ITGB8

Summary

ITGB8 (integrin subunit beta 8, HGNC:6163) is a protein-coding gene on chromosome 7p21.1, encoding Integrin beta-8 (P26012). Integrin alpha-V:beta-8 (ITGAV:ITGB8) is a receptor for fibronectin.

This gene is a member of the integrin beta chain family and encodes a single-pass type I membrane protein with a VWFA domain and four cysteine-rich repeats. This protein noncovalently binds to an alpha subunit to form a heterodimeric integrin complex. In general, integrin complexes mediate cell-cell and cell-extracellular matrix interactions and this complex plays a role in human airway epithelial proliferation. Alternatively spliced variants which encode different protein isoforms have been described; however, not all variants have been fully characterized.

Source: NCBI Gene 3696 — RefSeq curated summary.

At a glance

• GWAS associations: 70
• Clinical variants (ClinVar): 132 total — 2 pathogenic
• Druggable target: yes — 4 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_002214

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:6163
Approved symbol	ITGB8
Name	integrin subunit beta 8
Location	7p21.1
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000105855
Ensembl biotype	protein_coding
OMIM	604160
Entrez	3696

Gene structure

Transcript identifiers

Ensembl transcripts: 11 — 8 protein_coding, 2 retained_intron, 1 protein_coding_CDS_not_defined

ENST00000222573, ENST00000460204, ENST00000477859, ENST00000478974, ENST00000537992, ENST00000897604, ENST00000897605, ENST00000897606, ENST00000897607, ENST00000897608, ENST00000897609

RefSeq mRNA: 1 — MANE Select: NM_002214 NM_002214

CCDS: CCDS5370

Canonical transcript exons

ENST00000222573 — 14 exons

Exon	Start	End
ENSE00000672661	20398860	20398994
ENSE00000672663	20401721	20402126
ENSE00000672665	20404628	20404853
ENSE00000672667	20406062	20406171
ENSE00000672669	20409615	20409778
ENSE00000831899	20409875	20415754
ENSE00001875411	20330900	20331933
ENSE00003470902	20367012	20367186
ENSE00003513743	20394896	20394985
ENSE00003590940	20363637	20363722
ENSE00003598836	20391403	20391498
ENSE00003617797	20379051	20379297
ENSE00003671588	20381727	20381885
ENSE00003687962	20380666	20380831

Expression profiles

Bgee: expression breadth ubiquitous, 262 present calls, max score 99.74.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 19.1679 / max 723.5212, expressed in 1442 samples.

FANTOM5 promoters (23 alternative TSS)

Promoter ID	TPM avg	Samples expressed
77466	5.8554	1188
77469	3.3847	842
77468	1.8115	743
77472	1.1133	481
77480	1.0253	457
77481	1.0220	358
77483	0.9704	226
77477	0.3827	150
77478	0.3822	170
77476	0.3678	165

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
pigmented layer of retina	UBERON:0001782	99.74	gold quality
retina	UBERON:0000966	99.71	gold quality
lateral globus pallidus	UBERON:0002476	98.68	gold quality
ventricular zone	UBERON:0003053	98.49	gold quality
synovial joint	UBERON:0002217	98.23	gold quality
dorsal root ganglion	UBERON:0000044	97.70	gold quality
bronchial epithelial cell	CL:0002328	97.67	gold quality
corpus epididymis	UBERON:0004359	97.62	gold quality
mucosa of paranasal sinus	UBERON:0005030	97.59	gold quality
trigeminal ganglion	UBERON:0001675	97.56	gold quality
caput epididymis	UBERON:0004358	97.48	gold quality
seminal vesicle	UBERON:0000998	97.08	gold quality
substantia nigra pars reticulata	UBERON:0001966	96.94	gold quality
oral cavity	UBERON:0000167	96.90	gold quality
subthalamic nucleus	UBERON:0001906	96.84	gold quality
inferior vagus X ganglion	UBERON:0005363	96.67	gold quality
sural nerve	UBERON:0015488	96.59	gold quality
upper leg skin	UBERON:0004262	96.54	gold quality
substantia nigra pars compacta	UBERON:0001965	96.37	gold quality
globus pallidus	UBERON:0001875	96.12	gold quality
superior vestibular nucleus	UBERON:0007227	95.61	gold quality
tibial nerve	UBERON:0001323	95.57	gold quality
medial globus pallidus	UBERON:0002477	95.51	gold quality
cauda epididymis	UBERON:0004360	95.49	gold quality
epithelium of nasopharynx	UBERON:0001951	95.13	gold quality
skin of hip	UBERON:0001554	94.82	gold quality
germinal epithelium of ovary	UBERON:0001304	94.75	gold quality
corpus callosum	UBERON:0002336	94.75	gold quality
renal medulla	UBERON:0000362	94.74	gold quality
endometrium	UBERON:0001295	94.35	gold quality

Single-cell (SCXA)

Detected in 12 experiment(s), a significant marker in 11.

Experiment	Marker?	Max mean expression
E-GEOD-131882	yes	2328.33
E-CURD-119	yes	1815.36
E-GEOD-84465	yes	1753.66
E-GEOD-75688	yes	1501.34
E-GEOD-98556	yes	1193.80
E-MTAB-8559	yes	902.62
E-GEOD-135922	yes	16.89
E-GEOD-93593	yes	12.84
E-MTAB-7249	yes	11.38
E-MTAB-6678	yes	4.19
E-MTAB-7303	no	177.08
E-ANND-3	no	0.00

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

9 targets.

