ITGB1

Summary

ITGB1 (integrin subunit beta 1, HGNC:6153) is a protein-coding gene on chromosome 10p11.22, encoding Integrin beta-1 (P05556). Integrins alpha-1/beta-1, alpha-2/beta-1, alpha-10/beta-1 and alpha-11/beta-1 are receptors for collagen. It is a selective cancer dependency (DepMap: 17.6% of cell lines).

Integrins are heterodimeric proteins made up of alpha and beta subunits. At least 18 alpha and 8 beta subunits have been described in mammals. Integrin family members are membrane receptors involved in cell adhesion and recognition in a variety of processes including embryogenesis, hemostasis, tissue repair, immune response and metastatic diffusion of tumor cells. This gene encodes a beta subunit. Multiple alternatively spliced transcript variants which encode different protein isoforms have been found for this gene.

Source: NCBI Gene 3688 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 97 total
• Phenotypes (HPO): 2
• Druggable target: yes — 4 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 17.6% of screened cell lines
• MANE Select transcript: NM_002211

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:6153
Approved symbol	ITGB1
Name	integrin subunit beta 1
Location	10p11.22
Locus type	gene with protein product
Status	Approved
Aliases	CD29, GPIIA
Ensembl gene	ENSG00000150093
Ensembl biotype	protein_coding
OMIM	135630
Entrez	3688

Gene structure

Transcript identifiers

Ensembl transcripts: 89 — 79 protein_coding, 5 nonsense_mediated_decay, 4 retained_intron, 1 protein_coding_CDS_not_defined

ENST00000302278, ENST00000396033, ENST00000414670, ENST00000417122, ENST00000423113, ENST00000437302, ENST00000439974, ENST00000464001, ENST00000472147, ENST00000474568, ENST00000475184, ENST00000480226, ENST00000484088, ENST00000488427, ENST00000488494, ENST00000494395, ENST00000528877, ENST00000534049, ENST00000609742, ENST00000676460, ENST00000676623, ENST00000676659, ENST00000676895, ENST00000676964, ENST00000677310, ENST00000677363, ENST00000677999, ENST00000678120, ENST00000678479, ENST00000678591, ENST00000678701, ENST00000678766, ENST00000678943, ENST00000678952, ENST00000678989, ENST00000679187, ENST00000898616, ENST00000898617, ENST00000898618, ENST00000898619, ENST00000898620, ENST00000898621, ENST00000898622, ENST00000898623, ENST00000898624, ENST00000898625, ENST00000898626, ENST00000898627, ENST00000898628, ENST00000898629, ENST00000898630, ENST00000898631, ENST00000898632, ENST00000898633, ENST00000898634, ENST00000898635, ENST00000898636, ENST00000898637, ENST00000898638, ENST00000898639, ENST00000898640, ENST00000931352, ENST00000931353, ENST00000931354, ENST00000931355, ENST00000931356, ENST00000931357, ENST00000931358, ENST00000931359, ENST00000931360, ENST00000931361, ENST00000966585, ENST00000966586, ENST00000966587, ENST00000966588, ENST00000966589, ENST00000966590, ENST00000966591, ENST00000966592, ENST00000966593, ENST00000966594, ENST00000966595, ENST00000966596, ENST00000966597, ENST00000966598, ENST00000966599, ENST00000966600, ENST00000966601, ENST00000966602

RefSeq mRNA: 3 — MANE Select: NM_002211 NM_002211, NM_033668, NM_133376

CCDS: CCDS7174

Canonical transcript exons

ENST00000302278 — 16 exons

Exon	Start	End
ENSE00000993762	32923585	32923740
ENSE00000993763	32910223	32910455
ENSE00000993764	32911886	32912124
ENSE00000993765	32911448	32911670
ENSE00000993766	32919885	32920084
ENSE00000993772	32928094	32928264
ENSE00000993773	32922257	32922346
ENSE00000993776	32925871	32926109
ENSE00000993777	32920245	32920385
ENSE00000993778	32922640	32922735
ENSE00001899854	32958145	32958230
ENSE00001947973	32900318	32901635
ENSE00003562369	32929822	32930044
ENSE00003593702	32932515	32932600
ENSE00003606416	32908368	32908534
ENSE00003754922	32935492	32935558

Expression profiles

Bgee: expression breadth ubiquitous, 303 present calls, max score 99.91.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 300.6826 / max 3774.9955, expressed in 1821 samples.

FANTOM5 promoters (12 alternative TSS)

Promoter ID	TPM avg	Samples expressed
109043	278.4861	1821
109042	9.5462	1508
109044	3.2064	1278
109039	3.1998	849
109013	2.5286	924
109027	1.2570	609
109041	1.1115	517
109040	0.4840	255
205810	0.4114	228
109038	0.2620	151

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
visceral pleura	UBERON:0002401	99.91	gold quality
seminal vesicle	UBERON:0000998	99.82	gold quality
pleura	UBERON:0000977	99.81	gold quality
cauda epididymis	UBERON:0004360	99.80	gold quality
parietal pleura	UBERON:0002400	99.78	gold quality
stromal cell of endometrium	CL:0002255	99.76	gold quality
blood vessel layer	UBERON:0004797	99.74	gold quality
tibia	UBERON:0000979	99.73	gold quality
smooth muscle tissue	UBERON:0001135	99.72	gold quality
superficial temporal artery	UBERON:0001614	99.68	gold quality
descending thoracic aorta	UBERON:0002345	99.67	gold quality
palpebral conjunctiva	UBERON:0001812	99.63	gold quality
thoracic aorta	UBERON:0001515	99.60	gold quality
ascending aorta	UBERON:0001496	99.59	gold quality
heart right ventricle	UBERON:0002080	99.59	gold quality
saphenous vein	UBERON:0007318	99.59	gold quality
right coronary artery	UBERON:0001625	99.56	gold quality
caput epididymis	UBERON:0004358	99.55	gold quality
endometrium	UBERON:0001295	99.54	gold quality
mucosa of sigmoid colon	UBERON:0004993	99.54	gold quality
germinal epithelium of ovary	UBERON:0001304	99.53	gold quality
mammary duct	UBERON:0001765	99.53	gold quality
aorta	UBERON:0000947	99.52	gold quality
skin of hip	UBERON:0001554	99.50	gold quality
urethra	UBERON:0000057	99.48	gold quality
calcaneal tendon	UBERON:0003701	99.47	gold quality
corpus epididymis	UBERON:0004359	99.47	gold quality
popliteal artery	UBERON:0002250	99.46	gold quality
tibial artery	UBERON:0007610	99.46	gold quality
colonic epithelium	UBERON:0000397	99.45	gold quality

Single-cell (SCXA)

Detected in 33 experiment(s), a significant marker in 25.

Experiment	Marker?	Max mean expression
E-MTAB-9841	yes	983.10
E-CURD-112	yes	817.09
E-MTAB-6108	yes	757.27
E-MTAB-10018	yes	540.94
E-MTAB-8142	yes	119.98
E-HCAD-4	yes	71.77
E-CURD-122	yes	55.06
E-HCAD-10	yes	52.95
E-MTAB-6701	yes	49.45
E-HCAD-6	yes	40.56
E-MTAB-8410	yes	39.88
E-GEOD-135922	yes	39.02
E-HCAD-1	yes	36.25
E-GEOD-134144	yes	31.48
E-CURD-46	yes	28.22

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CTNNB1, ERP29, ESR1, FOXC2, FOXF2, FOXM1, GLI1, GLI2, HIF1A, HOXA4, HOXD1, HOXD3, ITGB8, JUN, LEF1, MYC, NFKB, PAX6, PPM1F, PRKCQ, SMAD3, SNAI2, SPI1, SRF, STAT1, TWIST1, TWIST2, YY1, ZBTB4

miRNA regulators (miRDB)

