ITGB5

Summary

ITGB5 (integrin subunit beta 5, HGNC:6160) is a protein-coding gene on chromosome 3q21.2, encoding Integrin beta-5 (P18084). Integrin alpha-V/beta-5 (ITGAV:ITGB5) is a receptor for fibronectin. It is a selective cancer dependency (DepMap: 37.9% of cell lines).

This gene encodes a beta subunit of integrin, which can combine with different alpha chains to form a variety of integrin heterodimers. Integrins are integral cell-surface receptors that participate in cell adhesion as well as cell-surface mediated signaling. The alphav beta5 integrin is involved in adhesion to vitronectin.

Source: NCBI Gene 3693 — RefSeq curated summary.

At a glance

• GWAS associations: 11
• Clinical variants (ClinVar): 128 total
• Druggable target: yes — 4 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 37.9% of screened cell lines
• MANE Select transcript: NM_002213

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:6160
Approved symbol	ITGB5
Name	integrin subunit beta 5
Location	3q21.2
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000082781
Ensembl biotype	protein_coding
OMIM	147561
Entrez	3693

Gene structure

Transcript identifiers

Ensembl transcripts: 37 — 31 protein_coding, 4 protein_coding_CDS_not_defined, 1 retained_intron, 1 nonsense_mediated_decay

ENST00000296181, ENST00000460797, ENST00000461306, ENST00000465464, ENST00000474838, ENST00000476988, ENST00000481591, ENST00000483168, ENST00000488466, ENST00000496703, ENST00000608107, ENST00000608657, ENST00000608945, ENST00000905025, ENST00000905026, ENST00000935895, ENST00000935896, ENST00000935897, ENST00000935898, ENST00000935899, ENST00000935900, ENST00000935901, ENST00000935902, ENST00000935903, ENST00000935904, ENST00000935905, ENST00000935906, ENST00000935907, ENST00000935908, ENST00000935909, ENST00000935910, ENST00000965612, ENST00000965613, ENST00000965614, ENST00000965615, ENST00000965616, ENST00000965617

RefSeq mRNA: 4 — MANE Select: NM_002213 NM_001354764, NM_001354765, NM_001354766, NM_002213

CCDS: CCDS3030

Canonical transcript exons

ENST00000296181 — 15 exons

Exon	Start	End
ENSE00001299954	124886931	124887365
ENSE00001919720	124761948	124763718
ENSE00003473362	124764391	124764557
ENSE00003537257	124817621	124817710
ENSE00003541206	124819739	124819834
ENSE00003547453	124773690	124773912
ENSE00003602813	124766226	124766345
ENSE00003605882	124859242	124859446
ENSE00003622904	124769013	124769113
ENSE00003624028	124848309	124848558
ENSE00003632570	124873446	124873531
ENSE00003641308	124821313	124821474
ENSE00003702760	124796388	124796817
ENSE00003707382	124841383	124841551
ENSE00003708330	124809022	124809156

Expression profiles

Bgee: expression breadth ubiquitous, 293 present calls, max score 99.50.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 40.1917 / max 238.0249, expressed in 1646 samples.

FANTOM5 promoters (10 alternative TSS)

Promoter ID	TPM avg	Samples expressed
44238	25.5883	1609
44239	4.8856	1355
44244	1.9114	1054
44242	1.8331	1111
44241	1.5543	941
44240	1.3802	844
44243	1.0746	700
44245	0.9001	625
44237	0.6215	374
44236	0.4426	243

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
stromal cell of endometrium	CL:0002255	99.50	gold quality
ascending aorta	UBERON:0001496	99.23	gold quality
right coronary artery	UBERON:0001625	99.23	gold quality
thoracic aorta	UBERON:0001515	99.22	gold quality
descending thoracic aorta	UBERON:0002345	99.12	gold quality
pancreatic ductal cell	CL:0002079	99.02	gold quality
aorta	UBERON:0000947	98.86	gold quality
cartilage tissue	UBERON:0002418	98.68	gold quality
tendon of biceps brachii	UBERON:0008188	98.68	gold quality
left coronary artery	UBERON:0001626	98.67	gold quality
metanephric glomerulus	UBERON:0004736	98.64	gold quality
popliteal artery	UBERON:0002250	98.61	gold quality
tibial artery	UBERON:0007610	98.61	gold quality
coronary artery	UBERON:0001621	98.60	gold quality
renal glomerulus	UBERON:0000074	98.59	gold quality
artery	UBERON:0001637	98.57	gold quality
gall bladder	UBERON:0002110	98.31	gold quality
skin of leg	UBERON:0001511	98.07	gold quality
cervix squamous epithelium	UBERON:0006922	98.07	gold quality
visceral pleura	UBERON:0002401	98.00	gold quality
apex of heart	UBERON:0002098	97.93	gold quality
subcutaneous adipose tissue	UBERON:0002190	97.92	gold quality
calcaneal tendon	UBERON:0003701	97.88	gold quality
blood vessel layer	UBERON:0004797	97.78	gold quality
germinal epithelium of ovary	UBERON:0001304	97.74	gold quality
colonic epithelium	UBERON:0000397	97.64	gold quality
omental fat pad	UBERON:0010414	97.52	gold quality
peritoneum	UBERON:0002358	97.51	gold quality
layer of synovial tissue	UBERON:0007616	97.49	gold quality
zone of skin	UBERON:0000014	97.45	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	17.60
E-CURD-112	no	2.98

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): ITGB8, PPARA, SMAD4, SPI1

miRNA regulators (miRDB)

49 targeting ITGB5, 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-1252-5P	100.00	69.80	2774
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-548N	99.98	71.94	4170
HSA-MIR-5688	99.96	73.23	4504
HSA-MIR-495-3P	99.96	72.81	4197
HSA-MIR-9983-3P	99.94	71.48	3631
HSA-MIR-205-3P	99.92	69.92	3165
HSA-MIR-589-3P	99.91	69.62	2088
HSA-MIR-129-5P	99.88	70.26	3273
HSA-MIR-4319	99.76	69.83	2586
HSA-MIR-3059-5P	99.70	69.93	2491
HSA-MIR-29B-2-5P	99.67	68.98	1726
HSA-MIR-3202	99.66	67.70	2737
HSA-MIR-4276	99.56	67.66	2514
HSA-MIR-4708-3P	99.51	67.99	870
HSA-MIR-1207-5P	99.49	69.11	2983
HSA-MIR-6165	99.44	67.12	1389
HSA-MIR-942-5P	99.41	68.40	1977
HSA-MIR-3182	99.40	68.15	2454
HSA-MIR-125A-5P	99.36	70.59	1640
HSA-MIR-125B-5P	99.36	70.36	1662
HSA-MIR-4528	99.18	69.77	1936
HSA-MIR-4763-3P	99.10	67.83	2649
HSA-MIR-4504	99.10	69.14	1328
HSA-MIR-622	98.99	66.48	1050
HSA-MIR-4801	98.96	69.42	2096
HSA-MIR-3190-5P	98.87	64.89	1345
HSA-MIR-4755-3P	98.77	65.59	1915
HSA-MIR-4731-3P	98.56	68.60	1860

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 37.9% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 40)