Target	Regulation
ITGA11	Repression
ITGA3	Repression
ITGA4	Repression
ITGA5	Activation
ITGA6	Repression
ITGA7	Repression
ITGAV	Repression
ITGB1	Repression
ITGB5	Repression

Upstream regulators (CollecTRI, top): ATF2, JUN

miRNA regulators (miRDB)

342 targeting ITGB8, 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-3163	100.00	77.23	8605
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-656-3P	100.00	72.15	2788
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-340-5P	100.00	72.50	4437
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-4776-3P	100.00	68.73	1340
HSA-MIR-126-5P	100.00	72.71	3180
HSA-MIR-6833-3P	100.00	70.63	3197
HSA-MIR-4768-5P	100.00	69.49	2861
HSA-MIR-6873-3P	100.00	71.42	2626
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-548AW	99.99	72.57	3559
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-181A-5P	99.99	72.96	2995
HSA-MIR-181B-5P	99.99	72.97	2996
HSA-MIR-181C-5P	99.99	72.95	2996
HSA-MIR-181D-5P	99.99	73.04	2997
HSA-MIR-4500	99.99	72.72	2367
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-19A-3P	99.98	75.33	2762
HSA-MIR-19B-3P	99.98	75.44	2754
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-5696	99.98	72.36	4487
HSA-MIR-520D-5P	99.98	73.34	4883

Literature-anchored findings (GeneRIF, showing 40)

• induced alpha(v)beta(8) integrin expression mediated Fas-stimulated migration (PMID:12324452)
• These data provide evidence for a functional role for integrin alphavbeta8-mediated activation of transforming growth factor-beta in control of human airway epithelial proliferation in vivo. (PMID:12875973)
• periostin has an active role in the epithelial-mesenchymal transformation and metastasis that requires cross-talk between integrin and EGFR signaling pathways (PMID:16702213)
• Fusion of epithelial cells by Epstein-Barr virus proteins is triggered by binding of viral glycoproteins gHgL to integrins alphavbeta6 or alphavbeta8. (PMID:19920174)
• Reduced expression of integrin beta8 may be involved in the pathogenesis of sporadic brain arteriovenous malformations. (PMID:20019187)
• Transcription of the transforming growth factor beta activating integrin beta8 subunit is regulated by SP3, AP-1, and the p38 pathway (PMID:20519498)
• The mRNA levels of IntegrinalphaV and Integrinbeta8 were significantly higher in LSCC tissues than that in corresponding adjacent normal tissues. (PMID:20942236)
• miR-93 promotes the growth of, and angiogenesis in astrocytomas, by suppressing, at least in part, integrin-beta8 expression. (PMID:20956944)
• The authors demonstrated that both integrins alphavbeta6 and alphavbeta8 can serve as specific receptors for Epstein-Barr virus gHgL proteins. (PMID:21178476)
• Data suggest that lung fibroblast chemokine secretion directs dendritic cell trafficking, in a manner that is critically dependent on alphavbeta8-mediated activation of TGF-beta by fibroblasts. (PMID:21646718)
• Highly angiogenic and poorly invasive glioblastomas expressed low levels of beta8 integrin, whereas highly invasive glioblastomas with limited neovascularization expressed high levels of beta8 integrin. (PMID:21859829)
• Interleukin-1beta induces increased transcriptional activation of the transforming growth factor-beta-activating integrin subunit beta8 through altering chromatin architecture. (PMID:21878622)
• Deletion of the Itgb8 gene from retinal ganglia cells and Mu ller glia, but not astrocytes, results in highly abnormal vascular patterning and instability. (PMID:22279205)
• ITGB8 silencing may change lung cancer cells to a less invasive phenotype through alteration in the expression of metastasis-related genes. (PMID:22753015)
• alphavbeta8 integrin, via interactions with RhoGDI1, regulates activation of Rho proteins to promote glioblastoma multiforme cell invasiveness. (PMID:23283986)
• Desmoglein-2 co-localizes with integrin-beta8 in N-MVECs. (PMID:23874518)
• Brain metastases ITGB8 expression exhibits considerable heterogeneity according to tumor origin. (PMID:24294359)
• alphavbeta6- and alphavbeta8-integrins acted independently and are thus interchangeable as receptors for Herpes simplex type 1 virus entry. (PMID:24367260)
• data show that integrin beta 8, but not integrin beta 5 or integrin beta 6, protein expression is increased in liver specimens of patients with biliary atresia (PMID:25079481)
• overexpression of integrin alphav induces integrin alphavb8 heterodimer formation and the binding of integrin alphavbeta8 to type collagen might enhance the proliferation and invasion of SCC cells via the activation of the MEK/ERK signaling pathway. (PMID:25190218)
• Integrin Beta8 plays a role in the motility of prostate cancer cells. (PMID:25886373)
• Herpes simplex virus entry is enabled by gH/gL interaction with alphavbeta6- or alphavbeta8-integrin receptors. (PMID:26157134)
• Integrins alphavbeta6 and alphavbeta8 were expressed in non-overlapping patterns by keratinocytes and maintained the epidermal residence of Langerhans cells and tissue resident memory T cells by activating latent TGF-beta. (PMID:26901152)
• Integrin beta8 was differentially expressed between Fibromyalgia patients and healthy controls. (PMID:27157394)
• Among Greek and Polish patients with intracerebral hemorrhage, heterozygous individuals with the rs10251386 and the rs10239099 of the ITGB8 gene had significantly lower age of ICH onset compared to the wild-type genotypes. (PMID:27476161)
• this study uncovers a novel pathway by which the TGFbeta-activating integrin alphavbeta8 is expressed in the human intestine on dendritic cell subsets, which is upregulated in patients with inflammatory bowel disease (PMID:27782111)
• Although Mn(2+) potently activates other integrins and increases affinity of alphaVbeta6 for pro-TGF-beta1 25- to 55-fold, it increases alphaVbeta8 affinity only 2- to 3-fold. (PMID:28484027)
• In cellular model, the microRNA-513a-3p was identified as a novel element targeting ITG-beta8, thereby controlling the protein level and its molecular function in the controlling of migration and pro-inflammatory environment. (PMID:29204818)
• The results demonstrated that the hsa_circ_0046701/miR-142-3p/ITGB8 axis might play critical regulatory roles in the pathogenesis and development of glioma. (PMID:29337055)
• our results indicate that miR-199a-3p enhances cisplatinsensitivity of ovarian cancer cells through downregulating ITGB8 expression, and miR-199a-3p may serve as a therapeutic target for the treatment of ovarian cancer patients with cisplatin-resistance. (PMID:29436681)
• ITGB8 is identified as a novel target of miR-26a-5p. (PMID:29746867)
• findings with the alphavbeta3 integrin suggests that our model of stabilizing the extended-closed conformation is generalizable to other integrins. (PMID:30061598)
• Data uncovered that ITGB8 was a target gene of miR-106b. ITGB8 mRNA and protein levels decreased in colon cancer cells overexpressing miR-106b. (PMID:30520100)
• ITGB8 was significantly upregulated in ovarian cancer tissues compared to that in normal ovary tissues. High-grade Serous Ovarian Carcinoma patients with high ITGB8 expression had significantly shorter overall survival and recurrence-free survival compared to their low-expression counterparts. Increased ITGB8 expression might be an independent prognostic indicator of unfavorable overall survival (PMID:30531684)
• ITGB8 gene SNPs may be implicated in the risk of hemorrhagic event after a traumatic brain injury. (PMID:31033358)
• Lack of a binding site for one of three betaI domain divalent cations and a unique beta6-alpha7 loop conformation in beta8 facilitate movements of the alpha1 and alpha1’ helices at the ligand binding pocket toward the high affinity state. (PMID:31792290)
• Circular RNA TTBK2 regulates cell proliferation, invasion and ferroptosis via miR-761/ITGB8 axis in glioma. (PMID:32196629)
• The long non-coding RNA PVT1/miR-145-5p/ITGB8 axis regulates cell proliferation, apoptosis, migration and invasion in non-small cell lung cancer cells. (PMID:32202906)
• lncRNA ITGB8-AS1 functions as a ceRNA to promote colorectal cancer growth and migration through integrin-mediated focal adhesion signaling. (PMID:34371180)
• Integrin subunit beta 8 contributes to lenvatinib resistance in HCC. (PMID:35238496)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	itgb8	ENSDARG00000028222
mus_musculus	Itgb8	ENSMUSG00000025321
rattus_norvegicus	Itgb8	ENSRNOG00000006569