91 targeting ITGB1, 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-5692A	100.00	74.40	6850
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-29A-3P	100.00	73.11	1835
HSA-MIR-29B-3P	100.00	73.18	1833
HSA-MIR-29C-3P	100.00	73.15	1833
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-548AW	99.99	72.57	3559
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-548AN	99.97	70.91	2817
HSA-MIR-3688-3P	99.97	72.02	2834
HSA-MIR-9-3P	99.96	70.88	2068
HSA-MIR-493-5P	99.96	72.47	2382
HSA-MIR-548AA	99.96	70.64	3753
HSA-MIR-548AP-3P	99.96	70.64	3753
HSA-MIR-548T-3P	99.96	70.64	3753
HSA-LET-7C-3P	99.95	73.42	2862
HSA-MIR-3910	99.95	71.13	2227
HSA-MIR-6753-3P	99.93	66.57	637
HSA-MIR-7107-3P	99.93	66.73	627
HSA-MIR-6768-5P	99.92	67.36	1942
HSA-MIR-1305	99.91	71.43	3443
HSA-MIR-7-1-3P	99.91	71.53	4384
HSA-MIR-7-2-3P	99.91	71.40	4394
HSA-MIR-8063	99.91	69.76	3146
HSA-MIR-498-3P	99.91	71.27	1114
HSA-MIR-124-3P	99.89	73.74	3043
HSA-MIR-506-3P	99.89	73.55	3057
HSA-MIR-605-3P	99.88	69.22	1833

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 17.6% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 40)

• the linkage between beta1 integrin and actin may be differentially regulated by its tyrosine and serine/threonine phosphorylation in normal and cancerous breast cells. (PMID:11716783)
• Mechanisms involved in alpha6beta1-integrin-mediated Ca(2+) signalling (PMID:11728829)
• Site-directed mutagenesis showed that Leu(135), Ile(138), and Ile(139) of Icap1 alpha, and Leu(82) and Tyr(144), are required for the Icap1 alpha-beta(1) integrin interaction (PMID:11741908)
• both VEGF-induced PI 3-kinase activation and beta(1) integrin-mediated binding to fibronectin are required for the recruitment and activation of PKC alpha. (PMID:11751905)
• Bromodeoxyuridine induces integrin expression at transcriptional (alpha2 subunit) and post-transcriptional (beta1 subunit) levels, and alters the adhesive properties of two human lung tumour cell lines. (PMID:11775028)
• Although cytoplasmic splice variants do not change the ligand-specificity of a beta 1 integrin, this review explains how clustering of different splice variants triggers signaling pathways that lead to a different cellular response. (PMID:11779688)
• beta 1-Integrin-mediated glioma cell adhesion and free radical-induced apoptosis are regulated by binding to a C-terminal domain of PG-M/versican (PMID:11805102)
• These results demonstrate that integrin-dependent cell to extracellular matrix adhesion reinforces E-cadherin-dependent cell-cell adhesion in Caco-2 cells. (PMID:11861761)
• Integrin activation involves a conformational change in the alpha 1 helix of the beta subunit A-domain (PMID:11893752)
• Data demonstrate that multiple tetraspanin (transmembrane 4 superfamily) proteins such as CD151 are palmitoylated, and that palmitoylation is not required for cd151-alpha3beta1 integrin association. (PMID:11907260)
• Activated Notch4 inhibits angiogenesis: role of beta 1-integrin activation. (PMID:11909975)
• role of the specificity-determining loop of the integrin beta subunit I-like domain in autonomous expression, association with the alpha subunit, and ligand binding (PMID:11914080)
• mechanical stress to the beta1-integrin subunit in osteoblasts revealed that cyclic forces of 1 Hz were more effective to stimulate the cellular calcium response than continuous load (PMID:11918217)
• beta1 and beta2 integrins activate different signalling pathways in monocytes. (PMID:11931654)
• Inv-induced cell death was mediated via beta1-integrins since Inv bound to the beta1-integrin subunit (CD29), anti-beta(1)-integrin antibodies blocked Inv-induced cell death and Inv-induced cell death was absent in two beta1-integrin- cell lines. (PMID:11932920)
• Beta1 integrin triggering affects leukemic cell line sensitivity to natural killer cells (PMID:11941451)
• Evidence for distinctive signaling of CD82- and beta1 integrin-mediated costimulation at the transcriptional level of IL-2 gene. (PMID:11981820)
• There is a desensitization of IL-8-mediated p42/p44 MAPK signaling in response to ligation of the alpha5beta1 integrin in PMNL. There may be an interplay between integrin and chemokine signaling during PMNL migration through the extracellular matrix. (PMID:11989791)
• Expression of beta1-integrins and N-cadherin in bladder cancer and melanoma cell lines (PMID:11996105)
• Ionizing radiation strongly induced the expression of functional beta1-integrin and ILK in the two lung cancer cell lines, A549 and SKMES1. (PMID:12020426)
• mediates adhesion of osteosarcoma to the core region of thrombospondin 1 (alpha 4 beta 1 integrin) (PMID:12054567)
• role in regulating beta 1 integrin-dependent leukocyte adhesion (PMID:12091396)
• results suggest that engagement of the alpha 5 beta 1 integrin promotes an NF-kappa B-dependent program of gene expression that coordinately regulates angiogenesis and inflammation (PMID:12138201)
• VLA4 integrin activation by chemokines requires cholesterol (PMID:12163503)
• role of Rap1 GTPase for Mn(2+)- and antibody-induced VLA-4-mediated cell adhesion [VLA-4] (PMID:12171996)
• Expression of focal adhesion kinase and alpha5 and beta1 integrins in carcinomas and its clinical significance. (PMID:12174366)
• Data show that, in vitro, under physiological conditions, CD98 is constitutively associated with beta1 integrins regardless of activation status. (PMID:12181350)
• Data report the identification of signaling pathways required for suppression of integrin alpha2beta1 function by c-erbB2. (PMID:12181354)
• ITGB1 activated by ERK1/2, p38 MAPK after hypoxia (PMID:12200131)
• data suggest that overexpression of beta 1-integrin confers resistance to apoptosis in hepatoma cells via a MAP kinase dependent pathway (PMID:12209735)
• regulation of alpha4beta1 integrin function in melanoma cells and T cells by ligands of CD47 (PMID:12218055)
• role in mediating pro-angiogenic activity of CYR61 (PMID:12364323)
• beta1 integrin engagement is required for bombesin-dependent pro-MMP-9 activation in prostatic cancer cells (PMID:12372334)
• beta1 integrin engagement is required for bombesin-dependent pro-MMP-9 activation in prostatic cancer cells (PMID:12372334)
• initial adhesion of endometrial cells to mesothelium is not mediated by beta1 integrins but attachment to collagen IV and collagen I, which are present in the submesothelial extracellular matrix, is mediated by beta1 integrins (PMID:12372459)
• molecular proximity of seprase and the urokinase-type plasminogen activator receptor on malignant melanoma cell membranes: dependence on the cytoskeleton and this protein (PMID:12376466)
• findings demonstrate that E-cadherin can interact with alpha2beta1 and suggest that heterotypic interactions between E-cadherin and integrins may be more common than originally thought (PMID:12392763)
• Temporal gene expression profile of precursor B leukemia cells induced by ITGB1 identifies pathways regulating B-cell survival. (PMID:12393420)
• results are consistent with an essential role for beta(1) integrins in maintenance of cardiomyocyte viability and interaction with extracellular matrix (PMID:12397575)
• Data show that the expression of the PAINS-13 epitope depends on CD9 association with alpha(6)beta(1) integrin. (PMID:12411441)

Cross-species orthologs

9 orthologs

Organism	Symbol	Gene ID
danio_rerio	itgb1b.2	ENSDARG00000022689
danio_rerio	itgb1b.1	ENSDARG00000053232
danio_rerio	itgb1a	ENSDARG00000071863
danio_rerio	itgb1b	ENSDARG00000104484
danio_rerio		ENSDARG00000109929
mus_musculus	Itgb1	ENSMUSG00000025809
rattus_norvegicus	Itgb1	ENSRNOG00000010966
drosophila_melanogaster	mys	FBGN0004657
caenorhabditis_elegans		WBGENE00003930

