ITGB6

Summary

ITGB6 (integrin subunit beta 6, HGNC:6161) is a protein-coding gene on chromosome 2q24.2, encoding Integrin beta-6 (P18564). Integrin alpha-V:beta-6 (ITGAV:ITGB6) is a receptor for fibronectin and cytotactin.

This gene encodes a protein that is a member of the integrin superfamily. Members of this family are adhesion receptors that function in signaling from the extracellular matrix to the cell. Integrins are heterodimeric integral membrane proteins composed of an alpha chain and a beta chain. The encoded protein forms a dimer with an alpha v chain and this heterodimer can bind to ligands like fibronectin and transforming growth factor beta 1. Alternate splicing results in multiple transcript variants.

Source: NCBI Gene 3694 — RefSeq curated summary.

At a glance

• Gene–disease (curated): amelogenesis imperfecta type 1H (Strong, GenCC) — +2 more curated relationships
• GWAS associations: 12
• Clinical variants (ClinVar): 225 total — 5 pathogenic, 5 likely-pathogenic
• Phenotypes (HPO): 32
• Druggable target: yes — 5 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_000888

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:6161
Approved symbol	ITGB6
Name	integrin subunit beta 6
Location	2q24.2
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000115221
Ensembl biotype	protein_coding
OMIM	147558
Entrez	3694

Gene structure

Transcript identifiers

Ensembl transcripts: 19 — 14 protein_coding, 2 nonsense_mediated_decay, 2 protein_coding_CDS_not_defined, 1 retained_intron

ENST00000283249, ENST00000409583, ENST00000409872, ENST00000409967, ENST00000428609, ENST00000475438, ENST00000485635, ENST00000498478, ENST00000620391, ENST00000652612, ENST00000873501, ENST00000873502, ENST00000873503, ENST00000958489, ENST00000958490, ENST00000958491, ENST00000958492, ENST00000958493, ENST00000958494

RefSeq mRNA: 7 — MANE Select: NM_000888 NM_000888, NM_001282353, NM_001282354, NM_001282355, NM_001282388, NM_001282389, NM_001282390

CCDS: CCDS2212, CCDS63040, CCDS74596, CCDS74597

Canonical transcript exons

ENST00000283249 — 15 exons

Exon	Start	End
ENSE00001215293	160099671	160101834
ENSE00001716162	160199179	160199258
ENSE00001900255	160200003	160200272
ENSE00003508997	160141982	160142071
ENSE00003523456	160126379	160126601
ENSE00003527585	160172569	160172730
ENSE00003545248	160137434	160137851
ENSE00003547665	160195369	160195615
ENSE00003549151	160196216	160196420
ENSE00003552511	160173974	160174139
ENSE00003565313	160107679	160107845
ENSE00003573213	160112080	160112199
ENSE00003607004	160138065	160138199
ENSE00003652443	160169212	160169307
ENSE00003689085	160123791	160123888

Expression profiles

Bgee: expression breadth ubiquitous, 188 present calls, max score 96.91.

FANTOM5 (CAGE): breadth broad, TPM avg 5.3998 / max 425.9074, expressed in 343 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter ID	TPM avg	Samples expressed
31468	4.5005	334
31469	0.5704	199
31470	0.1736	99
31467	0.1389	59
31466	0.0165	5

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
visceral pleura	UBERON:0002401	96.91	gold quality
biceps brachii	UBERON:0001507	96.87	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	96.54	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	95.52	gold quality
palpebral conjunctiva	UBERON:0001812	92.88	gold quality
lower lobe of lung	UBERON:0008949	91.53	gold quality
metanephros cortex	UBERON:0010533	91.47	gold quality
vastus lateralis	UBERON:0001379	91.10	gold quality
body of tongue	UBERON:0011876	90.97	gold quality
hindlimb stylopod muscle	UBERON:0004252	89.43	gold quality
quadriceps femoris	UBERON:0001377	88.91	gold quality
skeletal muscle tissue	UBERON:0001134	88.81	gold quality
mammary duct	UBERON:0001765	88.57	gold quality
esophagus squamous epithelium	UBERON:0006920	88.57	gold quality
islet of Langerhans	UBERON:0000006	88.36	gold quality
triceps brachii	UBERON:0001509	87.65	gold quality
jejunal mucosa	UBERON:0000399	87.40	gold quality
diaphragm	UBERON:0001103	87.15	gold quality
upper lobe of lung	UBERON:0008948	86.75	gold quality
upper lobe of left lung	UBERON:0008952	86.28	gold quality
gall bladder	UBERON:0002110	86.20	gold quality
gingival epithelium	UBERON:0001949	85.87	gold quality
jejunum	UBERON:0002115	85.08	gold quality
epithelium of mammary gland	UBERON:0003244	84.94	gold quality
lung	UBERON:0002048	84.71	gold quality
esophagus mucosa	UBERON:0002469	84.63	gold quality
gingiva	UBERON:0001828	83.93	gold quality
colonic mucosa	UBERON:0000317	83.54	gold quality
muscle tissue	UBERON:0002385	83.38	gold quality
deltoid	UBERON:0001476	83.07	gold quality

Single-cell (SCXA)

Detected in 7 experiment(s), a significant marker in 7.

Experiment	Marker?	Max mean expression
E-GEOD-131882	yes	2203.09
E-CURD-119	yes	1647.33
E-GEOD-75688	yes	918.80
E-GEOD-83139	yes	909.23
E-GEOD-130148	yes	10.27
E-ENAD-27	yes	6.73
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

119 targeting ITGB6, 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-8485	100.00	77.57	4731
HSA-MIR-126-5P	100.00	72.71	3180
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-6833-3P	100.00	70.63	3197
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-4768-5P	100.00	69.49	2861
HSA-MIR-4682	100.00	68.89	1258
HSA-MIR-3617-3P	99.98	67.86	918
HSA-MIR-4482-3P	99.98	72.50	3147
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-507	99.97	70.11	1915
HSA-MIR-4666A-3P	99.96	71.71	3434
HSA-MIR-1250-3P	99.96	70.04	4038
HSA-MIR-3605-5P	99.96	67.12	932
HSA-MIR-559	99.95	72.28	3609
HSA-MIR-548AB	99.95	71.31	3488
HSA-MIR-23A-3P	99.95	74.24	3163
HSA-MIR-23B-3P	99.95	74.24	3163
HSA-MIR-23C	99.95	73.92	3192
HSA-MIR-548A-5P	99.94	71.27	3482
HSA-MIR-548AD-5P	99.94	71.23	3502
HSA-MIR-548AE-5P	99.94	71.23	3502
HSA-MIR-548AK	99.94	71.24	3488
HSA-MIR-548AM-5P	99.94	71.24	3488
HSA-MIR-548AP-5P	99.94	71.14	3489
HSA-MIR-548AQ-5P	99.94	71.34	3426
HSA-MIR-548AR-5P	99.94	71.28	3515
HSA-MIR-548AS-5P	99.94	71.22	3482
HSA-MIR-548AU-5P	99.94	71.24	3488
HSA-MIR-548AY-5P	99.94	71.23	3502