Paralogs (8): ITGB5 (ENSG00000082781), ITGB6 (ENSG00000115221), ITGB4 (ENSG00000132470), ITGB7 (ENSG00000139626), ITGB1 (ENSG00000150093), ITGB2 (ENSG00000160255), ITGBL1 (ENSG00000198542), ITGB3 (ENSG00000259207)

Protein

Protein identifiers

Integrin beta-8 — P26012 (reviewed: P26012)

All UniProt accessions (1): P26012

UniProt curated annotations — full annotation on UniProt →

Function. Integrin alpha-V:beta-8 (ITGAV:ITGB8) is a receptor for fibronectin. It recognizes the sequence R-G-D in its ligands. 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 on the surface of activated regulatory T-cells (Tregs). Required during vasculogenesis.

Subunit / interactions. Heterodimer of an alpha and a beta subunit. Beta-8 (ITGB8) associates with alpha-V (ITGAV) to form ITGAV:ITGB8. ITGAV:ITGB8 interacts with TGFB1.

Subcellular location. Cell membrane.

Tissue specificity. Placenta, kidney, brain, ovary, uterus and in several transformed cells. Transiently expressed in 293 human embryonic kidney cells.

Domain organisation. The VWFA domain (or beta I domain) contains two cation-binding sites: the ligand-associated metal ion-binding site (LIMBS or SyMBS) and the metal ion-dependent adhesion site (MIDAS). Unlike in the other beta integrins, the cation-binding site adjacent MIDAS site (ADMIDAS) in ITGB8 is not functional due to the presence of two Asn residues instead of 2 Asp residues. This domain is also part of the ligand-binding site.

Similarity. Belongs to the integrin beta chain family.

Isoforms (2)

UniProt ID	Names	Canonical?
P26012-1	1	yes
P26012-2	2

RefSeq proteins (1): NP_002205* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000742	EGF	Domain
IPR002369	Integrin_bsu_VWA	Domain
IPR015812	Integrin_bsu	Family
IPR016201	PSI	Domain
IPR032695	Integrin_dom_sf	Homologous_superfamily
IPR033760	Integrin_beta_N	Domain
IPR036465	vWFA_dom_sf	Homologous_superfamily
IPR057073	EGF_integrin_2	Domain
IPR057243	Integrin_I-EGF_CS	Conserved_site

Pfam: PF00362, PF17205, PF23105, PF23106

UniProt features (91 total): disulfide bond 25, strand 22, helix 13, binding site 8, glycosylation site 7, domain 6, turn 3, topological domain 2, signal peptide 1, chain 1, transmembrane region 1, splice variant 1, sequence variant 1

Structure

Experimental structures (PDB)

11 structures.

PDB	Method	Resolution (Å)
6OM1	X-RAY DIFFRACTION	2.66
8VS6	ELECTRON MICROSCOPY	2.73
6OM2	X-RAY DIFFRACTION	2.77
9IND	ELECTRON MICROSCOPY	2.88
8TCF	ELECTRON MICROSCOPY	2.9
8VSD	ELECTRON MICROSCOPY	3.2
7Y1T	ELECTRON MICROSCOPY	3.24
6UJA	ELECTRON MICROSCOPY	3.3
6UJB	ELECTRON MICROSCOPY	3.51
6UJC	ELECTRON MICROSCOPY	3.56
6DJP	ELECTRON MICROSCOPY	4.8

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P26012-F1	76.57	0.34

Antibody-complex structures (SAbDab): 4 — 6DJP, 6UJB, 6UJC, 9IND

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 (8): 154 (in midas binding site); 156 (in midas binding site); 193 (in limbs binding site); 249 (in limbs binding site); 251 (in limbs binding site); 253 (in limbs binding site); 254 (in limbs binding site); 254 (in midas binding site)

Disulfide bonds (25): 47–65, 55–469, 58–83, 68–94, 211–218, 266–307, 407–419, 439–467, 471–494, 471–491, 481–494, 499–528, 511–526, 520–531, 533–546, 553–567, 561–572, 574–583, 585–609, 593–607 …