• Overexpression of the beta5 integrin in hematopoietic cells was associated with the inhibition of cell proliferation and apoptosis. (PMID:11877043)
• identification of a new alphavbeta5 integrin-interacting motif that is highly conserved in the fas-1 domains of many proteins suggesting that fas-1 domain-containing proteins may perform their biological functions by interacting with integrins (PMID:12270930)
• alphav subunit cleavage is essential for integrin function and has a considerable impact on integrin-dependent events, especially those leading to cell migration (PMID:14741360)
• Data suggest that modulating the expression of integrin subunits beta3/5 in human neurons may enhance adenoviral infectivity via the coxsackie-adenovirus receptor. (PMID:15456946)
• urokinase receptor-derived SRSRY peptide regulates cross-talk between fMLP and vitronectin receptors (PMID:15866865)
• different beta5 integrins: repeated-FNK (FNKFNK764-769) and single-FNK (FNK764-766) amino acid sequences in the cytoplasmic domain. (PMID:15979906)
• integrin alphavbeta6, alphavbeta3, alphavbeta5, alpha5beta1 and alpha9beta1 binding to osteopontin is controlled by specific structural motifs that are recognized by extracellular proteases (PMID:16005200)
• Expression of integrins alphavbeta1, alphavbeta3, and alphavbeta5 in cerebral arteriovenous malformations and cavernous malformations. (Integrins alphavbeta1, alphavbeta3, and alphavbeta5) (PMID:16385340)
• While tolerogenic DCs are not induced via alphavbeta5, coligation of CR3 and alphavbeta5 maintains the DC’s tolerogenic profile. (PMID:16614246)
• Alphavbeta5 integrin may play a role in the adhesion and migration of VSMCs during the pathogenesis of atherosclerosis. (PMID:16672769)
• upregulated expression of alphavbeta5 contributes to autocrine TGF-beta signaling in localized scleroderma fibroblasts (PMID:16675963)
• Cell surface expression of alphavbeta5 resulted in an attenuation of alphavbeta3-mediated migration on vitronectin (PMID:17074516)
• Our studies suggest that the phagocytic function of beta5 integrin is regulated by an unconventional NPxY-talin-independent activation signal and argue for the existence of molecular switches in the beta5 cytoplasmic tail for adhesion and phagocytosis. (PMID:17963729)
• Real-time PCR showed that ETOH significantly altered the expression of genes involved in cell adhesion. There was an increase in the expression of alpha and beta Laminins 1, beta Integrins 3 and 5, Secreted phosphoprotein1 and Sarcoglycan epsilon. (PMID:18162078)
• data identify PAI1 as a novel regulator of fibronectin matrix assembly, and indicate that this regulation occurs through a previously undescribed crosstalk between the alphavbeta5 and alpha5beta1 integrins (PMID:18445685)
• Oxidized LDL impairs angiogenic properties of endothelial progenitor cells at sub-apoptotic levels by downregulation of E-selectin and integrin alphavbeta5, both substantial mediators of EPC-endothelial cell (PMID:18590706)
• human umbilical vein endothelial cells adhere to immobilized CXCL4 through alphavbeta3 integrin, and also through other integrins, such as alphavbeta5 and alpha5beta1 (PMID:18648521)
• urokinase-derived antagonists of alphavbeta5 integrin activation inhibit migration and invasion of carcinoma cells (PMID:18844213)
• The active site within the Sdc1 core protein was identified and a peptide inhibitor called synstatin (SSTN) that disrupts Sdc1’s interaction with alpha(v)beta(3) and alpha(v)beta(5) integrins was derived. (PMID:19255147)
• Compound 4, having the DGR retro-sequence, is a low micromolar ligand for the alphavbeta5 integrin. (PMID:19267182)
• Periostin mediates vascular smooth muscle cell migration through the integrins alphavbeta3 and alphavbeta5 and focal adhesion kinase (FAK) pathway (PMID:19695571)
• Beta1 integrins are required for adhesion and proliferation of induced pluripotent stem cells on Matrigel. On vitronectin, the integrin alphavbeta5 is required for initial attachment, but both alphavbeta5 and beta1 is required for proliferation. (PMID:19811096)
• The angiogenic effects of leptin are mediated by circulating angiogenic cells and involve src kinase dependent phosphorylation of integrin alphavbeta5. (PMID:19910644)
• Definitive endoderm highly express the integrins alphaV and beta5, which have the ability to bind to vitronectin. (PMID:20026907)
• Ovarian cancer ascites induces FAK and Akt activation in an alphavbeta5 integrin-dependent pathway, which confers protection from TRAIL-induced cell death and caspase activation. (PMID:20400979)
• The beta5-integrin adhesions contribute to the TGFbeta-induced EMT and the tumorigenic potential of carcinoma cells. (PMID:20404485)
• Src kinase-mediated activation of STAT3 and subsequent angiogenic gene expression mediate the effects of integrin alpha v beta 5 and may be exploited to enhance the paracrine activities of circulating angiogenic cells. (PMID:20431064)
• p21-activated kinase 4 phosphorylation of integrin beta5 Ser-759 and Ser-762 regulates cell migration (PMID:20507994)
• Integrin alphavbeta5 is a primary receptor for adenovirus. (PMID:20615244)
• Data show that knockdown of integrin alphav and erbB3 by small-interfering RNAs significantly inhibited cell migration induced by HRG. (PMID:20626753)
• PAK4 is activated by cell attachment to vitronectin as mediated by PAK4 binding partner integrin alphavbeta5. (PMID:20719960)
• beta5 integrin is identified as the most important partner of the alpha vitronectin-coupled integrin dimer in monocyte-derived macrophages, thus rendering these cells more susceptible to NF-kappaB-dependent HIV-1 infection. (PMID:21098231)
• CCN3 enhances the migration of chondrosarcoma cells by increasing MMP-13 expression through the alphavbeta3/alphavbeta5 integrin receptor, FAK, PI3K, Akt, p65, and NF-kappaB signal transduction pathway. (PMID:21344378)
• alphanubeta3 and alphanubeta5 have roles in photon-induced hypermigration of malignant glioma cells (PMID:21978494)
• Letter: loss of integrin beta5 in polyomavirus positive Merkel cell carcinoma may influence cell adhesion/migration. (PMID:22503669)
• Cysteine-rich protein Cyr61 activates interleukin (IL)-6 production via the alphavbeta5/Akt/NF-kappaB signaling pathway in rheumatoid arthritis. (PMID:22547695)
• High beta5-integrin protein expression is associated with aggressive behavior in gastric cancer. (PMID:22561002)
• knockdown of endogenous alphavbeta5 expression or treatment with a function-blocking alphavbeta5 antibody significantly decreased stabilin-2-mediated phagocytosis in the absence of soluble factors (PMID:22566688)
• Active MMP-2 regulates VEGF-A in melanoma cells on a transcriptional level via an integrin alphavbeta5/phosphoinositide-3-kinase-dependent pathway. (PMID:22659470)
• Data indicate the role of CYR61 and alpha(V)beta5 integrin as proteins that cooperate to mediate cancer cell migration. (PMID:22692860)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	itgb5	ENSDARG00000012942
mus_musculus	Itgb5	ENSMUSG00000022817
rattus_norvegicus	Itgb5	ENSRNOG00000001795

Paralogs (8): ITGB8 (ENSG00000105855), ITGB6 (ENSG00000115221), ITGB4 (ENSG00000132470), ITGB7 (ENSG00000139626), ITGB1 (ENSG00000150093), ITGB2 (ENSG00000160255), ITGBL1 (ENSG00000198542), ITGB3 (ENSG00000259207)

Protein

Protein identifiers

Integrin beta-5 — P18084 (reviewed: P18084)

All UniProt accessions (9): P18084, F8WBG2, H7C4W1, H7C580, H7C5U2, L7RT22, V9GYD8, V9GYZ1, V9GZ57

UniProt curated annotations — full annotation on UniProt →

Function. Integrin alpha-V/beta-5 (ITGAV:ITGB5) is a receptor for fibronectin. It recognizes the sequence R-G-D in its ligand. (Microbial infection) Integrin ITGAV:ITGB5 acts as a receptor for adenovirus type C.