Literature-anchored findings (GeneRIF, showing 40)

• Integrin expression in colon cancer cells is regulated by the cytoplasmic domain of the beta6 integrin subunit (PMID:11992542)
• Loss of integrin alpha(v)beta6-mediated TGF-beta activation causes Mmp12-dependent emphysema (PMID:12634787)
• upon ligation of integrin beta6 with fibronectin, beta6 complexed with Fyn and activated it, activating a pathway leading to activation of the matrix metalloproteinase-3 gene, and promoting oral SCC cell proliferation and experimental metastasis in vivo (PMID:12917446)
• integrin alpha(v)beta(6) is an RGD-dependent receptor for Coxsackievirus A9 and may be important in natural Coxsackievirus A9 infections (PMID:15194773)
• beta(6) integrin is not normally expressed in adult native or transplanted kidneys but is commonly up-regulated in the distal tubule in disease. (PMID:15458435)
• We conclude that integrin alphavbeta6-dependent MMP-2 and -9 up-regulation is an important feature of increased migration in hypoxic human keratinocytes. (PMID:15828940)
• integrin alphavbeta6, alphavbeta3, alphavbeta5, alpha5beta1 and alpha9beta1 binding to osteopontin is controlled by specific structural motifs that are recognized by extracellular proteases (PMID:16005200)
• Alphavbeta6 integrin down-regulates MMP-13 expression in oral squamous cell carcinoma cells. (PMID:16024014)
• Mn(2+) promoted convergent changes in integrin alphavbeta6 conformation and Fb structure through activation of ERK/MAPK and MMP-9 (PMID:17275949)
• Constitutively activated STAT3 induces tumorigenesis and enhances cell motility of prostate epithelial cells through ITGB6. (PMID:17438134)
• Integrin alphavbeta6 is induced de novo in rodent and human liver fibrosis, where it is expressed on activated bile duct epithelia and (transitional) hepatocytes during fibrosis progression. (PMID:18221819)
• These results suggest that activation of TGF-beta1 by integrin alphavbeta6 contributes to pathological changes and may impair endothelial cell functions in tissues that are chronically infected with cytomegalovirus. (PMID:18349127)
• overexpressed in endometrial carcinomas, especially with high grade and in lymph node metastases (PMID:18698261)
• These data suggest that Coxsackievirus A9 binding to alphaVbeta6 is a high-affinity interaction, which may indicate its importance in clinical infections (PMID:19088289)
• Results show that alphavbeta6- and alpha5beta1-integrin-dependent activation of Rac1 was mediated through Eps8. (PMID:19448673)
• Tumors express alpha(v)beta(6) suggest that this probe has significant potential for the in vivo detection of the malignancy. (PMID:19549907)
• VEGF is critical to the invasive process in human gastric cancer and that this occurs via up-regulation of integrin alphavbeta6 expression and activation of ERK. (PMID:19581046)
• Fusion of epithelial cells by Epstein-Barr virus proteins is triggered by binding of viral glycoproteins gHgL to integrins alphavbeta6 or alphavbeta8. (PMID:19920174)
• Alpha(V)beta(6), but not alpha(V)beta(3), blocked human parechovirus 1 cellular infectivity. (PMID:20554778)
• Saturation transfer difference NMR was applied to the interaction of the integrin alphavbeta6 with a known peptide ligand and highlights novel contact points between the substrate and target protein (PMID:20838674)
• Integrin beta6 plays a role in the compromised wound healing associated with the diabetic state. (PMID:20854469)
• TF-PAR-1 pathway contributes to liver fibrosis induced by chronic cholestasis by increasing expression of the alphaVbeta6 integrin, an important regulator of transforming growth factor-beta1 activation. (PMID:21037076)
• These data identify a novel interaction between Psor and beta6 and demonstrate that it is required for alphavbeta6-dependent invasion by carcinoma cells. (PMID:21132011)
• The authors demonstrated that both integrins alphavbeta6 and alphavbeta8 can serve as specific receptors for Epstein-Barr virus gHgL proteins. (PMID:21178476)
• The endoproteolytic cleavage of alphav subunits is necessary for alphavbeta5/beta6 integrin to control alpha2beta1 function and could thus play an essential role in colon cancer cell migration. (PMID:21787362)
• Data suggest that colorectal cancer (CRC)-derived integrin alphavbeta6 is involved in the establishment of tumor immune tolerance in local tissues. (PMID:21913024)
• Data indicate that integrin beta6, CD46, tissue factor, and chromosome 14 open reading frame 1 (C14ORF1), were identified as overexpressed on pancreatic cancer cell lines. (PMID:21934552)
• our findings indicate that alphavbeta6 and TGF-beta act in a common tumor suppressor pathway (PMID:22787119)
• Increased alphavbeta6 integrin expression is associated with poor prognosis and decreased survival in oral squamous cell carcinoma patients. (PMID:23331428)
• the integrin avb6 plays an important role in the fusion of endosome/lysosome in corneal epithelial cells; inhibition of avb6 results in corneal epithelial barrier dysfunction. (PMID:23412966)
• Results show that stromal cell-derived factor-1 (SDF-1) enhanced ovarian cancer cell invasion through alphavbeta6 integrin-mediated urokinase-type plasminogen activator (uPA) expression via the p38 MAPK and PI3 K/Akt pathway. (PMID:23615713)
• ADAM 10 is over expressed in oral squamous cell carcinoma and contributes to invasive behaviour through a functional association with alphavbeta6 integrin (PMID:24055471)
• upregulation of alphavbeta6 on myoepithelial cells generates a tumor promoter function through TGFbeta upregulation of MMP-9. These data suggest that expression of alphavbeta6 may be used to stratify patients with DCIS. (PMID:24150233)
• Brain metastases ITGB6 expression exhibits considerable heterogeneity according to tumor origin. (PMID:24294359)
• ITGB6 loss-of-function mutations cause autosomal recessive amelogenesis imperfecta. (PMID:24305999)
• alphavbeta6- and alphavbeta8-integrins acted independently and are thus interchangeable as receptors for Herpes simplex type 1 virus entry. (PMID:24367260)
• In conclusion NSCLC cell lines, positive for E-Cadherin,EpCAM and avb6 expression, activate normal fibroblasts through avbeta6/TGFbeta signalling in vitro, and influence both gene expression and response to therapeutic agents. (PMID:24488011)
• Expression of Gli1 and alphavbeta6 inversely correlates in tumours in vivo, and Hh targeting up-regulates TGF-beta1/Smad2/3-dependent alphavbeta6 expression, promoting pro-tumourigenic cell functions in vitro. (PMID:24573955)
• The deficiency of avb6-related hyperpermeability in T84 monolayers could be compensated by adding exogenous avb6 to the culture. (PMID:24677750)
• Integrin beta6 expression correlated significantly with MMP-9 expression, and may be a valuable recurrence indicator for follicular thyroid carcinomas (PMID:24844802)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	itgb6	ENSDARG00000002494
mus_musculus	Itgb6	ENSMUSG00000026971
rattus_norvegicus	Itgb6	ENSRNOG00000008346