Glycosylation sites (7): 233, 402, 421, 431, 456, 466, 648

Function

Pathways and Gene Ontology

Reactome pathways

8 pathways

ID	Pathway
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-1474244	Extracellular matrix organization
R-HSA-1566948	Elastic fibre formation
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: 476 (showing top): GSE45365_HEALTHY_VS_MCMV_INFECTION_CD8_TCELL_IFNAR_KO_UP, GOBP_MYELOID_CELL_DIFFERENTIATION, RNGTGGGC_UNKNOWN, GOBP_DENDRITIC_CELL_DIFFERENTIATION, REACTOME_SIGNALING_BY_TGF_BETA_RECEPTOR_COMPLEX, GU_PDEF_TARGETS_DN, PAX4_01, GOBP_CARTILAGE_DEVELOPMENT, GOBP_SKELETAL_SYSTEM_DEVELOPMENT, SP3_Q3, GOZGIT_ESR1_TARGETS_DN, GOBP_POSITIVE_REGULATION_OF_VASCULATURE_DEVELOPMENT, GOCC_CELL_SURFACE, AREB6_01, KYNG_DNA_DAMAGE_DN

GO Biological Process (21): vasculogenesis (GO:0001570), ganglioside metabolic process (GO:0001573), 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), positive regulation of gene expression (GO:0010628), negative regulation of gene expression (GO:0010629), cell migration (GO:0016477), cell adhesion mediated by integrin (GO:0033627), memory T cell differentiation (GO:0043379), positive regulation of angiogenesis (GO:0045766), cartilage development (GO:0051216), hard palate development (GO:0060022), placenta blood vessel development (GO:0060674), Langerhans cell differentiation (GO:0061520), cell-cell adhesion (GO:0098609), immune response (GO:0006955), cell surface receptor signaling pathway (GO:0007166), cell differentiation (GO:0030154)

GO Molecular Function (3): integrin binding (GO:0005178), metal ion binding (GO:0046872), extracellular matrix protein binding (GO:1990430)

GO Cellular Component (7): plasma membrane (GO:0005886), focal adhesion (GO:0005925), integrin complex (GO:0008305), cell surface (GO:0009986), integrin alphav-beta8 complex (GO:0034686), extracellular exosome (GO:0070062), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-5 pathways:

Category	Pathways
Extracellular matrix organization	2
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
gene expression	2
regulation of gene expression	2
cell adhesion	2
cellular anatomical structure	2
cell differentiation	1
blood vessel morphogenesis	1
ceramide metabolic process	1
glycosphingolipid metabolic process	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
positive regulation of macromolecule biosynthetic process	1
negative regulation of macromolecule biosynthetic process	1
cell motility	1
T cell differentiation involved in immune response	1
immunological memory formation process	1
angiogenesis	1
regulation of angiogenesis	1
positive regulation of vasculature development	1
skeletal system development	1
animal organ development	1
connective tissue development	1
anatomical structure development	1
secondary palate development	1
blood vessel development	1
placenta development	1
myeloid dendritic cell differentiation	1
immune system process	1
response to stimulus	1
signal transduction	1
signaling receptor binding	1
protein-containing complex binding	1
cell adhesion molecule binding	1
cation binding	1
protein binding	1
membrane	1
cell periphery	1

Protein interactions and networks

STRING

1410 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
ITGB8	ITGAV	P06756	925
ITGB8	ITGA10	O75578	678
ITGB8	ITGA11	Q9UKX5	658
ITGB8	ITGA5	P08648	641
ITGB8	ITGA2	P17301	640
ITGB8	TGFB1	P01137	638
ITGB8	TGFB3	P10600	628
ITGB8	ITGA4	P13612	616
ITGB8	ITGA3	P26006	615
ITGB8	ITGA1	P56199	613
ITGB8	TGFB2	P08112	597
ITGB8	COL4A1	P02462	553
ITGB8	LAMC2	Q13753	543
ITGB8	COL1A1	P02452	538
ITGB8	LAMC3	Q9Y6N6	530

IntAct

21 interactions, top by confidence:

A	B	Type	Score
LRRC32	SMPD2	psi-mi:“MI:0914”(association)	0.640
ITGB8	GET1	psi-mi:“MI:0914”(association)	0.530
RHBDL1	ITGB8	psi-mi:“MI:0914”(association)	0.530
TGFB1	LAMC1	psi-mi:“MI:0914”(association)	0.530
CENPH	PSMD11	psi-mi:“MI:0914”(association)	0.530
FBXO2	TMEM131L	psi-mi:“MI:0914”(association)	0.530
LGALS1	PODXL	psi-mi:“MI:0914”(association)	0.530
ITGAV	ITGB8	psi-mi:“MI:0915”(physical association)	0.400
Prdm16	ESYT2	psi-mi:“MI:0914”(association)	0.350
TREX1	ITGB8	psi-mi:“MI:0914”(association)	0.350
ITGB8	TARS3	psi-mi:“MI:0914”(association)	0.350
TYROBP	KCNN4	psi-mi:“MI:0914”(association)	0.350
CD3D	ITGB8	psi-mi:“MI:0914”(association)	0.350
CLGN	TMEM131L	psi-mi:“MI:0914”(association)	0.350
LRRC32	ORC4	psi-mi:“MI:0914”(association)	0.350
TYROBP	SCAMP2	psi-mi:“MI:0914”(association)	0.350
DISC1	ITGB8	psi-mi:“MI:0915”(physical association)	0.000
DYRK1A	ITGB8	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (51): RHEB (Affinity Capture-MS), RPL23 (Affinity Capture-MS), SLC25A16 (Affinity Capture-MS), GINM1 (Affinity Capture-MS), LMF1 (Affinity Capture-MS), WRB (Affinity Capture-MS), NME4 (Affinity Capture-MS), GINM1 (Affinity Capture-MS), ACTR3C (Affinity Capture-MS), LMF1 (Affinity Capture-MS), NME4 (Affinity Capture-MS), L2HGDH (Affinity Capture-MS), WRB (Affinity Capture-MS), B3GNT2 (Affinity Capture-MS), ITGB8 (Affinity Capture-MS)

ESM2 similar proteins: A0A1D5PUP4, A5YT95, O35757, O62650, O75882, O95980, P07225, P09858, P10669, P17247, P19883, P21214, P21674, P26012, P26013, P27090, P30371, P31514, P31515, P47931, P49767, P50291, P61811, P61812, P97299, P97953, Q07257, Q0VBD0, Q17QD6, Q38L25, Q5RA73, Q6NW40, Q6V9H4, Q6ZQ11, Q863H1, Q86X52, Q8BFR2, Q8CI19, Q8JG54, Q8N475

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

7 interactions.