Subunit / interactions. Heterodimer of an alpha and a beta subunit. Beta-5 (ITGB5) associates with alpha-V (ITGAV). Interacts with MYO10. Interacts with DAB2. Integrin ITGAV:ITGB5 interacts with FBLN5 (via N-terminus). ITGAV:ITGB5 interacts with CCN3. Interacts with tensin TNS3; TNS3 also interacts with PEAK1, thus acting as an adapter molecule to bridge the association of PEAK1 with ITGB5. (Microbial infection) Integrin ITGAV:ITGB5 interacts with adenovirus type C penton protein.

Subcellular location. Cell membrane.

Domain organisation. The VWFA domain (or beta I domain) contains three cation-binding sites: the ligand-associated metal ion-binding site (LIMBS or SyMBS), the metal ion-dependent adhesion site (MIDAS), and the adjacent MIDAS site (ADMIDAS). This domain is also part of the ligand-binding site.

Similarity. Belongs to the integrin beta chain family.

RefSeq proteins (4): NP_001341693, NP_001341694, NP_001341695, NP_002204* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002035	VWF_A	Domain
IPR002369	Integrin_bsu_VWA	Domain
IPR012896	Integrin_bsu_tail	Domain
IPR014836	Integrin_bsu_cyt_dom	Domain
IPR015812	Integrin_bsu	Family
IPR016201	PSI	Domain
IPR032695	Integrin_dom_sf	Homologous_superfamily
IPR033760	Integrin_beta_N	Domain
IPR036349	Integrin_bsu_tail_dom_sf	Homologous_superfamily
IPR036465	vWFA_dom_sf	Homologous_superfamily
IPR040622	EGF_integrin_1	Domain
IPR057073	EGF_integrin_2	Domain

Pfam: PF00362, PF07965, PF08725, PF17205, PF18372, PF23105

UniProt features (66 total): disulfide bond 28, binding site 12, glycosylation site 8, domain 6, sequence variant 3, sequence conflict 3, topological domain 2, signal peptide 1, chain 1, modified residue 1, transmembrane region 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
7S48	X-RAY DIFFRACTION	1.9
7S47	X-RAY DIFFRACTION	2
7S46	X-RAY DIFFRACTION	2.1

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P18084-F1	82.40	0.34

Functional residue map

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

Ligand- & substrate-binding residues (12): 147 (in midas binding site); 149 (in admidas binding site); 149 (in midas binding site); 152 (in admidas binding site); 153 (in admidas binding site); 184 (in limbs binding site); 242 (in limbs binding site); 244 (in limbs binding site); 246 (in limbs binding site); 247 (in limbs binding site); 247 (in midas binding site); 362 (in admidas binding site)

Post-translational modifications (1): 770

Disulfide bonds (28): 28–46, 36–463, 39–64, 49–75, 202–211, 259–300, 401–413, 433–461, 465–484, 476–487, 489–498, 500–530, 513–528, 522–533, 535–548, 550–571, 555–569, 563–574, 576–585, 587–610 …

Glycosylation sites (8): 347, 460, 477, 505, 552, 586, 654, 705

Function

Pathways and Gene Ontology

Reactome pathways

18 pathways

ID	Pathway
R-HSA-1236973	Cross-presentation of particulate exogenous antigens (phagosomes)
R-HSA-2129379	Molecules associated with elastic fibres
R-HSA-216083	Integrin cell surface interactions
R-HSA-2173789	TGF-beta receptor signaling activates SMADs
R-HSA-3000170	Syndecan interactions
R-HSA-3000178	ECM proteoglycans
R-HSA-445355	Smooth Muscle Contraction
R-HSA-1236975	Antigen processing-Cross presentation
R-HSA-1280218	Adaptive Immune System
R-HSA-1474244	Extracellular matrix organization
R-HSA-1566948	Elastic fibre formation
R-HSA-162582	Signal Transduction
R-HSA-168256	Immune System
R-HSA-170834	Signaling by TGF-beta Receptor Complex
R-HSA-3000171	Non-integrin membrane-ECM interactions
R-HSA-397014	Muscle contraction
R-HSA-9006936	Signaling by TGFB family members
R-HSA-983169	Class I MHC mediated antigen processing & presentation

MSigDB gene sets: 0 (showing top):

GO Biological Process (13): cell-matrix adhesion (GO:0007160), transforming growth factor beta receptor signaling pathway (GO:0007179), integrin-mediated signaling pathway (GO:0007229), cell migration (GO:0016477), cell adhesion mediated by integrin (GO:0033627), wound healing, spreading of epidermal cells (GO:0035313), endodermal cell differentiation (GO:0035987), stress fiber assembly (GO:0043149), epithelial cell-cell adhesion (GO:0090136), cell-cell adhesion (GO:0098609), formation of primary germ layer (GO:0001704), cell adhesion (GO:0007155), symbiont entry into host cell (GO:0046718)

GO Molecular Function (5): virus receptor activity (GO:0001618), integrin binding (GO:0005178), metal ion binding (GO:0046872), signaling receptor binding (GO:0005102), protein binding (GO:0005515)

GO Cellular Component (9): plasma membrane (GO:0005886), focal adhesion (GO:0005925), integrin complex (GO:0008305), cell surface (GO:0009986), integrin alphav-beta5 complex (GO:0034684), signaling receptor complex (GO:0043235), phagocytic vesicle (GO:0045335), extracellular exosome (GO:0070062), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-11 pathways:

Category	Pathways
Extracellular matrix organization	4
Antigen processing-Cross presentation	1
Elastic fibre formation	1
Signaling by TGF-beta Receptor Complex	1
Non-integrin membrane-ECM interactions	1
Muscle contraction	1
Class I MHC mediated antigen processing & presentation	1
Immune System	1
Signaling by TGFB family members	1
Signal Transduction	1
Adaptive Immune System	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cell adhesion	2
cellular anatomical structure	2
cell-substrate adhesion	1
cellular response to transforming growth factor beta stimulus	1
transforming growth factor beta receptor superfamily signaling pathway	1
cell surface receptor signaling pathway	1
cell motility	1
wound healing, spreading of cells	1
endoderm formation	1
cell differentiation	1
contractile actin filament bundle assembly	1
actomyosin structure organization	1
cell-cell adhesion	1
gastrulation	1
anatomical structure formation involved in morphogenesis	1
cellular process	1
viral life cycle	1
symbiont entry into host	1
symbiont entry into host cell	1
exogenous protein binding	1
signaling receptor binding	1
protein-containing complex binding	1
cell adhesion molecule binding	1
cation binding	1
protein binding	1
binding	1
membrane	1
cell periphery	1
cell-substrate junction	1
protein complex involved in cell adhesion	1
plasma membrane signaling receptor complex	1
integrin complex	1
protein-containing complex	1
endocytic vesicle	1
extracellular vesicle	1