Paralogs (8): ITGB5 (ENSG00000082781), ITGB8 (ENSG00000105855), ITGB4 (ENSG00000132470), ITGB7 (ENSG00000139626), ITGB1 (ENSG00000150093), ITGB2 (ENSG00000160255), ITGBL1 (ENSG00000198542), ITGB3 (ENSG00000259207)

Protein

Protein identifiers

Integrin beta-6 — P18564 (reviewed: P18564)

All UniProt accessions (5): A0A087WXP3, A0AAQ5BIF8, E9PEE8, P18564, F8WBJ8

UniProt curated annotations — full annotation on UniProt →

Function. Integrin alpha-V:beta-6 (ITGAV:ITGB6) is a receptor for fibronectin and cytotactin. It recognizes the sequence R-G-D in its ligands. Internalization of integrin alpha-V/beta-6 via clathrin-mediated endocytosis promotes carcinoma cell invasion. ITGAV:ITGB6 acts as a receptor for fibrillin-1 (FBN1) and mediates R-G-D-dependent cell adhesion to FBN1. Integrin alpha-V:beta-6 (ITGAV:ITGB6) mediates R-G-D-dependent release of transforming growth factor beta-1 (TGF-beta-1) from regulatory Latency-associated peptide (LAP), thereby playing a key role in TGF-beta-1 activation. (Microbial infection) Integrin ITGAV:ITGB6 acts as a receptor for Coxsackievirus A9 and Coxsackievirus B1. (Microbial infection) Integrin ITGAV:ITGB6 acts as a receptor for Herpes simplex virus-1/HHV-1.

Subunit / interactions. Heterodimer of an alpha and a beta subunit. Interacts with FLNB. Interacts with HAX1. ITGAV:ITGB6 interacts with FBN1. ITGAV:ITGB6 interacts with TGFB1. (Microbial infection) Integrin ITGAV:ITGB6 interacts with coxsackievirus A9, coxsackievirus B1 capsid proteins. (Microbial infection) Integrin ITGAV:ITGB6 interacts with herpes simplex virus-1/HHV-1 gH:gL proteins.

Subcellular location. Cell membrane. Cell junction. Focal adhesion.

Disease relevance. Amelogenesis imperfecta 1H (AI1H) [MIM:616221] A disorder characterized by defective enamel formation, resulting in hypoplastic and hypomineralized tooth enamel that may be rough, pitted, and/or discolored. The disease is caused by variants affecting the gene represented in this entry.

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.

Isoforms (2)

UniProt ID	Names	Canonical?
P18564-1	1	yes
P18564-2	2

RefSeq proteins (7): NP_000879, NP_001269282, NP_001269283, NP_001269284, NP_001269317, NP_001269318, NP_001269319 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002369	Integrin_bsu_VWA	Domain
IPR012896	Integrin_bsu_tail	Domain
IPR013111	EGF_extracell	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
IPR057243	Integrin_I-EGF_CS	Conserved_site

Pfam: PF00362, PF07965, PF07974, PF08725, PF17205, PF18372, PF23105

UniProt features (110 total): disulfide bond 28, strand 20, helix 16, binding site 14, glycosylation site 9, domain 6, turn 6, sequence variant 4, topological domain 2, signal peptide 1, chain 1, region of interest 1, transmembrane region 1, splice variant 1

Structure

Experimental structures (PDB)

14 structures.

PDB	Method	Resolution (Å)
9CZD	X-RAY DIFFRACTION	2.23
5FFG	X-RAY DIFFRACTION	2.25
9CZA	X-RAY DIFFRACTION	2.49
4UM9	X-RAY DIFFRACTION	2.5
9CZF	X-RAY DIFFRACTION	2.53
9CZ7	X-RAY DIFFRACTION	2.57
4UM8	X-RAY DIFFRACTION	2.85
9XMM	ELECTRON MICROSCOPY	2.88
8TCG	ELECTRON MICROSCOPY	3.4
5FFO	X-RAY DIFFRACTION	3.49
5NET	ELECTRON MICROSCOPY	8.6
5NEM	ELECTRON MICROSCOPY	10.8
5NER	ELECTRON MICROSCOPY	11.5
5NEU	ELECTRON MICROSCOPY	12.3

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P18564-F1	82.96	0.40

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 (14): 140 (in midas binding site); 142 (in midas binding site); 144 (in admidas binding site); 144 (in midas binding site); 147 (in admidas binding site); 148 (in admidas binding site); 179 (in limbs binding site); 235 (in limbs binding site); 237 (in limbs binding site); 239 (in limbs binding site); 240 (in limbs binding site); 240 (in midas binding site) …

Disulfide bonds (28): 23–41, 31–454, 34–59, 44–70, 197–204, 252–293, 394–406, 426–452, 456–476, 467–479, 481–490, 492–519, 502–517, 511–522, 524–537, 539–560, 544–558, 552–563, 565–574, 576–599 …

Glycosylation sites (9): 48, 97, 260, 387, 396, 463, 471, 541, 575

Function

Pathways and Gene Ontology

Reactome pathways

9 pathways

ID	Pathway
R-HSA-1566948	Elastic fibre formation
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-3000178	ECM proteoglycans
R-HSA-1474244	Extracellular matrix organization
R-HSA-162582	Signal Transduction
R-HSA-170834	Signaling by TGF-beta Receptor Complex
R-HSA-9006936	Signaling by TGFB family members

MSigDB gene sets: 320 (showing top): GOBP_MYELOID_CELL_DIFFERENTIATION, GOBP_RESPONSE_TO_IONIZING_RADIATION, GOBP_DENDRITIC_CELL_DIFFERENTIATION, REACTOME_SIGNALING_BY_TGF_BETA_RECEPTOR_COMPLEX, GU_PDEF_TARGETS_DN, GOBP_SKELETAL_SYSTEM_DEVELOPMENT, GOBP_INFLAMMATORY_RESPONSE, GOCC_CELL_SURFACE, TGACCTY_ERR1_Q2, GOBP_MYELOID_LEUKOCYTE_DIFFERENTIATION, GOBP_TOOTH_MINERALIZATION, SRF_Q5_01, HINATA_NFKB_TARGETS_KERATINOCYTE_UP, GOBP_LIPID_HOMEOSTASIS, GOBP_WOUND_HEALING