A	Effect	B	Mechanism
ITGB8	up-regulates	TGFB1
ITGB1BP1	“down-regulates activity”	ITGB8	binding
DOK1	“down-regulates activity”	ITGB8	binding
ITGB8	“up-regulates activity”	PTK2
Kindlin	“up-regulates activity”	ITGB8	binding
TLN1	“up-regulates activity”	ITGB8	binding
ITGB8	“form complex”	“Av/b8 integrin”	binding

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	2
Likely pathogenic	0
Uncertain significance	98
Likely benign	3
Benign	1

Top pathogenic / likely-pathogenic (2)

Variant ID	HGVS	Classification
148859	GRCh38/hg38 7p21.2-15.3(chr7:15533812-24851432)x1	Pathogenic
563419	GRCh37/hg19 7p21.2-15.3(chr7:14544155-21719929)x3	Pathogenic

SpliceAI

2907 predictions. Top by Δscore:

Variant	Effect	Δscore
7:20332025:T:G	donor_loss	1.0000
7:20363635:A:AG	acceptor_gain	1.0000
7:20363636:G:GG	acceptor_gain	1.0000
7:20363636:GAA:G	acceptor_gain	1.0000
7:20380661:C:G	acceptor_gain	1.0000
7:20380661:CACA:C	acceptor_loss	1.0000
7:20380662:ACAGT:A	acceptor_gain	1.0000
7:20380663:C:G	acceptor_gain	1.0000
7:20380663:CAGT:C	acceptor_loss	1.0000
7:20380664:A:AG	acceptor_gain	1.0000
7:20380664:A:C	acceptor_loss	1.0000
7:20380664:AGT:A	acceptor_gain	1.0000
7:20380665:G:GG	acceptor_gain	1.0000
7:20380665:GT:G	acceptor_gain	1.0000
7:20380665:GTG:G	acceptor_gain	1.0000
7:20380794:G:GT	donor_gain	1.0000
7:20380827:GTGAA:G	donor_gain	1.0000
7:20380828:TG:T	donor_gain	1.0000
7:20380829:G:GT	donor_gain	1.0000
7:20380829:GAA:G	donor_gain	1.0000
7:20380832:G:GG	donor_gain	1.0000
7:20381725:A:G	acceptor_gain	1.0000
7:20381726:GA:G	acceptor_gain	1.0000
7:20381726:GAGTC:G	acceptor_gain	1.0000
7:20381894:GCA:G	donor_gain	1.0000
7:20381896:A:AG	donor_gain	1.0000
7:20381897:G:GG	donor_gain	1.0000
7:20390328:A:AG	donor_gain	1.0000
7:20391494:ATAAG:A	donor_loss	1.0000
7:20391497:AGGTA:A	donor_loss	1.0000

AlphaMissense

5093 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
7:20379293:T:A	C211S	1.000
7:20379294:G:C	C211S	1.000
7:20380682:T:A	C218S	1.000
7:20380683:G:A	C218Y	1.000
7:20380683:G:C	C218S	1.000
7:20380684:C:G	C218W	1.000
7:20380777:C:A	N249K	1.000
7:20380777:C:G	N249K	1.000
7:20380826:T:C	C266R	1.000
7:20380827:G:A	C266Y	1.000
7:20380828:T:G	C266W	1.000
7:20381739:T:A	W272R	1.000
7:20381739:T:C	W272R	1.000
7:20381741:G:C	W272C	1.000
7:20381741:G:T	W272C	1.000
7:20381790:C:G	H289D	1.000
7:20379108:T:C	L149P	0.999
7:20379117:T:C	L152P	0.999
7:20379122:G:C	D154H	0.999
7:20379122:G:T	D154Y	0.999
7:20379123:A:C	D154A	0.999
7:20379123:A:G	D154G	0.999
7:20379123:A:T	D154V	0.999
7:20379124:T:A	D154E	0.999
7:20379124:T:G	D154E	0.999
7:20379222:G:A	G187E	0.999
7:20379228:G:A	G189D	0.999
7:20379230:T:C	S190P	0.999
7:20379243:A:T	K194I	0.999
7:20379244:A:C	K194N	0.999

dbSNP variants (sampled 300 via entrez): RS1000024208 (7:20354226 G>T), RS1000045034 (7:20405133 C>T), RS1000054011 (7:20365044 T>C,G), RS1000098888 (7:20358806 G>A,T), RS1000122336 (7:20366292 C>A), RS1000147508 (7:20370690 A>C), RS1000154280 (7:20358655 G>A), RS1000173407 (7:20369481 C>T), RS1000179367 (7:20329310 A>G), RS1000223430 (7:20409215 T>C), RS1000272756 (7:20397895 T>C), RS1000311983 (7:20363821 A>G), RS1000353078 (7:20393400 C>A,G), RS1000355384 (7:20336273 G>A), RS1000355787 (7:20376772 G>A)

Disease associations

OMIM: gene MIM:604160 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

70 associations (top):