Paralogs (8): ITGB5 (ENSG00000082781), ITGB8 (ENSG00000105855), ITGB6 (ENSG00000115221), ITGB4 (ENSG00000132470), ITGB7 (ENSG00000139626), ITGB2 (ENSG00000160255), ITGBL1 (ENSG00000198542), ITGB3 (ENSG00000259207)

Protein

Protein identifiers

Integrin beta-1 — P05556 (reviewed: P05556)

Alternative names: Fibronectin receptor subunit beta, Glycoprotein IIa, VLA-4 subunit beta

All UniProt accessions (17): P05556, A0A7I2V2F9, A0A7I2V2T4, A0A7I2V348, A0A7I2V5T3, A0A7I2V5Z8, C9JNE0, C9JPK5, E7EQW5, E7EUI6, E9PLR6, E9PQJ2, H7C4K3, H7C4N8, Q5T3E4, Q5T3E5, Q5T3E6

UniProt curated annotations — full annotation on UniProt →

Function. Integrins alpha-1/beta-1, alpha-2/beta-1, alpha-10/beta-1 and alpha-11/beta-1 are receptors for collagen. Integrins alpha-1/beta-1 and alpha-2/beta-2 recognize the proline-hydroxylated sequence G-F-P-G-E-R in collagen. Integrins alpha-2/beta-1, alpha-3/beta-1, alpha-4/beta-1, alpha-5/beta-1, alpha-8/beta-1, alpha-10/beta-1, alpha-11/beta-1 and alpha-V/beta-1 are receptors for fibronectin. Alpha-4/beta-1 recognizes one or more domains within the alternatively spliced CS-1 and CS-5 regions of fibronectin. Integrin alpha-5/beta-1 is a receptor for fibrinogen. Integrin alpha-1/beta-1, alpha-2/beta-1, alpha-6/beta-1 and alpha-7/beta-1 are receptors for lamimin. Integrin alpha-6/beta-1 (ITGA6:ITGB1) is present in oocytes and is involved in sperm-egg fusion. Integrin alpha-4/beta-1 is a receptor for VCAM1. It recognizes the sequence Q-I-D-S in VCAM1. Integrin alpha-9/beta-1 is a receptor for VCAM1, cytotactin and osteopontin. It recognizes the sequence A-E-I-D-G-I-E-L in cytotactin. Integrin alpha-3/beta-1 is a receptor for epiligrin, thrombospondin and CSPG4. Alpha-3/beta-1 may mediate with LGALS3 the stimulation by CSPG4 of endothelial cells migration. Integrin alpha-V/beta-1 is a receptor for vitronectin. Beta-1 integrins recognize the sequence R-G-D in a wide array of ligands. When associated with alpha-7 integrin, regulates cell adhesion and laminin matrix deposition. Involved in promoting endothelial cell motility and angiogenesis. Involved in osteoblast compaction through the fibronectin fibrillogenesis cell-mediated matrix assembly process and the formation of mineralized bone nodules. May be involved in up-regulation of the activity of kinases such as PKC via binding to KRT1. Together with KRT1 and RACK1, serves as a platform for SRC activation or inactivation. Plays a mechanistic adhesive role during telophase, required for the successful completion of cytokinesis. Integrin alpha-3/beta-1 provides a docking site for FAP (seprase) at invadopodia plasma membranes in a collagen-dependent manner and hence may participate in the adhesion, formation of invadopodia and matrix degradation processes, promoting cell invasion. ITGA4:ITGB1 binds to fractalkine (CX3CL1) and may act as its coreceptor in CX3CR1-dependent fractalkine signaling. ITGA4:ITGB1 and ITGA5:ITGB1 bind to PLA2G2A via a site (site 2) which is distinct from the classical ligand-binding site (site 1) and this induces integrin conformational changes and enhanced ligand binding to site 1. ITGA5:ITGB1 acts as a receptor for fibrillin-1 (FBN1) and mediates R-G-D-dependent cell adhesion to FBN1. ITGA5:ITGB1 acts as a receptor for fibronectin FN1 and mediates R-G-D-dependent cell adhesion to FN1. ITGA5:ITGB1 is a receptor for IL1B and binding is essential for IL1B signaling. ITGA5:ITGB3 is a receptor for soluble CD40LG and is required for CD40/CD40LG signaling. Plays an important role in myoblast differentiation and fusion during skeletal myogenesis. ITGA9:ITGB1 may play a crucial role in SVEP1/polydom-mediated myoblast cell adhesion. Integrins ITGA9:ITGB1 and ITGA4:ITGB1 repress PRKCA-mediated L-type voltage-gated channel Ca(2+) influx and ROCK-mediated calcium sensitivity in vascular smooth muscle cells via their interaction with SVEP1, thereby inhibit vasocontraction. Interferes with isoform 1 resulting in a dominant negative effect on cell adhesion and migration (in vitro). Isoform 5 displaces isoform 1 in striated muscles. (Microbial infection) Integrin ITGA2:ITGB1 acts as a receptor for Human echoviruses 1 and 8. (Microbial infection) Acts as a receptor for Cytomegalovirus/HHV-5. (Microbial infection) Acts as a receptor for Epstein-Barr virus/HHV-4. (Microbial infection) Integrin ITGA5:ITGB1 acts as a receptor for Human parvovirus B19. (Microbial infection) Integrin ITGA2:ITGB1 acts as a receptor for Human rotavirus. (Microbial infection) Acts as a receptor for Mammalian reovirus. (Microbial infection) In case of HIV-1 infection, integrin ITGA5:ITGB1 binding to extracellular viral Tat protein seems to enhance angiogenesis in Kaposi’s sarcoma lesions. (Microbial infection) Interacts with CotH proteins expressed by fungi of the order mucorales, the causative agent of mucormycosis, which plays an important role in epithelial cell invasion by the fungi. Integrin ITGA3:ITGB1 may act as a receptor for R.delemar CotH7 in alveolar epithelial cells, which may be an early step in pulmonary mucormycosis disease progression. (Microbial infection) May serve as a receptor for adhesin A (nadA) of N.meningitidis. (Microbial infection) Facilitates rabies infection in a fibronectin-dependent manner and participates in rabies virus traffic after internalization.