GO Biological Process (28): cell morphogenesis (GO:0000902), inflammatory response (GO:0006954), cell adhesion (GO:0007155), cell-matrix adhesion (GO:0007160), transforming growth factor beta receptor signaling pathway (GO:0007179), integrin-mediated signaling pathway (GO:0007229), response to virus (GO:0009615), cell migration (GO:0016477), cell adhesion mediated by integrin (GO:0033627), wound healing (GO:0042060), surfactant homeostasis (GO:0043129), memory T cell differentiation (GO:0043379), skin development (GO:0043588), lung alveolus development (GO:0048286), phospholipid homeostasis (GO:0055091), hard palate development (GO:0060022), bone development (GO:0060348), bronchiole development (GO:0060435), Langerhans cell differentiation (GO:0061520), enamel mineralization (GO:0070166), cellular response to ionizing radiation (GO:0071479), transforming growth factor beta production (GO:0071604), amelogenesis (GO:0097186), cell-cell adhesion (GO:0098609), immune response (GO:0006955), response to wounding (GO:0009611), gene expression (GO:0010467), 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), molecular function activator activity (GO:0140677), protein binding (GO:0005515)

GO Cellular Component (9): plasma membrane (GO:0005886), focal adhesion (GO:0005925), integrin complex (GO:0008305), external side of plasma membrane (GO:0009897), cell surface (GO:0009986), integrin alphav-beta6 complex (GO:0034685), signaling receptor complex (GO:0043235), membrane (GO:0016020), anchoring junction (GO:0070161)

Reactome top-level categories

Rollup of top-5 pathways:

Category	Pathways
Extracellular matrix organization	3
Elastic fibre formation	1
Signaling by TGF-beta Receptor Complex	1
Signaling by TGFB family members	1
Signal Transduction	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
animal organ development	2
lung development	2
anatomical structure development	2
cellular anatomical structure	2
anatomical structure morphogenesis	1
defense response	1
cellular process	1
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
response to other organism	1
cell motility	1
cell adhesion	1
response to wounding	1
tissue regeneration	1
multicellular organismal-level chemical homeostasis	1
T cell differentiation involved in immune response	1
immunological memory formation process	1
lipid homeostasis	1
secondary palate development	1
skeletal system development	1
respiratory tube development	1
myeloid dendritic cell differentiation	1
tooth mineralization	1
amelogenesis	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
molecular function regulator activity	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
plasma membrane	1

Protein interactions and networks

STRING

1432 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
ITGB6	ITGAV	P06756	871
ITGB6	FN1	P02751	820
ITGB6	S100A7	P31151	774
ITGB6	TLN1	Q9Y490	752
ITGB6	ITGA3	P26006	745
ITGB6	TGFB1	P01137	743
ITGB6	ITGA2	P17301	715
ITGB6	TGFB2	P08112	701
ITGB6	MMP12	P39900	701
ITGB6	ITGA1	P56199	688
ITGB6	ITGA6	P23229	642
ITGB6	ELN	P15502	638
ITGB6	TGFB3	P10600	603
ITGB6	ITGA4	P13612	598
ITGB6	TLN2	Q9Y4G6	586

IntAct

13 interactions, top by confidence:

A	B	Type	Score
ITGAV	ITGB6	psi-mi:“MI:0407”(direct interaction)	0.800
CFTR	ESYT2	psi-mi:“MI:2364”(proximity)	0.710
ITGAV	TGFB1	psi-mi:“MI:0915”(physical association)	0.490
ITGAV	TGFB3	psi-mi:“MI:0407”(direct interaction)	0.440
ITGB6	HMGN2	psi-mi:“MI:0915”(physical association)	0.400
	ITGAV	psi-mi:“MI:0407”(direct interaction)	0.360
CFTR	UBA6	psi-mi:“MI:2364”(proximity)	0.270

BioGRID (16): FHL2 (Affinity Capture-Western), ITGB6 (Proximity Label-MS), ITGB6 (Proximity Label-MS), ITGB6 (Proximity Label-MS), ITGB6 (Two-hybrid), ITGB6 (Two-hybrid), ITGB6 (Proximity Label-MS), ITGB6 (Reconstituted Complex), ITGB6 (Two-hybrid), ITGB6 (Affinity Capture-Western), ITGB6 (Reconstituted Complex), ITGB6 (Proximity Label-MS), HSPD1 (Cross-Linking-MS (XL-MS)), ITGB6 (Proximity Label-MS), MAPK1 (Affinity Capture-Western)

ESM2 similar proteins: A0A2D0TC04, A1A4K5, A2VDP5, A8K7I4, J3SBP3, J3SEZ3, O14638, P06802, P0DQQ4, P15396, P18563, P18564, P22413, P54793, P97259, P97675, Q08834, Q09328, Q13822, Q14CN2, Q1RPR6, Q29444, Q2TU62, Q32KH8, Q3SZI1, Q4FZV0, Q5FYA8, Q5GF25, Q5R5M5, Q64610, Q6AYF4, Q6DDW2, Q6DYE8, Q6NXH2, Q6PT52, Q6Q473, Q863C4, Q8BTJ4, Q8K1B9, Q8K2I4

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

6 interactions.

A	Effect	B	Mechanism
ITGB1BP1	“down-regulates activity”	ITGB6	binding
DOK1	“down-regulates activity”	ITGB6	binding
ITGB6	“up-regulates activity”	PTK2
Kindlin	“up-regulates activity”	ITGB6	binding
TLN1	“up-regulates activity”	ITGB6	binding
ITGB6	“form complex”	“Av/b6 integrin”	binding

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	5
Likely pathogenic	5
Uncertain significance	135
Likely benign	25
Benign	40

Top pathogenic / likely-pathogenic (10)

Variant ID	HGVS	Classification
1333182	NM_000888.5(ITGB6):c.625G>T (p.Gly209Ter)	Pathogenic
180683	NM_000888.5(ITGB6):c.427G>A (p.Ala143Thr)	Pathogenic
180684	NM_000888.5(ITGB6):c.825T>A (p.His275Gln)	Pathogenic
180685	NM_000888.5(ITGB6):c.1846C>T (p.Arg616Ter)	Pathogenic
217305	NM_000888.5(ITGB6):c.898G>A (p.Glu300Lys)	Pathogenic
1333183	NM_000888.5(ITGB6):c.1661-3C>G	Likely pathogenic
180686	NM_000888.5(ITGB6):c.586C>A (p.Pro196Thr)	Likely pathogenic
2444003	NM_000888.5(ITGB6):c.718G>A (p.Glu240Lys)	Likely pathogenic
4849344	NM_000888.5(ITGB6):c.62-2A>G	Likely pathogenic
4849433	NM_000888.5(ITGB6):c.594-1G>A	Likely pathogenic

SpliceAI

2346 predictions. Top by Δscore:

Variant	Effect	Δscore
2:160107674:CATA:C	donor_loss	1.0000
2:160107675:ATAC:A	donor_loss	1.0000
2:160107676:TA:T	donor_loss	1.0000
2:160107678:C:CT	donor_loss	1.0000
2:160107842:CAAT:C	acceptor_gain	1.0000
2:160107844:ATC:A	acceptor_loss	1.0000
2:160107846:C:CA	acceptor_loss	1.0000
2:160107846:C:CC	acceptor_gain	1.0000
2:160107847:T:C	acceptor_loss	1.0000
2:160107854:A:AC	acceptor_gain	1.0000
2:160110528:T:A	donor_gain	1.0000
2:160123793:T:A	donor_gain	1.0000
2:160126374:ATTAC:A	donor_loss	1.0000
2:160126375:TTACC:T	donor_loss	1.0000
2:160126376:TACC:T	donor_loss	1.0000
2:160126377:ACCGT:A	donor_loss	1.0000
2:160141980:A:AC	donor_gain	1.0000
2:160141981:C:CC	donor_gain	1.0000
2:160141983:T:TA	donor_gain	1.0000
2:160172532:ATAGC:A	donor_gain	1.0000
2:160172565:ACACC:A	donor_loss	1.0000
2:160172567:A:AC	donor_gain	1.0000
2:160172567:ACCAA:A	donor_loss	1.0000
2:160172568:C:CC	donor_gain	1.0000
2:160173961:C:CA	donor_gain	1.0000
2:160173971:TACCT:T	donor_loss	1.0000
2:160173972:A:C	donor_loss	1.0000
2:160174135:TACTA:T	acceptor_gain	1.0000
2:160174137:CTA:C	acceptor_gain	1.0000
2:160174138:TA:T	acceptor_gain	1.0000

AlphaMissense

5220 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
2:160172612:C:G	C293S	0.999
2:160172613:A:T	C293S	0.999
2:160172680:A:C	S270R	0.999
2:160172680:A:T	S270R	0.999
2:160172682:T:G	S270R	0.999
2:160172696:A:G	L265P	0.999
2:160172716:C:A	W258C	0.999
2:160172716:C:G	W258C	0.999
2:160172718:A:G	W258R	0.999
2:160172718:A:T	W258R	0.999
2:160173977:A:C	C252W	0.999
2:160173979:A:G	C252R	0.999
2:160195438:C:T	G175E	0.999
2:160195549:A:G	L138P	0.999
2:160199191:C:A	W43C	0.999
2:160199191:C:G	W43C	0.999
2:160137844:A:G	F417S	0.998
2:160169285:A:G	L315P	0.998
2:160172613:A:G	C293R	0.998
2:160172650:G:C	S280R	0.998
2:160172650:G:T	S280R	0.998
2:160172652:T:G	S280R	0.998
2:160172667:G:C	H275D	0.998
2:160173978:C:G	C252S	0.998
2:160173978:C:T	C252Y	0.998
2:160173979:A:T	C252S	0.998
2:160174028:A:C	N235K	0.998
2:160174028:A:T	N235K	0.998
2:160174121:A:C	C204W	0.998
2:160174122:C:G	C204S	0.998

dbSNP variants (sampled 300 via entrez): RS1000018704 (2:160173543 C>G), RS1000073888 (2:160130936 T>A,C), RS1000161996 (2:160135571 A>T), RS1000181504 (2:160189741 T>G), RS1000204396 (2:160180634 T>C), RS1000214100 (2:160183698 C>A), RS1000229321 (2:160139135 T>A,C), RS1000273941 (2:160135264 GACAA>G), RS1000286292 (2:160184513 G>A), RS1000298725 (2:160145634 C>A,T), RS1000304106 (2:160118149 C>A), RS1000322206 (2:160167253 G>A), RS1000324217 (2:160181828 T>C), RS1000330199 (2:160163496 G>A,C,T), RS1000409115 (2:160151496 A>G)

Disease associations

OMIM: gene MIM:147558 | disease phenotypes: MIM:616221

GenCC curated gene-disease

Disease	Classification	Inheritance
amelogenesis imperfecta type 1H	Strong	Autosomal recessive
amelogenesis imperfecta type 1	Supportive	Autosomal dominant
amelogenesis imperfecta, type 3A	Supportive	Autosomal dominant

Mondo (5): amelogenesis imperfecta type 1H (MONDO:0014540), prostate cancer (MONDO:0008315), microcephaly (MONDO:0001149), amelogenesis imperfecta type 1 (MONDO:0015047), amelogenesis imperfecta, type 3A (MONDO:0007538)

Orphanet (2): Amelogenesis imperfecta (Orphanet:88661), Familial prostate cancer (Orphanet:1331)

HPO phenotypes

32 total (30 of 32 shown, HPO-id order):

HPO	Term
HP:0000007	Autosomal recessive inheritance
HP:0000252	Microcephaly
HP:0000365	Hearing impairment
HP:0000400	Macrotia
HP:0000613	Photophobia
HP:0000705	Amelogenesis imperfecta
HP:0000815	Hypergonadotropic hypogonadism
HP:0000962	Hyperkeratosis
HP:0001156	Brachydactyly
HP:0001171	Split hand
HP:0001249	Intellectual disability
HP:0001250	Seizure
HP:0001252	Hypotonia
HP:0001371	Flexion contracture
HP:0001510	Growth delay
HP:0001596	Alopecia
HP:0002209	Sparse scalp hair
HP:0002231	Sparse body hair
HP:0002353	EEG abnormality
HP:0002650	Scoliosis
HP:0002750	Delayed skeletal maturation
HP:0004322	Short stature
HP:0005105	Abnormal nasal morphology
HP:0006286	Yellow-brown discoloration of the teeth
HP:0006297	Enamel hypoplasia
HP:0008064	Ichthyosis
HP:0008070	Sparse hair
HP:0009102	Anterior open-bite malocclusion
HP:0009722	Dental enamel pits
HP:0011842	Abnormal skeletal morphology

GWAS associations

12 associations (top):

Study	Trait	p-value
GCST000665_1	Type 2 diabetes	4.000000e-08
GCST000984_1	Idiopathic membranous nephropathy	9.000000e-29
GCST004063_146	Waist circumference adjusted for body mass index	2.000000e-07
GCST004063_167	Waist circumference adjusted for body mass index	7.000000e-09
GCST007277_3	Tourette syndrome	2.000000e-07
GCST007995_50	Asthma (childhood onset)	9.000000e-09
GCST010916_9	Proportion of activated microglia (inferior temporal cortex)	2.000000e-06
GCST90000025_820	Appendicular lean mass	3.000000e-10
GCST90002381_50	Eosinophil count	4.000000e-09
GCST90002383_190	Hematocrit	7.000000e-10
GCST90002384_236	Hemoglobin	4.000000e-10
GCST90014033_16	Haemorrhoidal disease	2.000000e-11

EFO canonical traits (5, from GWAS)

EFO ID	Trait name
EFO:0007789	BMI-adjusted waist circumference
EFO:0004980	appendicular lean mass
EFO:0004842	eosinophil count
EFO:0004348	hematocrit
EFO:0004509	hemoglobin measurement

MeSH disease descriptors (3)