Study	Trait	p-value
GCST004063_111	Waist circumference adjusted for body mass index	4.000000e-09
GCST004063_118	Waist circumference adjusted for body mass index	7.000000e-06
GCST004131_10	Inflammatory bowel disease	3.000000e-08
GCST004500_18	Waist circumference adjusted for BMI (adjusted for smoking behaviour)	2.000000e-08
GCST004501_93	Waist circumference adjusted for BMI (joint analysis main effects and smoking interaction)	6.000000e-08
GCST004504_66	Waist circumference adjusted for BMI in non-smokers	2.000000e-07
GCST004562_136	Waist circumference adjusted for body mass index	2.000000e-08
GCST004562_30	Waist circumference adjusted for body mass index	9.000000e-09
GCST004563_113	Waist circumference adjusted for BMI (joint analysis main effects and physical activity interaction)	4.000000e-08
GCST004563_250	Waist circumference adjusted for BMI (joint analysis main effects and physical activity interaction)	2.000000e-08
GCST004564_214	Waist circumference adjusted for BMI in active individuals	7.000000e-07
GCST004564_215	Waist circumference adjusted for BMI in active individuals	7.000000e-07
GCST005038_113	Allergic disease (asthma, hay fever or eczema)	2.000000e-14
GCST005038_114	Allergic disease (asthma, hay fever or eczema)	7.000000e-09
GCST005975_14	Eosinophil count	3.000000e-18
GCST006085_87	Prostate cancer	8.000000e-09
GCST007294_146	Body fat distribution (trunk fat ratio)	2.000000e-14
GCST007294_85	Body fat distribution (trunk fat ratio)	3.000000e-21
GCST007295_109	Body fat distribution (leg fat ratio)	6.000000e-16
GCST007295_93	Body fat distribution (leg fat ratio)	3.000000e-11
GCST007564_11	Asthma or allergic disease (pleiotropy)	3.000000e-10
GCST007692_106	Chronic obstructive pulmonary disease	7.000000e-09
GCST007797_54	Asthma onset (childhood vs adult)	7.000000e-08
GCST007798_80	Asthma	1.000000e-12
GCST007798_81	Asthma	2.000000e-15
GCST007800_60	Asthma (childhood onset)	8.000000e-17
GCST007800_73	Asthma (childhood onset)	7.000000e-22
GCST007941_11	Medication use (adrenergics, inhalants)	3.000000e-10
GCST008876_26	Non-lobar intracerebral hemorrhage (MTAG)	2.000000e-06
GCST008916_31	Asthma	2.000000e-10

EFO canonical traits (12, from GWAS)

EFO ID	Trait name
EFO:0007789	BMI-adjusted waist circumference
EFO:0004318	smoking behavior
EFO:0008002	physical activity measurement
EFO:0004842	eosinophil count
EFO:0004341	body fat distribution
EFO:0004847	age at onset
EFO:0009941	Inhalant adrenergic use measurement
EFO:0010178	non-lobar intracerebral hemorrhage
EFO:0010517	oxalate measurement
EFO:0007991	eosinophil percentage of leukocytes
EFO:0007788	BMI-adjusted waist-hip ratio
EFO:0008039	BMI-adjusted hip circumference

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (3): CHEMBL3430892 (PROTEIN COMPLEX), CHEMBL6066568 (PROTEIN COMPLEX), CHEMBL6066571 (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: 185 (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
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	7.6	pKi

Binding affinities (BindingDB)

20 measured of 20 human assays (20 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
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
3-[3-[4-(1,4-dihydroisoquinolin-3-ylamino)butyl]-2-oxoimidazolidin-1-yl]-3-[3-(trifluoromethyl)phenyl]propanoic acid	IC50	622 nM	US-10118929: Nonanoic and decanoic acid derivatives and uses thereof

ChEMBL bioactivities

261 potent at pChembl≥5 of 261 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.22	IC50	0.06	nM	CHEMBL4443665
9.89	IC50	0.13	nM	CHEMBL5790863
9.70	IC50	0.2	nM	CHEMBL3319237
9.70	IC50	0.2	nM	CHEMBL5914164
9.52	IC50	0.3	nM	CHEMBL5781301
9.52	IC50	0.3	nM	CHEMBL5964326
9.52	IC50	0.3	nM	CHEMBL5786200
9.52	IC50	0.3	nM	CHEMBL5748399
9.52	IC50	0.3	nM	CHEMBL5770209
9.52	IC50	0.3	nM	CHEMBL5980310
9.40	IC50	0.4	nM	CHEMBL5974146
9.40	IC50	0.4	nM	CHEMBL5920684
9.40	IC50	0.4	nM	CHEMBL5889173
9.30	IC50	0.5	nM	CHEMBL5766697
9.30	IC50	0.5	nM	CHEMBL5802710
9.22	IC50	0.6	nM	CHEMBL5975238
9.22	IC50	0.6	nM	CHEMBL5790208
9.19	IC50	0.65	nM	CHEMBL244434
9.15	IC50	0.7	nM	CHEMBL5819051
9.00	IC50	1	nM	CHEMBL5951981
8.96	IC50	1.1	nM	CHEMBL5802648
8.92	IC50	1.2	nM	GLPG-0187
8.88	IC50	1.31	nM	CHEMBL4449438
8.81	IC50	1.54	nM	CHEMBL4520646
8.77	IC50	1.71	nM	CHEMBL244013
8.74	IC50	1.83	nM	CHEMBL4584228
8.70	IC50	2	nM	CHEMBL5784734
8.60	IC50	2.512	nM	CHEMBL4237498
8.56	Kd	2.754	nM	GSK-3008348 FREE BASE
8.56	Kd	2.74	nM	GSK-3008348 FREE BASE
8.52	IC50	3	nM	CHEMBL244013
8.50	IC50	3.162	nM	CHEMBL4242175
8.43	IC50	3.73	nM	CHEMBL4445931
8.40	IC50	3.981	nM	CHEMBL4240155
8.37	IC50	4.3	nM	CHEMBL4541418
8.35	IC50	4.5	nM	CHEMBL4546687
8.30	IC50	5.012	nM	CHEMBL4241584
8.30	IC50	5	nM	CHEMBL6027181
8.30	IC50	5	nM	CHEMBL242061
8.24	IC50	5.8	nM	CHEMBL4537950
8.23	IC50	5.92	nM	CHEMBL5825233
8.22	IC50	6	nM	CHEMBL5982261
8.22	IC50	6	nM	CHEMBL5946569
8.20	IC50	6.31	nM	CHEMBL4242635
8.20	IC50	6.31	nM	CHEMBL4246111
8.20	IC50	6.31	nM	CHEMBL4243686
8.20	IC50	6.31	nM	CHEMBL4249172
8.20	IC50	6.31	nM	CHEMBL4242732
8.20	IC50	6.3	nM	CHEMBL4577219
8.19	IC50	6.4	nM	CHEMBL4455010