Subunit / interactions. Heterodimer of an alpha and a beta subunit. Beta-1 associates with either alpha-1, alpha-2, alpha-3, alpha-4, alpha-5, alpha-6, alpha-7, alpha-8, alpha-9, alpha-10, alpha-11 or alpha-V. ITGA6:ITGB1 is found in a complex with CD9; interaction takes place in oocytes and is involved in sperm-egg fusion. Interacts with seprase FAP (seprase); the interaction occurs at the cell surface of invadopodia membrane in a collagen-dependent manner. Binds LGALS3BP and NMRK2, when associated with alpha-7, but not with alpha-5. Interacts with FGR and HCK. Interacts (via the cytoplasmic region) with RAB25 (via the hypervariable C-terminal region). Interacts with RAB21. Interacts with KRT1 in the presence of RACK1 and SRC. Interacts with JAML; integrin alpha-4/beta-1 may regulate leukocyte to endothelial cells adhesion by controlling JAML homodimerization. Interacts with FLNB and RANBP9. Interacts with MYO10. Interacts with DAB2. Interacts with FERMT2; the interaction is inhibited in presence of ITGB1BP1. Interacts with ITGB1BP1 (via C-terminal region); the interaction is a prerequisite for focal adhesion disassembly. Interacts with TLN1; the interaction is prevented by competitive binding of ITGB1BP1. Interacts with ACAP1; required for ITGB1 recycling. Interacts with ASAP3. Interacts with EMP2; the interaction may be direct or indirect and ITGB1 has a heterodimer form. ITGA5:ITGB1 interacts with CCN3. ITGA4:ITGB1 is found in a ternary complex with CX3CR1 and CX3CL1. ITGA5:ITGB1 interacts with FBN1. ITGA5:ITGB1 interacts with IL1B. ITGA4:ITGB1 interacts with MDK; this interaction mediates MDK-induced osteoblast cells migration through PXN phosphorylation. ITGA6:ITGB1 interacts with MDK; this interaction mediates MDK-induced neurite-outgrowth. ITGA5:ITGB1 interacts with ACE2. Interacts with TMEM182 and LAMB1. Interacts with tensin TNS3; TNS3 also interacts with PEAK1, thus acting as an adapter molecule to bridge the association of PEAK1 with ITGB1. Interacts with tensin TNS4; the interaction displaces tensin TNS3 from the ITGB1 cytoplasmic tail and promotes ITGB1 stability. Integrin ITGA9:ITGB1 interacts with SPP1/OPN (via N-terminus). Integrin ITGA9:ITGB1 interacts with TNC/TNFN3 (via the 3rd Fibronectin type-III domain). Integrins ITGA4:ITGB1 and ITGA9:ITGB1 interact with SVEP1 (via Sushi domain 21); thereby inhibit Ca(2+) intracellular signaling and as a result repress vasocontraction. ITGA4:ITGB1 and ITGA5:ITGB1 interacts with SELP. Interacts with CD248. ITGA5:ITGB1 interacts with IGFBP1. ITGA4:ITGB1 interacts with BCAM. Interacts with ADGRG6. Interacts with the C-terminal region of FLNC. Interacts with filamin FLNA isoform 3/VAR-1. Interacts with ACE2. Interacts with alpha-7B in cardiomyocytes of adult heart and alpha-7A and alpha-7B in adult skeletal muscle. Interacts with filamin FLNA isoform 3/VAR-1. (Microbial infection) Integrin ITGA2:ITGB1 interacts with human echoviruses 1 and 8 capsid proteins. (Microbial infection) Interacts with human cytomegalovirus/HHV-5 envelope glycoprotein B/gB. (Microbial infection) Interacts with Epstein-Barr virus/HHV-4 gB protein. (Microbial infection) Integrin ITGA5:ITGB1 interacts with human parvovirus B19 capsid protein. (Microbial infection) Integrin ITGA2:ITGB1 interacts with human rotavirus VP4 protein. (Microbial infection) Interacts with mammalian reovirus capsid proteins. (Microbial infection) Integrin ITGA5:ITGB1 interacts with HIV-1 Tat. (Microbial infection) ITGA5:ITGB1 interacts with SARS coronavirus-2/SARS-CoV-2 spike protein. (Microbial infection) Interacts with R.delemar CotH7 on the surface of alveolar epithelial cells. (Microbial infection) Interacts with N.meningitidis serogroup B adhesin A (nadA). (Microbial infection) Interacts with rabies virus glycoprotein G.

Subcellular location. Cell membrane. Cell projection. Invadopodium membrane. Ruffle membrane. Recycling endosome. Melanosome. Cleavage furrow. Lamellipodium. Cell junction. Focal adhesion Cell membrane. Sarcolemma.

Tissue specificity. Expressed in vascular smooth muscle cells (at protein level). Expressed in placenta (at protein level). Widely expressed, other isoforms are generally coexpressed with a more restricted distribution. Expressed in skin, liver, skeletal muscle, cardiac muscle, placenta, umbilical vein endothelial cells, neuroblastoma cells, lymphoma cells, hepatoma cells and astrocytoma cells. Together with isoform 4, is expressed in muscle, kidney, liver, placenta, cervical epithelium, umbilical vein endothelial cells, fibroblast cells, embryonal kidney cells, platelets and several blood cell lines. Expressed in non-proliferating and differentiated prostate gland epithelial cells and in platelets, on the surface of erythroleukemia cells and in various hematopoietic cell lines. Together with isoform 3, is expressed in muscle, kidney, liver, placenta, cervical epithelium, umbilical vein endothelial cells, fibroblast cells, embryonal kidney cells, platelets and several blood cell lines. Rather than isoform 3, is selectively expressed in peripheral T-cells. Expressed specifically in striated muscle (skeletal and cardiac muscle).

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.

Induction. Induced in alveolar epithelial cells during exposure to the fungus R.delemar, a causative agent of mucormycosis.

Similarity. Belongs to the integrin beta chain family.

Isoforms (5)

UniProt ID	Names	Canonical?
P05556-1	1, Beta-1A	yes
P05556-2	2, Beta-1B
P05556-3	3, Beta-1C
P05556-4	4, Beta-1C-2
P05556-5	5, Beta-1D

RefSeq proteins (3): NP_002202, NP_391988, NP_596867 (=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 (154 total): disulfide bond 28, strand 26, helix 22, mutagenesis site 15, binding site 12, glycosylation site 12, domain 6, turn 6, region of interest 6, modified residue 5, sequence conflict 5, splice variant 4, topological domain 2, signal peptide 1, chain 1, compositionally biased region 1, transmembrane region 1, cross-link 1

Structure

Experimental structures (PDB)

22 structures.

PDB	Method	Resolution (Å)
4WK0	X-RAY DIFFRACTION	1.78
4WJK	X-RAY DIFFRACTION	1.85
3G9W	X-RAY DIFFRACTION	2.17
3T9K	X-RAY DIFFRACTION	2.3
8W30	X-RAY DIFFRACTION	2.45
4WK2	X-RAY DIFFRACTION	2.5
4WK4	X-RAY DIFFRACTION	2.5
9NAB	ELECTRON MICROSCOPY	2.54
9B9J	ELECTRON MICROSCOPY	2.6
9P6S	ELECTRON MICROSCOPY	2.61
9B9K	ELECTRON MICROSCOPY	2.7
7CEB	X-RAY DIFFRACTION	2.89
3VI3	X-RAY DIFFRACTION	2.9
3VI4	X-RAY DIFFRACTION	2.9
9DIA	ELECTRON MICROSCOPY	2.97
4DX9	X-RAY DIFFRACTION	2.99
7NWL	ELECTRON MICROSCOPY	3.1
9CKV	ELECTRON MICROSCOPY	3.19
9EF2	ELECTRON MICROSCOPY	3.36
7CEC	ELECTRON MICROSCOPY	3.9
7NXD	ELECTRON MICROSCOPY	4.6
8RPQ	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P05556-F1	86.02	0.50

Antibody-complex structures (SAbDab): 8 — 3VI3, 3VI4, 7CEB, 7CEC, 7NWL, 9B9J, 9B9K, 9NAB

Functional residue map

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

Ligand- & substrate-binding residues (12): 152 (in midas binding site); 154 (in admidas binding site); 154 (in midas binding site); 157 (in admidas binding site); 158 (in admidas binding site); 189 (in limbs binding site); 244 (in limbs binding site); 246 (in limbs binding site); 248 (in limbs binding site); 249 (in limbs binding site); 249 (in midas binding site); 362 (in admidas binding site)

Post-translational modifications (6): 777, 783, 785, 789, 794, 794

Disulfide bonds (28): 27–45, 35–464, 38–64, 48–75, 207–213, 261–301, 401–415, 435–462, 466–486, 477–489, 491–500, 502–533, 516–531, 525–536, 538–553, 555–576, 560–574, 568–579, 581–590, 592–615 …

Glycosylation sites (12): 50, 94, 97, 212, 269, 363, 406, 417, 481, 520, 584, 669

Mutagenesis-validated functional residues (15):

Position	Phenotype
760–761	no effect on interaction with acap1.
762–767	strongly reduces interaction with acap1 and ability to recycle; does not affect heterodimerization with itga5.
762–763	slightly reduces interaction with acap1.
765	reduces interaction with acap1.
766–767	slightly reduces interaction with acap1.
768–769	no effect on interaction with acap1.
778	loss of beta-1a interaction with flna and flnb.
783	no effect on cell surface location but impairs interaction with tns3 and peak1.
786–791	does not interact with itgb1bp1.
786	loss of beta-1a interaction with flna and flnb.
787	reduces interaction with itgb1bp1, but not with fermt2 or tln1. inhibits fibronectin deposition and mineralized bone nod
788	strongly reduces itgb1bp1 binding; when associated with d-790.
790	strongly reduces itgb1bp1 binding; when associated with d-788.
792	strongly reduces itgb1bp1 binding; when associated with a-795.
795	no effect on cell surface location but impairs interaction with tns3 and peak1. strongly reduces itgb1bp1 binding; when