Descriptor	Name	Tree numbers
D008831	Microcephaly	C05.660.207.620; C10.500.507.400.500; C16.131.621.207.620; C16.131.666.507.400.500
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
C562880	Amelogenesis Imperfecta, Type III (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (4): CHEMBL2111416 (PROTEIN COMPLEX), CHEMBL4876 (SINGLE PROTEIN), CHEMBL6066570 (PROTEIN COMPLEX), CHEMBL6066571 (PROTEIN COMPLEX)

Molecules with ChEMBL bioactivity

5 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 10,308 (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
CHEMBL5315046	NESVATEGRAST	2	72
CHEMBL3319236	GLPG-0187	1	96
CHEMBL4241824	GSK-3008348 FREE BASE	1	8
CHEMBL4246089	GSK-3008348	1	9

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

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	9.97	pKi

Binding affinities (BindingDB)

20 measured of 24 human assays (24 total across all organisms); most potent 20 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
(2R)-2-[[(6R)-4,5,6,7-tetrahydro-1H-indazole-6-carbonyl]amino]-4-[3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]cyclobutyl]oxybutanoic acid	IC50	150 nM	US-11180494: Substituted amino acids as integrin inhibitors
3-[3-[4-(1H-benzimidazol-2-ylamino)butyl]-2-oxoimidazolidin-1-yl]-3-[3-(trifluoromethyl)phenyl]propanoic acid	IC50	376 nM	US-10118929: Nonanoic and decanoic acid derivatives and uses thereof
3-[2-oxo-3-[4-(pyridin-2-ylamino)butyl]imidazolidin-1-yl]-3-[3-(trifluoromethyl)phenyl]propanoic acid	IC50	394 nM	US-10118929: Nonanoic and decanoic acid derivatives and uses thereof

ChEMBL bioactivities

810 potent at pChembl≥5 of 826 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	Ki	0.01	nM	GSK-3008348 FREE BASE
10.80	Kd	0.01585	nM	GSK-3008348 FREE BASE
10.70	Ki	0.01995	nM	CHEMBL4244784
10.70	Kd	0.02	nM	GSK-3008348 FREE BASE
10.60	Ki	0.02512	nM	CHEMBL4238909
10.50	Ki	0.03162	nM	CHEMBL4242263
10.40	IC50	0.04	nM	CHEMBL267434
10.40	Ki	0.03981	nM	GSK-3008348 FREE BASE
10.40	Ki	0.03981	nM	CHEMBL4241584
10.40	Ki	0.03981	nM	CHEMBL4249629
10.40	Ki	0.03981	nM	CHEMBL4249172
10.40	Ki	0.03981	nM	GSK-3008348
10.30	Ki	0.05012	nM	CHEMBL4237919
10.20	Ki	0.0631	nM	CHEMBL4238909
10.20	Ki	0.0631	nM	CHEMBL4243367
10.20	Ki	0.0631	nM	CHEMBL4237868
10.20	Ki	0.0631	nM	CHEMBL4239085
10.10	Ki	0.07943	nM	CHEMBL4242635
10.10	Ki	0.07943	nM	CHEMBL4247149
10.10	Ki	0.07943	nM	CHEMBL4248589
10.00	Ki	0.1	nM	CHEMBL4251444
9.97	Ki	0.1072	nM	CHEMBL4468357
9.89	IC50	0.13	nM	CHEMBL5790863
9.82	IC50	0.15	nM	CHEMBL9278
9.80	EC50	0.1585	nM	GSK-3008348 FREE BASE
9.76	Ki	0.1738	nM	CHEMBL4573716
9.70	IC50	0.2	nM	CHEMBL5914164
9.59	IC50	0.26	nM	CHEMBL4441624
9.59	IC50	0.26	nM	CHEMBL4780301
9.55	IC50	0.28	nM	CHEMBL4441624
9.52	IC50	0.3	nM	CHEMBL5766697
9.52	IC50	0.3	nM	CHEMBL5920684
9.52	IC50	0.3	nM	CHEMBL5786200
9.52	IC50	0.3	nM	CHEMBL5748399
9.40	IC50	0.4	nM	CHEMBL9200
9.40	IC50	0.4	nM	CHEMBL5781301
9.40	IC50	0.4	nM	CHEMBL5964326
9.40	IC50	0.4	nM	CHEMBL5974146
9.40	IC50	0.4	nM	CHEMBL5802710
9.40	IC50	0.4	nM	CHEMBL5889173
9.40	IC50	0.4	nM	CHEMBL5951981
9.30	IC50	0.5	nM	CHEMBL5975238
9.30	IC50	0.5	nM	CHEMBL5790208
9.30	IC50	0.5	nM	CHEMBL5770209
9.30	IC50	0.5	nM	CHEMBL6150463
9.24	IC50	0.57	nM	CHEMBL5903364
9.22	IC50	0.6	nM	CHEMBL9555
9.22	IC50	0.6	nM	CHEMBL5819051
9.22	IC50	0.6	nM	CHEMBL5802648
9.17	IC50	0.67	nM	CHEMBL4575627