Protein interactions and networks

STRING

1838 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
ITGB5	ITGAV	P06756	990
ITGB5	FN1	P02751	935
ITGB5	VTN	P01141	927
ITGB5	ITGA5	P08648	874
ITGB5	ITGA3	P26006	796
ITGB5	MFGE8	Q08431	777
ITGB5	ITGA2	P17301	774
ITGB5	ITGA6	P23229	772
ITGB5	PAK4	O96013	743
ITGB5	ITGA1	P56199	740
ITGB5	POSTN	Q15063	719
ITGB5	ITGA11	Q9UKX5	699
ITGB5	ILK	P57043	691
ITGB5	ITGA7	Q13683	690
ITGB5	ITGA10	O75578	677

IntAct

162 interactions, top by confidence:

A	B	Type	Score
KLK5	DENND11	psi-mi:“MI:0914”(association)	0.640
FRMD5	ITGB5	psi-mi:“MI:0915”(physical association)	0.600
ITGB5	FRMD5	psi-mi:“MI:0915”(physical association)	0.600
ITGB5	FRMD5	psi-mi:“MI:0407”(direct interaction)	0.600
CYSRT1	ITGB5	psi-mi:“MI:0915”(physical association)	0.560
ITGB5	KRTAP10-9	psi-mi:“MI:0915”(physical association)	0.560
EFEMP2	ITGB5	psi-mi:“MI:0915”(physical association)	0.560
KRT34	ITGB5	psi-mi:“MI:0915”(physical association)	0.560
NOTCH2NLC	ITGB5	psi-mi:“MI:0915”(physical association)	0.560
ITGB5	FHL3	psi-mi:“MI:0915”(physical association)	0.560
KRTAP1-3	ITGB5	psi-mi:“MI:0915”(physical association)	0.560
ITGAV	VTN	psi-mi:“MI:0915”(physical association)	0.560
ITGB5	MTUS2	psi-mi:“MI:0915”(physical association)	0.560
ITGB5	KRT31	psi-mi:“MI:0915”(physical association)	0.560
ITGB5	GOLGA2	psi-mi:“MI:0915”(physical association)	0.560
ITGB5	APPBP2	psi-mi:“MI:0915”(physical association)	0.560
ITGB5	KRTAP10-7	psi-mi:“MI:0915”(physical association)	0.560
ITGB5	KRTAP10-8	psi-mi:“MI:0915”(physical association)	0.560
ITGB5	KRTAP5-7	psi-mi:“MI:0915”(physical association)	0.560
ITGB5	KRTAP1-1	psi-mi:“MI:0915”(physical association)	0.560
ITGB5	ZNF655	psi-mi:“MI:0915”(physical association)	0.560
ITGB5	KRTAP3-2	psi-mi:“MI:0915”(physical association)	0.560
ITGB5	ANGPTL4	psi-mi:“MI:0407”(direct interaction)	0.560
ANGPTL4	ITGB5	psi-mi:“MI:0914”(association)	0.560
ITGB5	ANGPTL4	psi-mi:“MI:2364”(proximity)	0.560
MYO10	ITGB5	psi-mi:“MI:0407”(direct interaction)	0.540
ITGB5	Myo7a	psi-mi:“MI:0915”(physical association)	0.540
Myo7a	ITGB5	psi-mi:“MI:0915”(physical association)	0.540

BioGRID (194): EHMT2 (Two-hybrid), MTUS2 (Two-hybrid), KRT40 (Two-hybrid), KRTAP10-9 (Two-hybrid), KRTAP10-8 (Two-hybrid), NOTCH2NL (Two-hybrid), ITGA5 (Affinity Capture-Western), ITGB5 (Affinity Capture-MS), ITGB5 (Affinity Capture-MS), ITGB5 (Affinity Capture-MS), ITGB5 (Affinity Capture-MS), ITGB5 (Reconstituted Complex), ZBTB17 (Two-hybrid), ITGB5 (Affinity Capture-Western), ADAM9 (Affinity Capture-Western)

ESM2 similar proteins: A0A0D3QS98, A0A0D3QS99, A4D0V7, C5H5C4, F6Q1T7, O70309, O75354, P17405, P18084, P18424, P22413, P50747, P52850, P58242, P61642, P80747, Q04519, Q0VBD0, Q0VD19, Q13219, Q52KP5, Q58CQ9, Q5QQ51, Q5STE3, Q64687, Q6DFZ6, Q6KFX9, Q6MZW2, Q6P988, Q6UWX4, Q6YGZ1, Q6ZXD2, Q71RP1, Q812F8, Q8BJQ9, Q8C1F4, Q8C419, Q8N5D6, Q8N6G5, Q8R116

Diamond homologs: A2A863, A5Z1X6, B0FYY4, O08680, O54890, O70309, P05106, P05107, P05556, P07228, P09055, P11584, P11835, P12606, P12607, P16144, P18084, P18563, P18564, P26010, P26011, P26012, P29319, P29320, P32592, P49134, P53712, P53713, P53714, P80747, Q07409, Q07441, Q09062, Q0VBD0, Q1RPR6, Q27591, Q27874, Q2VJ42, Q3UH53, Q3UV74

SIGNOR signaling

8 interactions.

A	Effect	B	Mechanism
PAK4	up-regulates	ITGB5	phosphorylation
ITGB1BP1	“down-regulates activity”	ITGB5	binding
DOK1	“down-regulates activity”	ITGB5	binding
ITGB5	“up-regulates activity”	PTK2
Kindlin	“up-regulates activity”	ITGB5	binding
TLN1	“up-regulates activity”	ITGB5	binding
ITGB5	“form complex”	“Av/b5 integrin”	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 126 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
Immunoregulatory interactions between a Lymphoid and a non-Lymphoid cell	8	8.5×	6e-04
Keratinization	10	6.8×	5e-04

GO biological processes:

GO term	Partners	Fold	FDR
integrin-mediated signaling pathway	7	11.0×	3e-03
cell adhesion	12	4.4×	5e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	98
Likely benign	4
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

3657 predictions. Top by Δscore:

Variant	Effect	Δscore
3:124762924:A:T	acceptor_gain	1.0000
3:124763719:C:CC	acceptor_gain	1.0000
3:124763720:T:C	acceptor_loss	1.0000
3:124763730:G:T	acceptor_gain	1.0000
3:124764386:CTTA:C	donor_loss	1.0000
3:124764387:TTACC:T	donor_loss	1.0000
3:124764388:TA:T	donor_loss	1.0000
3:124764389:A:AG	donor_loss	1.0000
3:124764390:C:CA	donor_loss	1.0000
3:124764554:CACT:C	acceptor_gain	1.0000
3:124764556:CT:C	acceptor_gain	1.0000
3:124764558:C:CC	acceptor_gain	1.0000
3:124764568:C:CT	acceptor_gain	1.0000
3:124766222:CTA:C	donor_loss	1.0000
3:124766224:A:AC	donor_gain	1.0000
3:124766225:C:A	donor_loss	1.0000
3:124766225:C:CC	donor_gain	1.0000
3:124766225:CCTGG:C	donor_gain	1.0000
3:124766256:T:TA	donor_gain	1.0000
3:124766257:C:A	donor_gain	1.0000
3:124766341:TTTCA:T	acceptor_gain	1.0000
3:124766342:TTCA:T	acceptor_gain	1.0000
3:124766343:TCA:T	acceptor_gain	1.0000
3:124766344:CA:C	acceptor_gain	1.0000
3:124766344:CAC:C	acceptor_gain	1.0000
3:124766345:AC:A	acceptor_loss	1.0000
3:124766346:C:CC	acceptor_gain	1.0000
3:124766346:CTG:C	acceptor_loss	1.0000
3:124769116:T:C	acceptor_gain	1.0000
3:124809155:CT:C	acceptor_gain	1.0000