Function

Pathways and Gene Ontology

Reactome pathways

72 pathways

ID	Pathway
R-HSA-1566948	Elastic fibre formation
R-HSA-1566977	Fibronectin matrix formation
R-HSA-198933	Immunoregulatory interactions between a Lymphoid and a non-Lymphoid cell
R-HSA-202733	Cell surface interactions at the vascular wall
R-HSA-210991	Basigin interactions
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-3000157	Laminin interactions
R-HSA-3000170	Syndecan interactions
R-HSA-3000178	ECM proteoglycans
R-HSA-416700	Other semaphorin interactions
R-HSA-445144	Signal transduction by L1
R-HSA-446343	Localization of the PINCH-ILK-PARVIN complex to focal adhesions
R-HSA-447041	CHL1 interactions
R-HSA-5663220	RHO GTPases Activate Formins
R-HSA-6785807	Interleukin-4 and Interleukin-13 signaling
R-HSA-75892	Platelet Adhesion to exposed collagen
R-HSA-8874081	MET activates PTK2 signaling
R-HSA-8875513	MET interacts with TNS proteins
R-HSA-9013149	RAC1 GTPase cycle
R-HSA-9013404	RAC2 GTPase cycle
R-HSA-9013408	RHOG GTPase cycle
R-HSA-9013423	RAC3 GTPase cycle
R-HSA-9609690	HCMV Early Events
R-HSA-9634597	GPER1 signaling
R-HSA-9679191	Potential therapeutics for SARS
R-HSA-9725554	Differentiation of Keratinocytes in Interfollicular Epidermis in Mammalian Skin
R-HSA-9830674	Formation of the ureteric bud
R-HSA-9856532	Mechanical load activates signaling by PIEZO1 and integrins in osteocytes

MSigDB gene sets: 898 (showing top): GOBP_CELLULAR_RESPONSE_TO_LIPOPROTEIN_PARTICLE_STIMULUS, GOBP_MORPHOGENESIS_OF_AN_EPITHELIUM, GOBP_DENDRITE_DEVELOPMENT, TGGTGCT_MIR29A_MIR29B_MIR29C, GOBP_ESTABLISHMENT_OF_SPINDLE_ORIENTATION, BIOCARTA_PTEN_PATHWAY, GOBP_HINDBRAIN_DEVELOPMENT, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, RODRIGUES_THYROID_CARCINOMA_ANAPLASTIC_UP, GOBP_REGULATION_OF_CELLULAR_RESPONSE_TO_GROWTH_FACTOR_STIMULUS, GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, GOBP_EPITHELIUM_DEVELOPMENT, GOBP_ACTIN_FILAMENT_BUNDLE_ORGANIZATION, GOBP_MUSCLE_TISSUE_DEVELOPMENT, GOBP_COGNITION

GO Biological Process (77): G1/S transition of mitotic cell cycle (GO:0000082), establishment of mitotic spindle orientation (GO:0000132), angiogenesis (GO:0001525), in utero embryonic development (GO:0001701), cell migration involved in sprouting angiogenesis (GO:0002042), positive regulation of neuroblast proliferation (GO:0002052), phagocytosis (GO:0006909), autophagy (GO:0006914), cellular defense response (GO:0006968), cell adhesion (GO:0007155), homophilic cell-cell adhesion (GO:0007156), leukocyte cell-cell adhesion (GO:0007159), cell-matrix adhesion (GO:0007160), calcium-independent cell-matrix adhesion (GO:0007161), integrin-mediated signaling pathway (GO:0007229), neuroblast proliferation (GO:0007405), muscle organ development (GO:0007517), myoblast fusion (GO:0007520), primordial germ cell migration (GO:0008354), visual learning (GO:0008542), negative regulation of autophagy (GO:0010507), regulation of collagen catabolic process (GO:0010710), positive regulation of fibroblast migration (GO:0010763), response to muscle activity (GO:0014850), cell migration (GO:0016477), formation of radial glial scaffolds (GO:0021943), central nervous system neuron differentiation (GO:0021953), CD40 signaling pathway (GO:0023035), cell projection organization (GO:0030030), lamellipodium assembly (GO:0030032), B cell differentiation (GO:0030183), extracellular matrix organization (GO:0030198), positive regulation of cell migration (GO:0030335), cell-substrate adhesion (GO:0031589), receptor internalization (GO:0031623), cell adhesion mediated by integrin (GO:0033627), cell-cell adhesion mediated by integrin (GO:0033631), heterotypic cell-cell adhesion (GO:0034113), negative regulation of Rho protein signal transduction (GO:0035024), wound healing, spreading of epidermal cells (GO:0035313)

GO Molecular Function (22): magnesium ion binding (GO:0000287), virus receptor activity (GO:0001618), fibronectin binding (GO:0001968), protease binding (GO:0002020), actin binding (GO:0003779), cell adhesion receptor activity (GO:0004895), integrin binding (GO:0005178), calcium ion binding (GO:0005509), coreceptor activity (GO:0015026), protein kinase binding (GO:0019901), laminin binding (GO:0043236), protein-containing complex binding (GO:0044877), cadherin binding (GO:0045296), protein heterodimerization activity (GO:0046982), cell adhesion molecule binding (GO:0050839), collagen binding involved in cell-matrix adhesion (GO:0098639), integrin binding involved in cell-matrix adhesion (GO:0098640), protein tyrosine kinase binding (GO:1990782), protein binding (GO:0005515), C-X3-C chemokine binding (GO:0019960), signaling receptor activity (GO:0038023), metal ion binding (GO:0046872)

GO Cellular Component (48): ruffle (GO:0001726), cytoplasm (GO:0005737), plasma membrane (GO:0005886), focal adhesion (GO:0005925), integrin complex (GO:0008305), external side of plasma membrane (GO:0009897), cell surface (GO:0009986), endosome membrane (GO:0010008), intercalated disc (GO:0014704), membrane (GO:0016020), lamellipodium (GO:0030027), filopodium (GO:0030175), neuromuscular junction (GO:0031594), cleavage furrow (GO:0032154), ruffle membrane (GO:0032587), integrin alpha1-beta1 complex (GO:0034665), integrin alpha2-beta1 complex (GO:0034666), integrin alpha3-beta1 complex (GO:0034667), integrin alpha4-beta1 complex (GO:0034668), integrin alpha5-beta1 complex (GO:0034674), integrin alpha6-beta1 complex (GO:0034675), integrin alpha7-beta1 complex (GO:0034677), integrin alpha8-beta1 complex (GO:0034678), integrin alpha9-beta1 complex (GO:0034679), integrin alpha10-beta1 complex (GO:0034680), integrin alpha11-beta1 complex (GO:0034681), integrin alphav-beta1 complex (GO:0034682), myelin sheath abaxonal region (GO:0035748), sarcolemma (GO:0042383), melanosome (GO:0042470), dendritic spine (GO:0043197), signaling receptor complex (GO:0043235), membrane raft (GO:0045121), synapse (GO:0045202), perinuclear region of cytoplasm (GO:0048471), recycling endosome (GO:0055037), extracellular exosome (GO:0070062), synaptic membrane (GO:0097060), glial cell projection (GO:0097386), Schaffer collateral - CA1 synapse (GO:0098685)

Reactome top-level categories

Rollup of top-13 pathways:

Category	Pathways
Extracellular matrix organization	5
Hemostasis	2
L1CAM interactions	2
MET promotes cell motility	2
Adaptive Immune System	1
Cell surface interactions at the vascular wall	1
Elastic fibre formation	1
Signaling by TGF-beta Receptor Complex	1
Non-integrin membrane-ECM interactions	1
Semaphorin interactions	1
Cell-extracellular matrix interactions	1
RHO GTPase Effectors	1
Signaling by Interleukins	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
integrin complex	5
cell-matrix adhesion	3
protein binding	3
cellular anatomical structure	3
mitotic cell cycle	2
cell-cell adhesion	2
metal ion binding	2
signaling receptor activity	2
cell adhesion molecule binding	2
binding	2
cell-matrix adhesion mediator activity	2
cell leading edge	2
plasma membrane bounded cell projection	2
mitotic cell cycle phase transition	1
cell cycle G1/S phase transition	1
establishment of mitotic spindle localization	1
establishment of spindle orientation	1
blood vessel morphogenesis	1
anatomical structure formation involved in morphogenesis	1
chordate embryonic development	1
sprouting angiogenesis	1
blood vessel endothelial cell migration	1
neuroblast proliferation	1
positive regulation of neurogenesis	1
regulation of neuroblast proliferation	1
positive regulation of neural precursor cell proliferation	1
endocytosis	1
catabolic process	1
transmembrane transport	1
process utilizing autophagic mechanism	1
defense response	1
cellular process	1
cell-substrate adhesion	1
cell surface receptor signaling pathway	1
generation of neurons	1
neural precursor cell proliferation	1
animal organ development	1
muscle structure development	1
syncytium formation by cell-cell fusion	1
myotube differentiation	1

Protein interactions and networks

STRING

4452 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
ITGB1	ITGA5	P08648	999
ITGB1	FN1	P02751	998
ITGB1	ITGA4	P13612	998
ITGB1	ITGA2	P17301	997
ITGB1	ITGA6	P23229	997
ITGB1	ITGA1	P56199	996
ITGB1	VCAM1	P19320	996
ITGB1	ITGA3	P26006	995
ITGB1	ITGAV	P06756	994
ITGB1	TLN1	Q9Y490	994
ITGB1	ILK	P57043	993
ITGB1	CD63	P08962	992
ITGB1	CD81	P18582	987
ITGB1	TLN2	Q9Y4G6	979
ITGB1	PXN	P49023	967
ITGB1	DPP4	P27487	967

IntAct

293 interactions, top by confidence:

A	B	Type	Score
ITGB1	ITGA5	psi-mi:“MI:0914”(association)	0.910
ITGB1	ITGA5	psi-mi:“MI:0915”(physical association)	0.910
ITGA5	ITGB1	psi-mi:“MI:0915”(physical association)	0.910
TSPAN15	ADAM10	psi-mi:“MI:0914”(association)	0.840
ITGA5	FN1	psi-mi:“MI:0407”(direct interaction)	0.840
TSPAN5	ADAM10	psi-mi:“MI:0914”(association)	0.800
FN1	ITGB1	psi-mi:“MI:0915”(physical association)	0.750
FN1	ITGB3	psi-mi:“MI:0915”(physical association)	0.750
CD9	ADAM10	psi-mi:“MI:0914”(association)	0.750
CFTR	ESYT2	psi-mi:“MI:2364”(proximity)	0.710
CFTR	ESYT2	psi-mi:“MI:0914”(association)	0.710
CD9	ITGB1	psi-mi:“MI:0914”(association)	0.690
ITGA4	ITGB1	psi-mi:“MI:0915”(physical association)	0.680
ITGA2	ITGB1	psi-mi:“MI:0915”(physical association)	0.680
ITGB1	ADAM17	psi-mi:“MI:0915”(physical association)	0.610
CFTR	HAX1	psi-mi:“MI:0914”(association)	0.610
CD81	EGFR	psi-mi:“MI:0914”(association)	0.600
Tln1	ITGB1	psi-mi:“MI:0407”(direct interaction)	0.570
CANX	PGRMC1	psi-mi:“MI:0914”(association)	0.570
ITGB1	ACE2	psi-mi:“MI:0915”(physical association)	0.570

BioGRID (580): ITGB1 (Two-hybrid), SEL1L (Affinity Capture-Western), ACAP1 (Affinity Capture-Western), ACAP1 (Reconstituted Complex), ITGB1 (Affinity Capture-MS), ITGB1 (Affinity Capture-MS), ITGB1 (Affinity Capture-MS), ITGB1 (Affinity Capture-MS), ITGB1 (Affinity Capture-MS), ITGB1 (Affinity Capture-RNA), ITGB1 (Co-fractionation), ITGB1 (Co-fractionation), ITGB1 (Co-fractionation), ITGB1 (Affinity Capture-MS), ITGB1 (Reconstituted Complex)

ESM2 similar proteins: A0A8M9PFP2, A2A863, A5Z1X6, B0FYY4, B2RXS4, O13146, O15031, O73875, P05107, P05556, P07228, P09055, P09958, P11584, P11835, P12606, P12607, P16144, P18563, P18564, P23188, P23229, P23377, P26007, P26010, P26011, P29317, P32592, P49134, P53712, P53713, P53714, P97278, Q13753, Q1KL86, Q1RPR6, Q27874, Q28193, Q29052, Q2VJ42

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

48 interactions.

A	Effect	B	Mechanism
ITGB1	“form complex”	“a7/b1 integrin”	binding
TWIST2	“up-regulates quantity by expression”	ITGB1	“transcriptional regulation”
TWIST1	“up-regulates quantity by expression”	ITGB1	“transcriptional regulation”
ITGB1BP1	“down-regulates activity”	ITGB1	binding
DOK1	“down-regulates activity”	ITGB1	binding
ITGB1	“up-regulates activity”	PTK2
Kindlin	“up-regulates activity”	ITGB1	binding
HOXD1	“up-regulates quantity by expression”	ITGB1	“transcriptional regulation”
PCDHA2	“up-regulates activity”	ITGB1	binding
PCDHA9	“up-regulates activity”	ITGB1	binding
PCDHA1	“up-regulates activity”	ITGB1	binding
PCDHA10	“up-regulates activity”	ITGB1	binding
PCDHA4	“up-regulates activity”	ITGB1	binding
PCDHA6	“up-regulates activity”	ITGB1	binding
PCDHA7	“up-regulates activity”	ITGB1	binding
PCDHA3	“up-regulates activity”	ITGB1	binding
PCDHA5	“up-regulates activity”	ITGB1	binding
PCDHA11	“up-regulates activity”	ITGB1	binding
PCDHA8	“up-regulates activity”	ITGB1	binding
PCDHA13	“up-regulates activity”	ITGB1	binding
PCDHA12	“up-regulates activity”	ITGB1	binding
PCDHAC1	“up-regulates activity”	ITGB1	binding
PCDHAC2	“up-regulates activity”	ITGB1	binding
PCDH10	“up-regulates activity”	ITGB1	binding
PCDH9	“up-regulates activity”	ITGB1	binding
Protocadherin_beta	“up-regulates activity”	ITGB1	binding
PTP4A3	“down-regulates activity”	ITGB1	dephosphorylation
KCNH2	“up-regulates activity”	ITGB1	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 149 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Erythropoietin activates RAS	5	35.9×	3e-05
Constitutive Signaling by EGFRvIII	5	33.7×	4e-05
Signaling by ERBB2 ECD mutants	5	31.7×	4e-05
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants	5	26.9×	6e-05
Signal transduction by L1	5	24.5×	7e-05
Signaling by phosphorylated juxtamembrane, extracellular and kinase domain KIT mutants	5	24.5×	7e-05
Syndecan interactions	5	19.9×	2e-04
Signaling by ERBB2 KD Mutants	5	19.9×	2e-04

GO biological processes:

GO term	Partners	Fold	FDR
cell-substrate adhesion	5	29.9×	7e-05
cell adhesion mediated by integrin	5	26.3×	1e-04
heterotypic cell-cell adhesion	5	22.7×	2e-04
integrin-mediated signaling pathway	15	18.8×	3e-12
substrate adhesion-dependent cell spreading	7	18.8×	2e-05
symbiont entry into host cell	5	15.7×	1e-03
cell-matrix adhesion	11	14.1×	1e-07
positive regulation of smooth muscle cell proliferation	5	12.9×	2e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	65
Likely benign	6
Benign	4

Top pathogenic / likely-pathogenic (0)

SpliceAI

2861 predictions. Top by Δscore:

Variant	Effect	Δscore
10:32908362:ACTT:A	donor_loss	1.0000
10:32908363:CTT:C	donor_loss	1.0000
10:32908366:A:AC	donor_gain	1.0000
10:32908366:ACCG:A	donor_loss	1.0000
10:32908367:C:CC	donor_gain	1.0000
10:32908530:ACACT:A	acceptor_gain	1.0000
10:32908531:CACT:C	acceptor_gain	1.0000
10:32908531:CACTC:C	acceptor_gain	1.0000
10:32908533:CT:C	acceptor_gain	1.0000
10:32908535:C:CA	acceptor_loss	1.0000
10:32908535:C:CC	acceptor_gain	1.0000
10:32911442:ACTT:A	donor_loss	1.0000
10:32911443:CTT:C	donor_loss	1.0000
10:32911444:TTA:T	donor_loss	1.0000
10:32911445:TA:T	donor_loss	1.0000
10:32911446:A:AC	donor_gain	1.0000
10:32911447:C:A	donor_loss	1.0000
10:32911447:C:CG	donor_gain	1.0000
10:32911447:CT:C	donor_gain	1.0000
10:32911447:CTT:C	donor_gain	1.0000
10:32911447:CTTA:C	donor_gain	1.0000
10:32911447:CTTAT:C	donor_gain	1.0000
10:32922248:TGTAC:T	donor_loss	1.0000
10:32922249:GTACT:G	donor_loss	1.0000
10:32922250:TACT:T	donor_loss	1.0000
10:32922251:ACTCA:A	donor_loss	1.0000
10:32922252:CT:C	donor_loss	1.0000
10:32922253:T:TA	donor_loss	1.0000
10:32922254:CA:C	donor_loss	1.0000
10:32922255:A:AC	donor_gain	1.0000

AlphaMissense

5339 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
10:32901627:A:C	N780K	1.000
10:32901627:A:T	N780K	1.000
10:32908374:C:A	W775C	1.000
10:32908374:C:G	W775C	1.000
10:32908376:A:G	W775R	1.000
10:32908376:A:T	W775R	1.000
10:32908401:A:C	F766L	1.000
10:32908401:A:T	F766L	1.000
10:32908402:A:C	F766C	1.000
10:32908402:A:G	F766S	1.000
10:32908403:A:G	F766L	1.000
10:32908423:T:A	D759V	1.000
10:32908423:T:G	D759A	1.000
10:32908424:C:G	D759H	1.000
10:32908468:C:T	G744D	1.000
10:32908469:C:G	G744R	1.000
10:32908483:C:T	G739E	1.000
10:32908484:C:G	G739R	1.000
10:32908484:C:T	G739R	1.000
10:32910315:C:G	C691S	1.000
10:32910316:A:T	C691S	1.000
10:32911559:C:G	C607S	1.000
10:32911560:A:T	C607S	1.000
10:32911610:C:G	C590S	1.000
10:32911611:A:T	C590S	1.000
10:32911658:C:G	C574S	1.000
10:32911659:A:T	C574S	1.000
10:32911915:C:G	C560S	1.000
10:32911916:A:T	C560S	1.000
10:32911936:C:G	C553S	1.000

dbSNP variants (sampled 300 via entrez): RS1000047047 (10:32947313 A>G), RS1000100800 (10:32939764 G>A), RS1000132030 (10:32913428 C>A,G), RS1000168827 (10:32930347 A>T), RS1000200782 (10:32912515 G>A), RS1000222337 (10:32902394 A>G), RS1000390094 (10:32934654 G>A,C), RS1000450999 (10:32900779 T>C), RS1000456127 (10:32931463 G>A,T), RS1000505816 (10:32903295 T>G), RS1000551523 (10:32941180 A>G), RS1000609176 (10:32935797 G>A), RS1000619868 (10:32940037 G>A), RS1000746765 (10:32936098 A>G), RS1000798133 (10:32928964 T>C)

Disease associations

OMIM: gene MIM:135630 | disease phenotypes:

GenCC curated gene-disease

Mondo (3): neural tube defect (MONDO:0018075), esophageal atresia (MONDO:0001044), pyloric stenosis (MONDO:0001561)

Orphanet (2): Neural tube defect (Orphanet:3388), Spina bifida and other spinal dysraphisms (Orphanet:823)

HPO phenotypes

2 total (2 of 2 shown, HPO-id order):

HPO	Term
HP:0002032	Esophageal atresia
HP:0002021	Pyloric stenosis

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST000779_6	Depression (quantitative trait)	5.000000e-06
GCST002699_2	Suicide in bipolar disorder	2.000000e-06

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0006882	suicide behaviour measurement

MeSH disease descriptors (4)

Descriptor	Name	Tree numbers
D004933	Esophageal Atresia	C06.198.330; C06.405.117.260; C16.131.314.330
D017219	Gastric Outlet Obstruction	C06.405.748.340
D009436	Neural Tube Defects	C10.500.680; C16.131.666.680
D011707	Pyloric Stenosis	C06.405.748.340.690

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (11): CHEMBL1905 (SINGLE PROTEIN), CHEMBL1907599 (PROTEIN COMPLEX), CHEMBL2095226 (PROTEIN COMPLEX), CHEMBL2111407 (PROTEIN COMPLEX), CHEMBL2111425 (PROTEIN COMPLEX GROUP), CHEMBL3137268 (PROTEIN COMPLEX), CHEMBL3137278 (PROTEIN COMPLEX), CHEMBL3430895 (PROTEIN COMPLEX), CHEMBL3885596 (PROTEIN COMPLEX), CHEMBL3885597 (PROTEIN COMPLEX)

Molecules with ChEMBL bioactivity

4 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 10,236 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL429876	CILENGITIDE	3	10,123
CHEMBL3319236	GLPG-0187	1	96
CHEMBL4241824	GSK-3008348 FREE BASE	1	8
CHEMBL4246089	GSK-3008348	1	9

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

PharmGKB variants

2 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs1187075	ITGB1		0.00	0
rs2230395	ITGB1		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: catalytic receptor — Integrins

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

Ligand	Action	Affinity	Parameter
compound 7 [PMID: 31381331]	Inhibition	7.7	pKi

Binding affinities (BindingDB)

