Evaluate the Safety and Tolerability of Zoledronic Acid in Patients With Prostate Cancer and Bone Metastases
NCT00280098	PHASE4	COMPLETED	Docetaxel in the Treatment of Hormone Refractory Prostate Cancer
NCT00293696	PHASE4	COMPLETED	Casodex/Zoladex Biomarkers in Localised Prostate Cancer
NCT00334139	PHASE4	COMPLETED	Effect of Zoledronic Acid on Bone Metabolism in Patients With Bone Metastasis and Prostate or Breast Cancer
NCT00375765	PHASE4	COMPLETED	Effects On Dihydrotestosterone Regulated Gene Expression In Benign Prostatic Hyperplasia Or Prostate Cancer
NCT00391690	PHASE4	COMPLETED	Evaluation of Bone Markers as Diagnostic Tools for Early Detection of Bone Metastases in Patients With High Risk Prostate Cancer
NCT00422708	PHASE4	COMPLETED	Local Anesthesia for Prostate Biopsy
NCT00526331	PHASE4	COMPLETED	Evaluation of Arterial Pressure Based Cardiac Output for Goal-Directed Perioperative Therapy
NCT00590213	PHASE4	COMPLETED	Compare the Value of Prophylactic Versus Therapeutic Breast Radiotherapy in CASODEX
NCT00629330	PHASE4	TERMINATED	Dissemination of Prostate Cancer Screening to PCP’s in African American Communities
NCT00771966	PHASE4	COMPLETED	Radical Prostatectomy and Perioperative Fluid Therapy
NCT00805701	PHASE4	COMPLETED	Study Assessing The Efficacy And Safety Of Avodart (Dutasteride) At Improving Urinary Symptoms In Men With Prostate Cancer Who Are Undergoing Seed Implantation
NCT00859027	PHASE4	COMPLETED	Effect Of Risedronate On Bone Mass In Older Men Receiving Neoadjuvant Therapy For Prostate Cancer
NCT00906269	PHASE4	UNKNOWN	Can Hyperbaric Oxygen Improve Erectile Function Following Surgery for Prostate Cancer
NCT00953277	PHASE4	COMPLETED	Study of Nerve Reconstruction Using AVANCE in Subjects Who Undergo Robotic Assisted Prostatectomy for Treatment of Prostate Cancer
NCT00982800	PHASE4	COMPLETED	Does Postoperative Gabapentin Reduce Pain, Opioid Consumption and Anxiety and Have a Positive Effect on Health Related Quality of Life After Radical Prostatectomy?
NCT01083199	PHASE4	COMPLETED	Global Performance Evaluation of the AMS CONTINUUM™ Device
NCT01136226	PHASE4	COMPLETED	Evaluate Recovery of Testosterone for Patients Using Eligard
NCT01161563	PHASE4	COMPLETED	Randomized Crossover Trial to Assess the Tolerability of Gonadotropin Releasing Hormone (GnRH) Analogue Administration
NCT01230905	PHASE4	COMPLETED	Study to Monitor the Effects of Androgen Suppression Treatment on the Heart
NCT01296672	PHASE4	COMPLETED	3 Month Finasteride Challenge Test Can Significantly Improve the Performance of Screening for Prostate Cancer
NCT01365143	PHASE4	TERMINATED	Prospective Randomized Trial Comparing Robotic Versus Open Radical Prostatectomy
NCT01379742	PHASE4	UNKNOWN	Comparison of Between ThinSeed™ and OncoSeed™ for Permanent Prostate Brachytherapy
NCT01486563	PHASE4	COMPLETED	Hydroxyethyl Starch and Renal Function After Radical Prostatectomy
NCT01511874	PHASE4	COMPLETED	Efficacy and Safety Study of ELIGARD 22.5mg With Prostate Cancer
NCT01512472	PHASE4	TERMINATED	Firmagon (Degarelix) Intermittent Therapy
NCT01547416	PHASE4	COMPLETED	The Effect of Combined General/Epidural Anesthesia Versus General Anesthesia on Diaphragmatic Function
NCT01571544	PHASE4	COMPLETED	The Use of Thermal Suits as Preventing Hypothermia During Surgery
NCT01581749	PHASE4	UNKNOWN	Evaluation of Truebeam for Low-Intermediate Risk Prostate Cancer
NCT01649635	PHASE4	COMPLETED	Study of Cabazitaxel Combined With Prednisone and Prophylaxis of Neutropenia Complications in the Treatment of Patients With Metastatic Castration-resistant Prostate Cancer