AlphaMissense

5289 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
3:124764424:A:C	F757L	0.999
3:124764424:A:T	F757L	0.999
3:124764425:A:C	F757C	0.999
3:124764426:A:G	F757L	0.999
3:124773852:C:G	C585S	0.999
3:124773853:A:T	C585S	0.999
3:124796393:C:G	C563S	0.999
3:124796394:A:T	C563S	0.999
3:124796438:C:G	C548S	0.999
3:124796438:C:T	C548Y	0.999
3:124796439:A:T	C548S	0.999
3:124796516:C:G	C522S	0.999
3:124796517:A:T	C522S	0.999
3:124817629:C:G	A374P	0.999
3:124821356:C:G	C300S	0.999
3:124821357:A:T	C300S	0.999
3:124821411:G:C	H282D	0.999
3:124821460:C:A	W265C	0.999
3:124821460:C:G	W265C	0.999
3:124821462:A:G	W265R	0.999
3:124821462:A:T	W265R	0.999
3:124841437:G:C	N242K	0.999
3:124841437:G:T	N242K	0.999
3:124841530:G:C	C211W	0.999
3:124841531:C:T	C211Y	0.999
3:124848314:G:C	C202W	0.999
3:124848315:C:G	C202S	0.999
3:124848315:C:T	C202Y	0.999
3:124848316:A:T	C202S	0.999
3:124848374:A:C	F182L	0.999

dbSNP variants (sampled 300 via entrez): RS1000059302 (3:124769915 T>C,G), RS1000066849 (3:124813341 A>G), RS1000097821 (3:124851535 T>A), RS1000098532 (3:124817982 C>T), RS1000112860 (3:124880893 T>C), RS1000118597 (3:124812254 A>C), RS1000145262 (3:124863192 C>T), RS1000178399 (3:124780850 G>A), RS1000189316 (3:124902154 C>T), RS1000193893 (3:124837751 A>T), RS1000225881 (3:124831197 T>G), RS1000231639 (3:124876606 G>C), RS1000235745 (3:124795926 C>T), RS1000240424 (3:124812546 C>A), RS1000252390 (3:124818064 C>A)

Disease associations

OMIM: gene MIM:147561 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

11 associations (top):

Study	Trait	p-value
GCST002152_1	Airway hyperresponsiveness	2.000000e-06
GCST004787_30	Coronary artery disease (myocardial infarction, percutaneous transluminal coronary angioplasty, coronary artery bypass grafting, angina or chromic ischemic heart disease)	2.000000e-09
GCST006979_75	Heel bone mineral density	6.000000e-09
GCST007094_21	Diastolic blood pressure	7.000000e-08
GCST007096_252	Pulse pressure	1.000000e-06
GCST007099_102	Systolic blood pressure	2.000000e-11
GCST007267_257	Systolic blood pressure	3.000000e-08
GCST007581_7	Carpal tunnel syndrome	4.000000e-09
GCST007990_6	Coronary artery disease	2.000000e-08
GCST90002391_16	Mean corpuscular hemoglobin concentration	1.000000e-09
GCST90020028_813	Hip circumference adjusted for BMI	9.000000e-11

EFO canonical traits (7, from GWAS)

EFO ID	Trait name
EFO:0005414	airway hyperresponsiveness
EFO:0009270	heel bone mineral density
EFO:0006336	diastolic blood pressure
EFO:0005763	pulse pressure measurement
EFO:0006335	systolic blood pressure
EFO:0004528	mean corpuscular hemoglobin concentration
EFO:0008039	BMI-adjusted hip circumference

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (3): CHEMBL2096675 (PROTEIN COMPLEX), CHEMBL2600 (SINGLE PROTEIN), CHEMBL4106150 (PROTEIN COMPLEX)

Molecules with ChEMBL bioactivity

4 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 10,236 (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
CHEMBL429876	CILENGITIDE	3	10,123
CHEMBL3319236	GLPG-0187	1	96
CHEMBL4241824	GSK-3008348 FREE BASE	1	8
CHEMBL4246089	GSK-3008348	1	9

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

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs10049380	ITGB5, UMPS		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: catalytic receptor — Integrins

Most potent curated ligand interactions (1 total), top 1:

Ligand	Action	Affinity	Parameter
compound 7 [PMID: 31381331]	Inhibition	7.3	pKi

Binding affinities (BindingDB)

17 measured of 17 human assays (17 total across all organisms); most potent 17 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(3S)-3-[3-bromo-5-(trifluoromethyl)phenyl]-3-[[2-[[5-[(5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino]pyridine-3-carbonyl]amino]acetyl]amino]propanoic acid	IC50	0.3 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
(3S)-3-[3-chloro-5-(difluoromethyl)phenyl)-3-(2-(3-hydroxy-5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)benzamido)acetamido]propanoic acid	IC50	0.5 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
(3S)-3-[3-bromo-5-methyl-phenyl)-3-(2-(3-hydroxy-5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)benzamido)acetamido)propanoic acid	IC50	0.5 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
(3S)-3-[3-bromo-5-chloro-phenyl)-3-(2-(3-hydroxy-5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)benzamido)acetamido]propanoic acid	IC50	0.6 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
(3S)-3-(3-bromo-5-chloro-phenyl)-3-[[2-[[5-[(5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino]pyridine-3-carbonyl]amino]acetyl]amino]propanoic acid	IC50	0.6 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
(3S)-3-[3-bromo-5-fluoro-phenyl)-3-(2-(3-hydroxy-5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)benzamido)acetamido)propanoic acid	IC50	0.6 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
(3S)-3-(3,5-dibromophenyl)-3-[[2-[[5-[(5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino]pyridine-3-carbonyl]amino]acetyl]amino]propanoic acid	IC50	0.6 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
(3S)-3-[3-bromo-5-(difluoromethyl)phenyl)-3-(2-(3-hydroxy-5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)benzamido)acetamido]propanoic acid	IC50	0.7 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
(3S)-3-[3-chloro-5-(trifluoromethyl)phenyl]3-[[2-[[5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino]pyridine-3-carbonyl]amino]acetyl]amino]propanoic acid	IC50	0.7 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
(3S)-3-(3-bromo-5-(trifluoromethyl)phenyl)-3-(2-(3-hydroxy-5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)benzamido)acetamido)propanoic acid	IC50	0.8 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
(3S)-3-[3-chloro-5-(trifluoromethyl)phenyl)-3-(2-(3-hydroxy-5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)benzamido)acetamido]propanoic acid	IC50	0.8 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
(3S)-3-(3,5-dibromophenyl)-3-(2-(3-hydroxy-5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)benzamido)acetamido)propanoic acid	IC50	1 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
(3S)-3-[3,5-bis(trifluoromethyl)phenyl)-3-(2-(3-hydroxy-5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)benzamido)acetamido]propanoic acid	IC50	1 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
(3S)-3-[3,5-dichloro-phenyl)-3-(2-(3-hydroxy-5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)benzamido)acetamido)propanoic acid	IC50	1 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
(3S)-3-[3-chloro-5-(trifluoromethoxy)phenyl)-3-(2-(3-hydroxy-5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)benzamido)acetamido)propanoic acid	IC50	1 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
(3S)-3-(3-bromo-5-(trifluoromethoxy)phenyl)-3-(2-(3-hydroxy-5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)benzamido)acetamido)propanoic acid	IC50	1 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
(3S)-3-[3-chloro-5-methyl-phenyl)-3-(2-(3-hydroxy-5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)benzamido)acetamido)propanoic acid	IC50	2 nM	US-10035778: Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists

ChEMBL bioactivities

506 potent at pChembl≥5 of 541 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.00	IC50	0.1	nM	CHEMBL109930
10.00	IC50	0.1	nM	CHEMBL5889173
10.00	IC50	0.1	nM	CHEMBL5951981
10.00	IC50	0.1	nM	CHEMBL5914164
9.96	IC50	0.11	nM	CYCLORGDFV
9.89	IC50	0.13	nM	CILENGITIDE
9.77	IC50	0.17	nM	CHEMBL590547
9.70	IC50	0.2	nM	CHEMBL327102
9.70	IC50	0.2	nM	CHEMBL5781301
9.70	IC50	0.2	nM	CHEMBL5964326
9.70	IC50	0.2	nM	CHEMBL5802710
9.70	IC50	0.2	nM	CHEMBL5920684
9.68	IC50	0.21	nM	CHEMBL190128
9.52	IC50	0.3	nM	CHEMBL109703
9.52	IC50	0.3	nM	CHEMBL5786200
9.52	IC50	0.3	nM	CHEMBL5790208
9.52	IC50	0.3	nM	CHEMBL5802648
9.46	IC50	0.35	nM	CHEMBL2372427
9.43	IC50	0.37	nM	CHEMBL590609
9.42	IC50	0.38	nM	CHEMBL285950
9.40	IC50	0.4	nM	CHEMBL5766697
9.40	IC50	0.4	nM	CHEMBL5974146
9.40	IC50	0.4	nM	CHEMBL5819051
9.40	IC50	0.4	nM	CHEMBL6027181
9.40	IC50	0.4	nM	CHEMBL5946569
9.39	IC50	0.41	nM	CHEMBL35360
9.30	IC50	0.5	nM	CHEMBL190309
9.30	IC50	0.5	nM	CHEMBL113063
9.30	IC50	0.5	nM	CHEMBL5975238
9.23	IC50	0.59	nM	CHEMBL556402
9.22	IC50	0.6	nM	CHEMBL5770209
9.22	IC50	0.6	nM	CHEMBL5980310
9.19	IC50	0.65	nM	CHEMBL590646
9.17	IC50	0.68	nM	CHEMBL372443
9.15	IC50	0.7	nM	CHEMBL186908
9.14	IC50	0.73	nM	CHEMBL2153646
9.12	IC50	0.76	nM	CHEMBL2153645
9.12	IC50	0.76	nM	CHEMBL431496
9.11	IC50	0.77	nM	CHEMBL208470
9.10	IC50	0.8	nM	CHEMBL113853
9.06	IC50	0.88	nM	CHEMBL437072
9.05	IC50	0.9	nM	CHEMBL111401
9.05	IC50	0.9	nM	CHEMBL392303
9.05	IC50	0.89	nM	CHEMBL37674
9.02	IC50	0.96	nM	CHEMBL228605
9.02	IC50	0.96	nM	CHEMBL37906
9.00	IC50	1	nM	CHEMBL2153643
9.00	IC50	1	nM	CHEMBL113853
9.00	IC50	1	nM	CHEMBL5748399
9.00	IC50	1	nM	CHEMBL5828678