PubChem BioAssay actives

362 with measured affinity, of 524 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
3-[[2-[4-[(4-methyl-2-pyridinyl)amino]butanoylamino]acetyl]amino]-3-(4-naphthalen-1-ylphenyl)propanoic acid	1171325: Inhibition of integrin alphavbeta6 (unknown origin) by Merck binding assay	ic50	<0.0001	uM
(3S)-3-(3-morpholin-4-ylphenyl)-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400456: Binding affinity to human integrin alphaVbeta6 assessed as dissociation constant up to 48 hrs by liquid scintillation counting	ki	<0.0001	uM
(3S)-3-[3-(3,5-dimethylpyrazol-1-yl)-5-morpholin-4-ylphenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400434: Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assay	ki	<0.0001	uM
(3S)-3-[3-(2,5-dimethyl-1H-imidazol-4-yl)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400434: Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assay	ki	<0.0001	uM
(3S)-3-[3-[(3S)-oxolan-3-yl]oxyphenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400434: Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assay	ki	<0.0001	uM
(3S)-3-[3-(oxolan-3-yl)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400434: Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assay	ki	<0.0001	uM
(3S)-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]-3-[3-(triazol-1-yl)phenyl]butanoic acid	1400434: Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assay	ki	<0.0001	uM
(3S)-3-[3-(3,5-dimethylpyrazol-1-yl)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400434: Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assay	ki	<0.0001	uM
(3S)-3-[3-(3,5-dimethylpyrazol-1-yl)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid;hydrochloride	1577126: Inhibition of integrin alphavbeta6 (unknown origin) by radioligand binding assay	ki	<0.0001	uM
3-[[2-[4-[(4-methyl-2-pyridinyl)amino]butanoylamino]acetyl]amino]-3-[3-(trifluoromethoxy)phenyl]propanoic acid	220626: Inhibition of fibronectin binding to recombinant human alphaV-beta6 integrin	ic50	0.0001	uM
(3S)-3-(3-cyclopropyl-5-morpholin-4-ylphenyl)-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400434: Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assay	ki	0.0001	uM
(3S)-3-[3-[(3R)-oxolan-3-yl]oxyphenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400434: Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assay	ki	0.0001	uM
(3S)-3-[3-(3-methyl-1,2,4-triazol-4-yl)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400434: Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assay	ki	0.0001	uM
(3S)-3-[3-(3,5-dimethyl-1,2,4-triazol-1-yl)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400434: Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assay	ki	0.0001	uM
(3S)-3-[3-(3,5-dimethylpyrazol-1-yl)phenyl]-4-[(1S,3R)-1-methyl-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-ium-1-yl]butanoate	1577126: Inhibition of integrin alphavbeta6 (unknown origin) by radioligand binding assay	ki	0.0001	uM
(3S)-3-[3-(3-methylpyrazol-1-yl)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400434: Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assay	ki	0.0001	uM
(3S)-3-(3-pyrazol-1-ylphenyl)-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400434: Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assay	ki	0.0001	uM
(3S)-3-[3-(5-methylpyrazol-1-yl)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400434: Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assay	ki	0.0001	uM
(3S)-3-(3-cyclopropylphenyl)-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400434: Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assay	ki	0.0001	uM
(3S)-3-[3-(3,5-dimethylpyrazol-1-yl)phenyl]-4-[(1R,3R)-1-methyl-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-ium-1-yl]butanoate	1577126: Inhibition of integrin alphavbeta6 (unknown origin) by radioligand binding assay	ki	0.0002	uM
2-[(2,6-dichlorobenzoyl)amino]-3-[5-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)pentanoylamino]propanoic acid	2065303: Inhibition of recombinant human Integrin alphaVbeta6 using TMB as substrate incubated for 2 hrs in presence of LAP by ELISA	ic50	0.0002	uM
2-[(3S,6S,9S,12S,18S,21S,24S,27R)-24-(4-aminobutyl)-3,21-dibenzyl-18-[3-(diaminomethylideneamino)propyl]-6,25-dimethyl-9-(2-methylpropyl)-2,5,8,11,14,17,20,23,26-nonaoxo-1,4,7,10,13,16,19,22,25-nonazabicyclo[25.3.0]triacontan-12-yl]acetic acid	1614468: Inhibition of LAP binding to human integrin alphavbeta6 receptor after 1 hr by solid-phase binding assay	ic50	0.0003	uM
2-[(3S,6S,9S,12S,18S,21S,24S,27S)-24-(4-aminobutyl)-3,21-dibenzyl-18-[3-(diaminomethylideneamino)propyl]-6,25-dimethyl-9-(2-methylpropyl)-2,5,8,11,14,17,20,23,26-nonaoxo-1,4,7,10,13,16,19,22,25-nonazabicyclo[25.3.0]triacontan-12-yl]acetic acid	1744037: Binding affinity to human integrin alphaVbeta6 incubated for 1 hr by ELISA based solid phase integrin binding assay	ic50	0.0003	uM
3-(3,5-dichlorophenyl)-3-[[2-[5-[(4-methyl-2-pyridinyl)amino]pentanoylamino]acetyl]amino]propanoic acid	220626: Inhibition of fibronectin binding to recombinant human alphaV-beta6 integrin	ic50	0.0004	uM
3-(4-phenylphenyl)-3-[[2-[5-(pyridin-2-ylamino)pentanoylamino]acetyl]amino]propanoic acid	1177803: Antagonist activity at alphavbeta6 integrin receptor (unknown origin) by cell-free ELISA	ic50	0.0006	uM
2-[(3R,9S,12S,15S,18S,24S,27S,30S)-9-benzyl-24-[3-(diaminomethylideneamino)propyl]-12,27-dimethyl-15-(2-methylpropyl)-2,8,11,14,17,20,23,26,29-nonaoxo-1,7,10,13,16,19,22,25,28-nonazatricyclo[28.3.0.03,7]tritriacontan-18-yl]acetic acid	1614468: Inhibition of LAP binding to human integrin alphavbeta6 receptor after 1 hr by solid-phase binding assay	ic50	0.0007	uM
(3S)-3-[3-(oxetan-3-yloxy)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400429: Antagonist activity at human integrin alphaVbeta6 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0010	uM
(3S)-3-(3-bromo-5-chloro-2-hydroxyphenyl)-3-[[2-[[5-[(5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino]pyridine-3-carbonyl]amino]acetyl]amino]propanoic acid	1177807: Antagonist activity at alphavbeta6 integrin receptor in human HT29 cells after 4 hrs using p-nitrophenyl phosphate by colorimetry	ic50	0.0011	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	1177803: Antagonist activity at alphavbeta6 integrin receptor (unknown origin) by cell-free ELISA	ic50	0.0014	uM
(3S)-3-(3-bromo-5-tert-butylphenyl)-3-[[2-[[3-hydroxy-5-[(5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino]benzoyl]amino]acetyl]amino]propanoic acid	1177815: Antagonist activity at alphavbeta6 integrin receptor (unknown origin) by cell-based ELISA	ic50	0.0015	uM
(3S)-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]-3-[3-(1,2,4-triazol-4-yl)phenyl]butanoic acid	1400429: Antagonist activity at human integrin alphaVbeta6 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0016	uM
(3S)-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]-3-[3-(1,2,4-triazol-1-yl)phenyl]butanoic acid	1400429: Antagonist activity at human integrin alphaVbeta6 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0016	uM
3-(3,5-dichlorophenyl)-3-[[5-[(4-methyl-2-pyridinyl)amino]pentanoylamino]carbamoylamino]propanoic acid	220626: Inhibition of fibronectin binding to recombinant human alphaV-beta6 integrin	ic50	0.0017	uM
(3S)-3-[3-(1,4-dimethylimidazol-2-yl)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400429: Antagonist activity at human integrin alphaVbeta6 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0020	uM
(3S)-3-[3-(5-methylpyrazol-1-yl)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid;hydrochloride	1577144: Inhibition of integrin alphavbeta6 (unknown origin) expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP1 (242 to 252 amino acids) incubated for 30 mins by fluorescent probe BCECF-AM based fluorescence assay	ic50	0.0020	uM
3-[[2-[[3-(diaminomethylideneamino)benzoyl]amino]acetyl]amino]-3-(3,5-dichlorophenyl)propanoic acid	1400456: Binding affinity to human integrin alphaVbeta6 assessed as dissociation constant up to 48 hrs by liquid scintillation counting	ki	0.0020	uM
(3S)-3-[3-(5-methyl-1H-pyrazol-3-yl)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400429: Antagonist activity at human integrin alphaVbeta6 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0025	uM
(3S)-3-[3-(oxan-4-yloxy)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400429: Antagonist activity at human integrin alphaVbeta6 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0025	uM
3-(3-nitrophenyl)-3-[[2-[4-(pyridin-2-ylamino)butanoylamino]acetyl]amino]propanoic acid	1177803: Antagonist activity at alphavbeta6 integrin receptor (unknown origin) by cell-free ELISA	ic50	0.0040	uM
(3S)-3-(3-bromophenyl)-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400429: Antagonist activity at human integrin alphaVbeta6 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0040	uM
3-[[2-[4-[(4-methyl-2-pyridinyl)amino]butanoylamino]acetyl]amino]-3-(4-naphthalen-1-ylphenyl)propanoic acid;2,2,2-trifluoroacetic acid	730660: Inhibition of latency-associated peptide binding to Integrin alphaVbeta6 receptor (unknown origin) by competitive ELISA	ic50	0.0040	uM
3-(3-imidazol-1-ylphenyl)-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400429: Antagonist activity at human integrin alphaVbeta6 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0063	uM
(3S)-3-(3-chlorophenyl)-3-[[6-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]pyridazin-3-yl]amino]propanoic acid	1558143: Inhibition of recombinant human integrin alphaV (31 to 992 residues) beta6 (22 to 707 residues) expressed in CHO cells preincubated for 15 mins followed by Cy3B-RGD probe addition and measured after 2 hrs by fluorescence polarization assay	ic50	0.0063	uM
(3S)-3-[3-(1,4-dimethylpyrazol-5-yl)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400429: Antagonist activity at human integrin alphaVbeta6 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0079	uM
(3S)-3-[3-(5-methylpyrazol-1-yl)phenyl]-4-[(3R)-1-methyl-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-ium-1-yl]butanoate	1577144: Inhibition of integrin alphavbeta6 (unknown origin) expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP1 (242 to 252 amino acids) incubated for 30 mins by fluorescent probe BCECF-AM based fluorescence assay	ic50	0.0079	uM
2-[(3R,9S,12S,15S,18S,21S,27S,30S,33S)-27-[3-(diaminomethylideneamino)propyl]-12,15,30-trimethyl-9,18-bis(2-methylpropyl)-2,8,11,14,17,20,23,26,29,32-decaoxo-1,7,10,13,16,19,22,25,28,31-decazatricyclo[31.3.0.03,7]hexatriacontan-21-yl]acetic acid	1614468: Inhibition of LAP binding to human integrin alphavbeta6 receptor after 1 hr by solid-phase binding assay	ic50	0.0083	uM
(3S)-4-[(3S)-3-fluoro-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]-3-(3-morpholin-4-ylphenyl)butanoic acid	1577138: Antagonist activity at integrin alphavbeta6 (unknown origin) expressed in human K562 cells assessed as reduction in cell adhesion to LAP-bi by fluorescent probe BCECF-AM based fluorescence assay	ic50	0.0100	uM
(3R)-3-(3-bromo-5-iodophenyl)-3-[[2-[[3-[(5-fluoro-1,4,5,6-tetrahydropyrimidin-2-yl)amino]-5-hydroxybenzoyl]amino]acetyl]amino]propanoic acid	295508: Inhibition of alpha-V-beta-6 integrin receptor in human HT29 cells	ic50	0.0110	uM
(3S)-3-(3-bromo-5-chloro-2-hydroxyphenyl)-3-[[2-[[3-hydroxy-5-[(5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino]benzoyl]amino]acetyl]amino]propanoic acid	1177807: Antagonist activity at alphavbeta6 integrin receptor in human HT29 cells after 4 hrs using p-nitrophenyl phosphate by colorimetry	ic50	0.0117	uM
(3S)-3-[3-(oxan-4-yl)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400429: Antagonist activity at human integrin alphaVbeta6 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0126	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	decreases expression, affects cotreatment, increases abundance, increases expression	7
Estradiol	decreases expression, decreases reaction, affects cotreatment, increases expression	6
Tetrachlorodibenzodioxin	decreases reaction, increases expression, affects expression, decreases expression	3
Zinc	affects expression, decreases expression, increases expression, affects cotreatment	3
mercuric bromide	affects cotreatment, increases expression	2
Air Pollutants	decreases expression, increases abundance	2
Benzo(a)pyrene	affects methylation, decreases expression, decreases methylation	2
Cycloheximide	decreases reaction, increases expression	2
Progesterone	affects cotreatment, decreases expression	2
Tobacco Smoke Pollution	affects expression, increases expression	2
Valproic Acid	increases expression, increases methylation	2
Cadmium Chloride	decreases expression, increases abundance	2
Genistein	affects expression, decreases expression	2
Particulate Matter	decreases expression, increases abundance	2
aristolochic acid I	decreases expression	1
pirinixic acid	affects binding, increases activity, increases expression	1
bisphenol A	increases methylation	1
sodium arsenate	decreases expression	1
titanium dioxide	increases expression	1
pyrogallol 1,3-dimethyl ether	affects cotreatment, affects localization, increases expression	1
trichostatin A	increases expression	1
zinc chloride	increases expression	1
perfluorooctanoic acid	decreases expression	1
manganese chloride	decreases methylation	1
4-hydroxy-2-nonenal	decreases expression	1
glycidamide	decreases expression	1
4-(4-fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)imidazole	decreases reaction, increases expression	1
CGP 52608	affects binding, increases reaction	1
SB 203580	decreases reaction, increases expression	1
2-palmitoylglycerol	increases expression	1