PubChem BioAssay actives

162 with measured affinity, of 195 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-[(3S,6S,12S,15S,21S,24R)-12-[3-(diaminomethylideneamino)propyl]-21-[4-[6-[3-(2,2-difluoro-10,12-dimethyl-3-aza-1-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-1(12),4,6,8,10-pentaen-4-yl)propanoylamino]hexanoylamino]butyl]-22-methyl-3,15-bis(2-methylpropyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,22-octazabicyclo[22.3.0]heptacosan-6-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0001	uM
2-[(2,6-dichlorobenzoyl)amino]-3-[5-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)pentanoylamino]propanoic acid	2065304: Inhibition of recombinant human Integrin alphaVbeta8 using TMB as substrate incubated for 2 hrs in presence of LAP by ELISA	ic50	0.0002	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	1177816: Antagonist activity at alphavbeta8 integrin receptor (unknown origin) by cell-free ELISA	ic50	0.0002	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	1177808: Antagonist activity at human recombinant alphavbeta8 integrin receptor expressed in HEK293 cells after 4 hrs using p-nitrophenyl phosphate by colorimetry	ic50	0.0006	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	1177816: Antagonist activity at alphavbeta8 integrin receptor (unknown origin) by cell-free ELISA	ic50	0.0012	uM
2-[(3R,9S,12S,18S,21S,24S,27S)-18-[3-(diaminomethylideneamino)propyl]-24-methyl-9,21-bis(2-methylpropyl)-2,8,11,14,17,20,23,26-octaoxo-1,7,10,13,16,19,22,25-octazatricyclo[25.3.0.03,7]triacontan-12-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0013	uM
2-[(3R,9S,12S,18S,21S,24S,27S)-21-[(2S)-butan-2-yl]-18-[3-(diaminomethylideneamino)propyl]-24-methyl-9-(2-methylpropyl)-2,8,11,14,17,20,23,26-octaoxo-1,7,10,13,16,19,22,25-octazatricyclo[25.3.0.03,7]triacontan-12-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0015	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	1177808: Antagonist activity at human recombinant alphavbeta8 integrin receptor expressed in HEK293 cells after 4 hrs using p-nitrophenyl phosphate by colorimetry	ic50	0.0017	uM
2-[(3R,9S,12S,18S,21S,24S,27S)-21-benzyl-18-[3-(diaminomethylideneamino)propyl]-24-methyl-9-(2-methylpropyl)-2,8,11,14,17,20,23,26-octaoxo-1,7,10,13,16,19,22,25-octazatricyclo[25.3.0.03,7]triacontan-12-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0018	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	1400433: Antagonist activity at human integrin alphaVbeta8 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-(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	1400447: Binding affinity to human integrin alphaVbeta8 after 2 hrs by liquid scintillation counting	kd	0.0027	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	1400433: Antagonist activity at human integrin alphaVbeta8 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0032	uM
2-[(3R,9S,12S,18S,21S,24S,27S)-18-[3-(diaminomethylideneamino)propyl]-21-(1H-indol-3-ylmethyl)-24-methyl-9-(2-methylpropyl)-2,8,11,14,17,20,23,26-octaoxo-1,7,10,13,16,19,22,25-octazatricyclo[25.3.0.03,7]triacontan-12-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0037	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	1400433: Antagonist activity at human integrin alphaVbeta8 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
2-[(3R,9S,12S,15S,18S,21S,24S,27S)-21-benzyl-18-[3-(diaminomethylideneamino)propyl]-15-[(1R)-1-hydroxyethyl]-24-methyl-9-(2-methylpropyl)-2,8,11,14,17,20,23,26-octaoxo-1,7,10,13,16,19,22,25-octazatricyclo[25.3.0.03,7]triacontan-12-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0043	uM
2-[(3R,9S,12S,18S,21S,27S)-18-[3-(diaminomethylideneamino)propyl]-9,21-bis(2-methylpropyl)-2,8,11,14,17,20,23,26-octaoxo-1,7,10,13,16,19,22,25-octazatricyclo[25.3.0.03,7]triacontan-12-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0045	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	1400433: Antagonist activity at human integrin alphaVbeta8 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0050	uM
2-[(3R,9S,12S,15S,18S,21S,24S,27S)-21-benzyl-18-[3-(diaminomethylideneamino)propyl]-15-(hydroxymethyl)-24-methyl-9-(2-methylpropyl)-2,8,11,14,17,20,23,26-octaoxo-1,7,10,13,16,19,22,25-octazatricyclo[25.3.0.03,7]triacontan-12-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0058	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	1400433: Antagonist activity at human integrin alphaVbeta8 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-[(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	1400433: Antagonist activity at human integrin alphaVbeta8 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-(oxan-4-yloxy)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400433: Antagonist activity at human integrin alphaVbeta8 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)-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	1400433: Antagonist activity at human integrin alphaVbeta8 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-cyclopropylphenyl)-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid	1400433: Antagonist activity at human integrin alphaVbeta8 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
2-[(3R,9S,12S,18S,21S,24S,27S)-21-(carboxymethyl)-18-[3-(diaminomethylideneamino)propyl]-24-methyl-9-(2-methylpropyl)-2,8,11,14,17,20,23,26-octaoxo-1,7,10,13,16,19,22,25-octazatricyclo[25.3.0.03,7]triacontan-12-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0063	uM
2-[(3R,9S,12S,18S,21S,24S,27S)-18-[3-(diaminomethylideneamino)propyl]-24-methyl-9-(2-methylpropyl)-2,8,11,14,17,20,23,26-octaoxo-21-phenyl-1,7,10,13,16,19,22,25-octazatricyclo[25.3.0.03,7]triacontan-12-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0064	uM
2-[(3R,9S,12S,18S,21S,24S,27S)-21-(4-aminobutyl)-18-[3-(diaminomethylideneamino)propyl]-24-methyl-9-(2-methylpropyl)-2,8,11,14,17,20,23,26-octaoxo-1,7,10,13,16,19,22,25-octazatricyclo[25.3.0.03,7]triacontan-12-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0073	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	1400433: Antagonist activity at human integrin alphaVbeta8 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-(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	1400433: Antagonist activity at human integrin alphaVbeta8 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-(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	1400433: Antagonist activity at human integrin alphaVbeta8 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
2-[(3S,6S,12S,15S,21S,24R)-21-(4-acetamidobutyl)-12-[3-(diaminomethylideneamino)propyl]-22-methyl-3,15-bis(2-methylpropyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,22-octazabicyclo[22.3.0]heptacosan-6-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0080	uM