PubChem BioAssay actives

451 with measured affinity, of 607 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
2-[7-[[4-(1,4,5,6-tetrahydropyrimidin-2-ylamino)butanoylamino]methyl]-8,9-dihydro-5H-benzo[7]annulen-9-yl]acetic acid	217444: Displacement of vitronectin from human integrin alphaV-beta5	ic50	0.0001	uM
2-[(2S,5R,8S,11S)-5-benzyl-11-[3-(diaminomethylideneamino)propyl]-7-methyl-3,6,9,12,15-pentaoxo-8-propan-2-yl-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid	256969: Displacement of [125I]-echistatin from alpha-v-beta-5 integrin receptor	ic50	0.0001	uM
2-[(2S,5R,8S,11S)-5-benzyl-11-[3-(diaminomethylideneamino)propyl]-3,6,9,12,15-pentaoxo-8-propan-2-yl-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid	256969: Displacement of [125I]-echistatin from alpha-v-beta-5 integrin receptor	ic50	0.0001	uM
4-[(2S,5S,11S,14R)-14-benzyl-11-(carboxymethyl)-5-[3-(diaminomethylideneamino)propyl]-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]butanoic acid	456270: Displacement of [125I]echistatin from integrin alphaVbeta5 receptor after 3 hrs by gamma counting	ic50	0.0002	uM
2-[7-[[4-(4,5-dihydro-1H-imidazol-2-ylamino)butanoylamino]methyl]-8,9-dihydro-5H-benzo[7]annulen-9-yl]acetic acid	217444: Displacement of vitronectin from human integrin alphaV-beta5	ic50	0.0002	uM
3-pyridin-3-yl-3-[5-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]indol-1-yl]propanoic acid	290108: Binding affinity to Integrin alpha-v-beta-5 receptor by ELISA assay	ic50	0.0002	uM
2-[7-[[4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)butanoylamino]methyl]-8,9-dihydro-5H-benzo[7]annulen-9-yl]acetic acid	217444: Displacement of vitronectin from human integrin alphaV-beta5	ic50	0.0003	uM
2-[(2S,5R,8S,11S)-5-benzyl-8-[4-[[[2-[2-[2-(carboxymethoxy)ethoxy]ethoxy]acetyl]amino]methyl]phenyl]-11-[3-(diaminomethylideneamino)propyl]-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid	456270: Displacement of [125I]echistatin from integrin alphaVbeta5 receptor after 3 hrs by gamma counting	ic50	0.0003	uM
3-[4-[[3-(diaminomethylideneamino)benzoyl]amino]-2-methoxyphenyl]-2-(propan-2-yloxycarbonylamino)propanoic acid	35533: Binding affinity towards alpha V-beta5 receptor expressed in HEK293 cells	ic50	0.0004	uM
3-[2-methoxy-4-[[3-(1,4,5,6-tetrahydropyrimidin-2-ylamino)benzoyl]amino]phenyl]-2-(propan-2-yloxycarbonylamino)propanoic acid	35533: Binding affinity towards alpha V-beta5 receptor expressed in HEK293 cells	ic50	0.0004	uM
2-[(2S,5R,8S,11S)-5-benzyl-11-[3-(diaminomethylideneamino)propyl]-8-[4-[2-[(Z)-[(19S)-19-ethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4,6,8,10,15(20)-heptaen-10-yl]methylideneamino]oxyethylamino]-4-oxobutyl]-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid	456270: Displacement of [125I]echistatin from integrin alphaVbeta5 receptor after 3 hrs by gamma counting	ic50	0.0004	uM
2-[7-[[4-(1H-benzimidazol-2-ylamino)butanoylamino]methyl]-8,9-dihydro-5H-benzo[7]annulen-9-yl]acetic acid	217444: Displacement of vitronectin from human integrin alphaV-beta5	ic50	0.0005	uM
3-(1,3-benzodioxol-5-yl)-3-[5-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]indol-1-yl]propanoic acid	290108: Binding affinity to Integrin alpha-v-beta-5 receptor by ELISA assay	ic50	0.0005	uM
2-[(1R,4S,10S,13R)-10-[3-(diaminomethylideneamino)propyl]-3,6,9,12-tetraoxo-2,5,8,11-tetrazabicyclo[11.2.1]hexadecan-4-yl]acetic acid;hydrochloride	256969: Displacement of [125I]-echistatin from alpha-v-beta-5 integrin receptor	ic50	0.0006	uM
2-[(2S,5R,8S,11S)-5-benzyl-11-[3-(diaminomethylideneamino)propyl]-8-[4-[[[2-[2-[2-(2-hydrazinyl-2-oxoethoxy)ethoxy]ethoxy]acetyl]amino]methyl]phenyl]-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid	456270: Displacement of [125I]echistatin from integrin alphaVbeta5 receptor after 3 hrs by gamma counting	ic50	0.0006	uM
3-phenyl-3-[5-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]indol-1-yl]propanoic acid	290108: Binding affinity to Integrin alpha-v-beta-5 receptor by ELISA assay	ic50	0.0007	uM
(2S)-2-[[4-[4-[[(19S)-8-[(dimethylamino)methyl]-19-ethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaen-7-yl]oxycarbonyl]piperazine-1-carbonyl]phenyl]methoxycarbonylamino]-5-oxo-5-[4-[3-(1,4,5,6-tetrahydropyrimidin-2-ylamino)phenyl]piperazin-1-yl]pentanoic acid	690724: Displacement of [125I]echistatin from integrin alpha5beta5 after 3 hrs by gamma counter	ic50	0.0007	uM
3-(2-methylpyrimidin-5-yl)-4-[1-[3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propanoyl]piperidin-4-yl]butanoic acid	1177801: Antagonist activity at alphavbeta5 integrin receptor (unknown origin) by cell-free ELISA	ic50	0.0007	uM
3-[4-[[3-(diaminomethylideneamino)benzoyl]amino]phenyl]-2-(propan-2-yloxycarbonylamino)propanoic acid	35533: Binding affinity towards alpha V-beta5 receptor expressed in HEK293 cells	ic50	0.0008	uM
(2S)-2-[[4-[4-[[(19S)-19-ethyl-19-hydroxy-10-[(E)-(2-methylpropan-2-yl)oxyiminomethyl]-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaen-7-yl]oxycarbonyl]piperazine-1-carbonyl]phenyl]methoxycarbonylamino]-5-oxo-5-[4-[3-(1,4,5,6-tetrahydropyrimidin-2-ylamino)phenyl]piperazin-1-yl]pentanoic acid	690724: Displacement of [125I]echistatin from integrin alpha5beta5 after 3 hrs by gamma counter	ic50	0.0008	uM
3-(1,3-benzodioxol-5-yl)-4-[1-methyl-5-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]pyrazol-3-yl]butanoic acid	265729: Inhibition of alpha-v-beta-5 integrin in 293 cells	ic50	0.0008	uM
2-[7-[[4-(pyridin-2-ylamino)butanoylamino]methyl]-8,9-dihydro-5H-benzo[7]annulen-9-yl]acetic acid	217444: Displacement of vitronectin from human integrin alphaV-beta5	ic50	0.0008	uM
2-[7-[[5-(pyridin-2-ylamino)pentanoylamino]methyl]-8,9-dihydro-5H-benzo[7]annulen-9-yl]acetic acid	217444: Displacement of vitronectin from human integrin alphaV-beta5	ic50	0.0009	uM
3-[4-[[3-[(5-oxo-1,4-dihydroimidazol-2-yl)amino]benzoyl]amino]phenyl]-2-(propan-2-yloxycarbonylamino)propanoic acid	35533: Binding affinity towards alpha V-beta5 receptor expressed in HEK293 cells	ic50	0.0009	uM
2-[(1S,4S,10S,13S)-10-[3-(diaminomethylideneamino)propyl]-14-heptyl-3,6,9,12-tetraoxo-2,5,8,11,14-pentazabicyclo[11.2.1]hexadecan-4-yl]acetic acid	317270: Displacement of [125I]echistatin from human integrin alphaVbeta5 receptor high affinity state by solid phase assay	ic50	0.0009	uM
2-[(1S,3R,9S,11R,14S)-9-[3-(diaminomethylideneamino)propyl]-4,7,10,18-tetraoxo-2,5,8,19-tetrazatricyclo[9.6.2.014,19]nonadecan-3-yl]acetic acid	317263: Displacement of [125I]echistatin from human integrin alpha-V-beta-5 receptor by solid phase assay	ic50	0.0009	uM
3-(1,3-benzodioxol-5-yl)-4-[5-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]-1-(2,2,2-trifluoroethyl)pyrazol-3-yl]butanoic acid	265729: Inhibition of alpha-v-beta-5 integrin in 293 cells	ic50	0.0010	uM
3-pyridin-3-yl-3-[4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]indol-1-yl]propanoic acid	290108: Binding affinity to Integrin alpha-v-beta-5 receptor by ELISA assay	ic50	0.0010	uM
3-[4-[[3-(diaminomethylideneamino)benzoyl]amino]phenyl]-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoic acid	35533: Binding affinity towards alpha V-beta5 receptor expressed in HEK293 cells	ic50	0.0010	uM
2-(benzenesulfonamido)-3-[4-[[3-(1,4,5,6-tetrahydropyrimidin-2-ylamino)benzoyl]amino]phenyl]propanoic acid	35533: Binding affinity towards alpha V-beta5 receptor expressed in HEK293 cells	ic50	0.0010	uM
(3S)-3-[[2-[4-[3-(diaminomethylideneamino)propyl]triazol-1-yl]acetyl]amino]-3-phenylpropanoic acid	1177801: Antagonist activity at alphavbeta5 integrin receptor (unknown origin) by cell-free ELISA	ic50	0.0010	uM