ChEMBL screening assays

79 unique, capped per target: 75 binding, 2 admet, 2 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1120565	Binding	Inhibition of integrin alpha-V-beta-6-mediated adhesion of human HT-29 cells	Emerging targets in osteoporosis disease modification. — J Med Chem
CHEMBL4139036	ADMET	Binding affinity to alphav/beta6 integrin in human A375Pbeta6 cells assessed as drug internalization at 100 nM after 15 mins by flow cytometric analysis relative to biotinylated A20FMDV2	Structure-activity relationship study of the tumour-targeting peptide A20FMDV2 via modification of Lys16, Leu13, and N- and/or C-terminal functionality. — Eur J Med Chem
CHEMBL816279	Functional	Inhibition of integrin alpha-v/beta-6 mediated UCLAP-3 cell adhesion to fibronectin; 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

7 cell lines: 5 cancer cell line, 1 spontaneously immortalized cell line, 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_1D33	DX3-puro/beta6	Cancer cell line	Female
CVCL_5F66	A375P-beta6/puro	Cancer cell line	Female
CVCL_D6AY	HyCyte BxPC-3 KO-hITGB6	Cancer cell line	Female
CVCL_D7SR	Ubigene A-549 ITGB6 KO	Cancer cell line	Male
CVCL_E4IS	Genomeditech CHO-K1 H_ITGB6	Spontaneously immortalized cell line	Female
CVCL_E4J4	Genomeditech HEK-293 H_alphaVbeta6	Transformed cell line	Female
CVCL_JY68	H357-VB6	Cancer cell line	Male

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