2-[(3R,9S,12S,18S,21S,24S,27S)-18-[3-(diaminomethylideneamino)propyl]-21,24-dimethyl-9-(2-methylpropyl)-2,8,11,14,17,20,23,26-octaoxo-1,7,10,13,16,19,22,25-octazatricyclo[25.3.0.03,7]triacontan-12-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0081	uM
2-[(3R,6S,9S,15S,18S,21S,24S)-3-benzyl-15-[3-(diaminomethylideneamino)propyl]-4,21-dimethyl-6,18-bis(2-methylpropyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,22-octazabicyclo[22.3.0]heptacosan-9-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0094	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	1400433: Antagonist activity at human integrin alphaVbeta8 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0100	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	1400433: Antagonist activity at human integrin alphaVbeta8 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0100	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	1400433: Antagonist activity at human integrin alphaVbeta8 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0100	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	1400433: Antagonist activity at human integrin alphaVbeta8 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0100	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	1400433: Antagonist activity at human integrin alphaVbeta8 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0100	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	1400433: Antagonist activity at human integrin alphaVbeta8 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0100	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	1400433: Antagonist activity at human integrin alphaVbeta8 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0100	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	1577143: Inhibition of integrin alphavbeta8 (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	0.0100	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	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0104	uM
2-[(3R,9S,12S,18S,21S,27S)-29-acetamido-18-[3-(diaminomethylideneamino)propyl]-9,21-bis(2-methylpropyl)-2,8,11,14,17,20,23,26-octaoxo-1,7,10,13,16,19,22,25-octazatricyclo[25.3.0.03,7]triacontan-12-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0105	uM
2-[(3R,6S,9S,15S,18S,21S,24S)-3-(4-aminobutyl)-15-[3-(diaminomethylideneamino)propyl]-4,21-dimethyl-6,18-bis(2-methylpropyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,22-octazabicyclo[22.3.0]heptacosan-9-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0121	uM
2-[(3R,9S,12S,18S,21S,24S,27S)-18-[3-(diaminomethylideneamino)propyl]-24-(hydroxymethyl)-9,21-bis(2-methylpropyl)-2,8,11,14,17,20,23,26-octaoxo-1,7,10,13,16,19,22,25-octazatricyclo[25.3.0.03,7]triacontan-12-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0125	uM
2-[(3R,9S,12S,18S,21S,27S)-18-[3-(diaminomethylideneamino)propyl]-29-(hexylamino)-9,21-bis(2-methylpropyl)-2,8,11,14,17,20,23,26-octaoxo-1,7,10,13,16,19,22,25-octazatricyclo[25.3.0.03,7]triacontan-12-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0128	uM
2-[(3R,6S,9S,15S,18S,21S,24S)-15-[3-(diaminomethylideneamino)propyl]-4,21-dimethyl-3,6,18-tris(2-methylpropyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,22-octazabicyclo[22.3.0]heptacosan-9-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0150	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	1400433: Antagonist activity at human integrin alphaVbeta8 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0158	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	1400433: Antagonist activity at human integrin alphaVbeta8 expressed in human K562 cells assessed as reduction in cell adhesion to GST-LAP after 30 mins by BCECF-AM-fluorescence based assay	ic50	0.0158	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	1577143: Inhibition of integrin alphavbeta8 (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	0.0158	uM
2-[(3R,9S,12S,18S,24S,27S)-18-[3-(diaminomethylideneamino)propyl]-24-methyl-9-(2-methylpropyl)-2,8,11,14,17,20,23,26-octaoxo-1,7,10,13,16,19,22,25-octazatricyclo[25.3.0.03,7]triacontan-12-yl]acetic acid	1614469: Inhibition of LAP binding to human integrin alphavbeta8 receptor after 1 hr by solid-phase binding assay	ic50	0.0159	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	increases expression, affects expression, decreases expression	5
Air Pollutants	increases expression, affects cotreatment, decreases expression, increases abundance	3
Asbestos, Serpentine	decreases methylation, increases expression	3
Particulate Matter	increases abundance, decreases expression	3
perfluorooctane sulfonic acid	decreases expression	2
Benzo(a)pyrene	increases expression	2
Copper	affects binding, decreases expression	2
Estradiol	affects expression, affects cotreatment, decreases expression	2
Phenylmercuric Acetate	affects cotreatment, increases expression	2
Aflatoxin B1	decreases methylation, increases methylation	2
Cadmium Chloride	increases expression	2
aristolochic acid I	decreases expression	1
peracetylated N-azidoacetylmannosamine	decreases expression	1
TL8-506	increases expression, affects cotreatment	1
tungsten carbide	affects cotreatment, decreases expression	1
methylmercuric chloride	increases expression	1
alpha-pinene	decreases expression, increases abundance, affects cotreatment	1
bisphenol A	decreases expression	1
trichostatin A	decreases expression, increases expression	1
2-butenal	affects cotreatment, decreases expression	1
2,4,5,2’,4’,5’-hexachlorobiphenyl	affects expression	1
sodium arsenite	decreases expression	1
butyraldehyde	decreases expression	1
nickel chloride	increases expression	1
3,4,5,3’,4’-pentachlorobiphenyl	increases expression	1
perfluorooctanoic acid	affects expression, decreases reaction	1
3,4,3’,4’-tetrachlorobiphenyl	affects expression	1
rutecarpine	increases expression	1
methacrylaldehyde	affects cotreatment, decreases expression, increases abundance	1
S-(1,2-dichlorovinyl)cysteine	affects cotreatment, increases expression, decreases reaction	1

ChEMBL screening assays

33 unique, capped per target: 32 binding, 1 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3368776	Binding	Antagonist activity at human recombinant alphavbeta8 integrin receptor expressed in HEK293 cells after 4 hrs using p-nitrophenyl phosphate by colorimetry	Strategies to inhibit tumor associated integrin receptors: rationale for dual and multi-antagonists. — J Med Chem
CHEMBL4709542	ADMET	Inhibition of integrin alphavbeta8 (unknown origin) by fluorescence polarization assay	Discovery of the first potent and selective αβ integrin inhibitor based on an amide-containing core. — Eur J Med Chem

Cellosaurus cell lines

1 cell lines: 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_D9HI	Ubigene HEK293 ITGB8 KO	Transformed cell line	Female

Clinical trials (associated diseases)

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