(2S)-2-[[4-[4-[[(19S)-10,19-diethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaen-7-yl]oxycarbonyl]piperazine-1-carbonyl]phenyl]methoxycarbonylamino]-5-oxo-5-[4-[3-(1,4,5,6-tetrahydropyrimidin-2-ylamino)phenyl]piperazin-1-yl]pentanoic acid;hydrochloride	690724: Displacement of [125I]echistatin from integrin alpha5beta5 after 3 hrs by gamma counter	ic50	0.0010	uM
2-[(1R,4S,10S,13R)-10-[3-(diaminomethylideneamino)propyl]-3,6,9,12-tetraoxo-2,5,8,11-tetrazabicyclo[11.2.1]hexadecan-4-yl]acetic acid	317263: Displacement of [125I]echistatin from human integrin alpha-V-beta-5 receptor by solid phase assay	ic50	0.0011	uM
3-phenyl-3-[4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]indol-1-yl]propanoic acid	290108: Binding affinity to Integrin alpha-v-beta-5 receptor by ELISA assay	ic50	0.0011	uM
3-(1,3-benzodioxol-5-yl)-4-[3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]-1,2-oxazol-5-yl]butanoic acid	265729: Inhibition of alpha-v-beta-5 integrin in 293 cells	ic50	0.0012	uM
3-(2-cyclopropyl-1,3-thiazol-5-yl)-4-[3-[3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl]-1,2,4-oxadiazol-5-yl]butanoic acid	260720: Inhibition of Integrin alphav-beta5 receptor expressed in HEK293 cell line	ic50	0.0012	uM
2-[(9S)-14-[3-(pyridin-2-ylamino)propoxy]-9-tricyclo[9.4.0.03,8]pentadeca-1(11),3,5,7,12,14-hexaenyl]acetic acid	223420: Binding affinity for integrin alpha V beta 5 receptor	ki	0.0013	uM
2-[2-[4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]phenyl]cyclopropyl]acetic acid	287982: Inhibition of integrin alpha-v-beta-5 receptor expressed in HEK293 cells	ic50	0.0014	uM
2-[(1R,4S,10S,13S,16R)-10-[3-(diaminomethylideneamino)propyl]-3,6,9,12,20-pentaoxo-2,5,8,11,21-pentazatricyclo[11.6.2.016,21]henicosan-4-yl]acetic acid	709959: Competitive inhibition of biotinylated vitronectin to integrin alphaVbeta5 receptor after 3 hrs by microplate reader analysis	ic50	0.0014	uM
3-(1,3-benzodioxol-5-yl)-4-[3-[2-(1-methyl-3,4-dihydro-2H-pyrido[2,3-b]pyrazin-6-yl)ethoxy]-1,2-oxazol-5-yl]butanoic acid	265729: Inhibition of alpha-v-beta-5 integrin in 293 cells	ic50	0.0015	uM
(3S)-3-(1,3-benzodioxol-5-yl)-4-[3-[3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl]-1,2,4-oxadiazol-5-yl]butanoic acid	260720: Inhibition of Integrin alphav-beta5 receptor expressed in HEK293 cell line	ic50	0.0017	uM
(2S)-3-[[4-[[1H-benzimidazol-2-ylmethyl(cyclohexylcarbamoyl)amino]methyl]benzoyl]amino]-2-(phenylmethoxycarbonylamino)propanoic acid	1177801: Antagonist activity at alphavbeta5 integrin receptor (unknown origin) by cell-free ELISA	ic50	0.0017	uM
3-(1,3-benzodioxol-5-yl)-4-[1-benzyl-5-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]pyrazol-3-yl]butanoic acid	265729: Inhibition of alpha-v-beta-5 integrin in 293 cells	ic50	0.0018	uM
3-(1,3-benzodioxol-5-yl)-4-[1-methyl-5-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethylsulfonyl]pyrazol-3-yl]butanoic acid	265729: Inhibition of alpha-v-beta-5 integrin in 293 cells	ic50	0.0019	uM
2-[(1R,4S,10S,13S)-10-[3-(diaminomethylideneamino)propyl]-3,6,9,12-tetraoxo-2,5,8,11,14-pentazabicyclo[11.2.1]hexadecan-4-yl]acetic acid	317270: Displacement of [125I]echistatin from human integrin alphaVbeta5 receptor high affinity state by solid phase assay	ic50	0.0019	uM
(2S)-3-[[2,5-dimethyl-6-[4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)piperidin-1-yl]pyrimidin-4-yl]amino]-2-[(4-methoxyphenyl)sulfonylamino]propanoic acid	1177801: Antagonist activity at alphavbeta5 integrin receptor (unknown origin) by cell-free ELISA	ic50	0.0020	uM
3-(1,3-benzodioxol-5-yl)-4-[3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]-1H-pyrazol-5-yl]butanoic acid	265729: Inhibition of alpha-v-beta-5 integrin in 293 cells	ic50	0.0021	uM
(2S)-2-[[4-[4-[[(19S)-19-ethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2(11),3,5,7,9,15(20)-heptaen-7-yl]oxycarbonyl]piperazine-1-carbonyl]phenyl]methoxycarbonylamino]-5-oxo-5-[4-[3-(1,4,5,6-tetrahydropyrimidin-2-ylamino)phenyl]piperazin-1-yl]pentanoic acid	690724: Displacement of [125I]echistatin from integrin alpha5beta5 after 3 hrs by gamma counter	ic50	0.0021	uM
(2S)-2-(benzenesulfonamido)-3-[[5-[2-[(diaminomethylideneamino)methyl]phenyl]thiophene-2-carbonyl]amino]propanoic acid;2,2,2-trifluoroacetic acid	220621: Inhibition of vitronectin binding to HT-29 cells expressing integrin alphaV-beta5	ic50	0.0022	uM
(3R)-3-quinolin-3-yl-4-[1-[3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propanoyl]piperidin-4-yl]butanoic acid	241459: Inhibitory concentration for human vitronectin binding to immobilized alphaV-beta5 integrin	ic50	0.0022	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects cotreatment, decreases expression, affects expression	5
Cadmium Chloride	decreases expression, increases expression	4
bisphenol A	decreases expression, decreases methylation, increases expression	3
trichostatin A	affects cotreatment, decreases expression	3
bisphenol F	increases expression, affects cotreatment, decreases expression	2
enzacamene	decreases expression, increases expression	2
entinostat	decreases expression, affects cotreatment	2
lipopolysaccharide, Escherichia coli O111 B4	affects reaction, increases secretion, affects binding, decreases reaction, increases expression	2
Panobinostat	affects cotreatment, decreases expression	2
Air Pollutants	affects cotreatment, increases abundance, increases oxidation, decreases expression	2
Arsenic	affects methylation, increases abundance, increases expression	2
Copper	affects binding, affects expression, increases expression	2
Hydrogen Peroxide	decreases expression, increases expression	2
Phenylmercuric Acetate	affects cotreatment, decreases expression	2
Polycyclic Aromatic Hydrocarbons	affects cotreatment, decreases expression, increases abundance, affects expression	2
Tobacco Smoke Pollution	decreases expression, increases expression	2
Particulate Matter	decreases expression, increases abundance, affects cotreatment	2
triphenyl phosphate	affects expression	1
alpha-pinene	affects cotreatment, increases oxidation, increases abundance	1
methylselenic acid	decreases expression	1
beta-lapachone	increases expression	1
methylparaben	decreases expression	1
trimellitic anhydride	increases expression	1
sodium bichromate	decreases expression	1
fenvalerate	decreases expression	1
sodium arsenite	increases abundance, increases expression	1
cobaltous chloride	decreases expression, increases expression	1
manganese chloride	increases expression	1
bleomycetin	increases expression	1
methacrylaldehyde	affects cotreatment, increases oxidation, increases abundance	1

ChEMBL screening assays

78 unique, capped per target: 76 binding, 2 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1042925	Binding	Inhibition of integrin alpha5beta5 receptor by ELISA	SAR of N-phenyl piperidine based oral integrin alpha5beta1 antagonists. — Bioorg Med Chem Lett
CHEMBL816280	Functional	Inhibition of integrin alpha-v/beta-5 mediated UCLAP-3 cell adhesion on vitronectin; ND is Not Determined.	Nanomolar small molecule inhibitors for alphav(beta)6, alphav(beta)5, and alphav(beta)3 integrins. — J Med Chem

Cellosaurus cell lines

5 cell lines: 5 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_E0FL	Ubigene HeLa ITGB5 KO	Cancer cell line	Female
CVCL_ST49	HAP1 ITGB5 (-) 1	Cancer cell line	Male
CVCL_ST50	HAP1 ITGB5 (-) 2	Cancer cell line	Male
CVCL_ST51	HAP1 ITGB5 (-) 3	Cancer cell line	Male
CVCL_ST52	HAP1 ITGB5 (-) 4	Cancer cell line	Male

Clinical trials (associated diseases)

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