392 measured of 431 human assays (432 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(5S)-5-[(1-carbamoylcyclohexyl)carbamoyl]-5-[(2S)-2-[1-(4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetamido]-6-[(2E)-3-(pyridin-3-yl)prop-2-enamido]hexanamido]pentanoic acid	IC50	0.0372 nM
(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
(5S)-5-[(2S)-2-{1-[4-(1H-1,3-benzodiazol-2-ylamino)phenyl]acetamido}-6-[(2E)-3-(pyridin-3-yl)prop-2-enamido]hexanamido]-5-[(1-carbamoylcyclohexyl)carbamoyl]pentanoic acid	IC50	0.305 nM
3-(4-{[3-(3-methoxy-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)-2-oxo-1,2-dihydropyridin-1-yl]methyl}phenyl)propanoic acid	KI	0.5 nM
(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
4-{[(2S,4S)-1-[2-(3-chloro-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetyl]-4-fluoropyrrolidin-2-yl]methoxy}benzoic acid	IC50	0.51 nM
(3S)-3-{[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]carbamoyl}-3-[(2S)-2-[1-(4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetamido]hexanamido]propanoic acid	IC50	0.6 nM
(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
CHEMBL4794201	IC50	0.7 nM
(S)-2-[(1-Benzyl-5-oxo-pyrrolidine-2-carbonyl)-amino]-3-[4-(4-fluoro-2-trifluoromethyl-benzoylamino)-phenyl]-propionic acid	IC50	0.75 nM
4-{[(2S,4S)-1-[2-(3-bromo-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetyl]-4-fluoropyrrolidin-2-yl]methoxy}benzoic acid	IC50	0.78 nM
(3R)-3-(4-{[3-(3-methoxy-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)-2-oxo-1,2-dihydropyridin-1-yl]methyl}phenyl)butanoic acid	KI	0.79 nM
(3R)-3-(4-{[3-(2-chloro-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)-2-oxo-1,2-dihydropyridin-1-yl]methyl}phenyl)butanoic acid	KI	0.79 nM
(3R)-3-{4-[2-(3-methoxy-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetamido]phenyl}butanoic acid	KI	0.79 nM
(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
4-{[(2S,4S)-1-[2-(4-{[(2-chlorophenyl)carbamoyl]amino}-3-methoxyphenyl)acetyl]-4-fluoropyrrolidin-2-yl]methoxy}benzoic acid	IC50	0.87 nM
2-(1-{[(2S,4R)-4-(benzyloxy)-1-[2-(3-methoxy-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetyl]pyrrolidin-2-yl]carbonyl}piperidin-4-yl)acetic acid	IC50	0.94 nM
2-(4-{[(2S,3S)-3-hydroxy-1-[2-(3-methoxy-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetyl]pyrrolidin-2-yl]carbonyl}piperazin-1-yl)acetic acid	IC50	0.96 nM
(2S)-3-{4-[(3,5-dichloropyridine-4-)amido]phenyl}-2-{[(3S)-2-(3-phenylpropanoyl)-2-azabicyclo[2.2.2]octan-3-yl]formamido}propanoic acid	IC50	1 nM
(3R)-3-(4-{[3-(4-{[(2-methylphenyl)carbamoyl]amino}phenyl)-2-oxo-1,2-dihydropyridin-1-yl]methyl}phenyl)butanoic acid	KI	1 nM
(3S)-3-(4-{[3-(3-methoxy-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)-2-oxo-1,2-dihydropyridin-1-yl]methyl}phenyl)butanoic acid	KI	1 nM
(3R)-3-(4-{[3-(3-chloro-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)-2-oxo-1,2-dihydropyridin-1-yl]methyl}phenyl)butanoic acid	KI	1 nM
(3R)-3-(4-{[3-(3-methyl-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)-2-oxo-1,2-dihydropyridin-1-yl]methyl}phenyl)butanoic acid	KI	1 nM
2-(4-{[(2S,4S)-4-fluoro-1-[2-(3-methoxy-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetyl]pyrrolidin-2-yl]carbonyl}piperazin-1-yl)acetic acid	IC50	1 nM
2-(4-{[(2S)-1-[2-(3-methoxy-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetyl]-octahydro-1H-indol-2-yl]carbonyl}piperazin-1-yl)acetic acid	IC50	1 nM
(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
CHEMBL4741135	IC50	1 nM
2-(1-{[(2S,4R)-4-methoxy-1-[2-(3-methoxy-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetyl]pyrrolidin-2-yl]carbonyl}piperidin-4-yl)acetic acid	IC50	1.1 nM
2-(1-{[(2S,4R)-4-hydroxy-1-[2-(3-methoxy-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetyl]pyrrolidin-2-yl]carbonyl}piperidin-4-yl)acetic acid	IC50	1.1 nM
2-(4-{[(2S,4S)-4-chloro-1-[2-(3-methoxy-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetyl]pyrrolidin-2-yl]carbonyl}piperazin-1-yl)acetic acid	IC50	1.1 nM
4-{[(2S,4S)-4-fluoro-1-[2-(3-methoxy-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetyl]pyrrolidin-2-yl]methoxy}benzoic acid	IC50	1.2 nM
2-(4-{[(2S,4S)-1-[2-(3-methoxy-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetyl]-4-phenoxypyrrolidin-2-yl]carbonyl}piperazin-1-yl)acetic acid	IC50	1.2 nM
4-{[(2S,4S)-1-[2-(3-chloro-4-{[(2-chlorophenyl)carbamoyl]amino}phenyl)acetyl]-4-fluoropyrrolidin-2-yl]methoxy}benzoic acid	IC50	1.3 nM
4-{[(2S,4S)-1-[2-(3-bromo-4-{[(2-chlorophenyl)carbamoyl]amino}phenyl)acetyl]-4-fluoropyrrolidin-2-yl]methoxy}benzoic acid	IC50	1.3 nM
2-(4-{[(2S,3S)-3-(benzyloxy)-1-[2-(3-methoxy-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetyl]pyrrolidin-2-yl]carbonyl}piperazin-1-yl)acetic acid	IC50	1.3 nM
(3S)-3-{[(2S,3S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]carbamoyl}-3-[(2S)-2-[1-(4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetamido]hexanamido]propanoic acid	IC50	1.4 nM
(3S)-3-{[(2S,3S)-1-[(2S)-2-carbamoylpiperidin-1-yl]-3-methyl-1-oxopentan-2-yl]carbamoyl}-3-[(2S)-2-[1-(4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetamido]hexanamido]propanoic acid	IC50	1.4 nM
4-{[(2S,4S)-1-[2-(3-bromo-4-{[(2-bromophenyl)carbamoyl]amino}phenyl)acetyl]-4-fluoropyrrolidin-2-yl]methoxy}benzoic acid	IC50	1.4 nM
2-(4-{[(2S,3R,4S)-3,4-dihydroxy-1-[2-(3-methoxy-4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetyl]pyrrolidin-2-yl]carbonyl}piperazin-1-yl)acetic acid	IC50	1.4 nM

ChEMBL bioactivities

2795 potent at pChembl≥5 of 2909 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.70	IC50	0.01995	nM	CHEMBL3962660
10.70	IC50	0.02	nM	CHEMBL3962660
10.70	IC50	0.02	nM	CHEMBL569442
10.66	IC50	0.022	nM	CHEMBL1241140
10.52	IC50	0.03	nM	CHEMBL296804
10.52	IC50	0.03	nM	CHEMBL566154
10.43	IC50	0.0372	nM	CHEMBL395150
10.43	IC50	0.037	nM	CHEMBL447509
10.30	IC50	0.05	nM	CHEMBL2110195
10.30	IC50	0.05	nM	CHEMBL69035
10.28	IC50	0.0525	nM	CHEMBL505769
10.22	IC50	0.06	nM	CHEMBL3893700
10.20	IC50	0.0631	nM	CHEMBL3893700
10.15	IC50	0.07	nM	CHEMBL309823
10.15	IC50	0.07	nM	CHEMBL4798264
10.15	IC50	0.07	nM	CHEMBL566154
10.15	IC50	0.07	nM	CHEMBL296804
10.15	IC50	0.07	nM	CHEMBL1829034
10.15	IC50	0.07	nM	CHEMBL355240
10.10	IC50	0.08	nM	CHEMBL76119
10.10	IC50	0.08	nM	CHEMBL56511
10.10	IC50	0.08	nM	CHEMBL293807
10.10	IC50	0.08	nM	CHEMBL56822
10.05	IC50	0.09	nM	CHEMBL91402
10.05	IC50	0.09	nM	CHEMBL91737
10.05	IC50	0.09	nM	CHEMBL298835
10.05	IC50	0.09	nM	CHEMBL56511
10.05	IC50	0.09	nM	CHEMBL292619
10.05	IC50	0.09	nM	CHEMBL171389
10.00	IC50	0.1	nM	CHEMBL430931
10.00	IC50	0.1	nM	CHEMBL330687
10.00	IC50	0.1	nM	CHEMBL423683
10.00	IC50	0.1	nM	CHEMBL183768
10.00	IC50	0.1	nM	CHEMBL182181
10.00	IC50	0.1	nM	CHEMBL338417
10.00	IC50	0.1	nM	CHEMBL420936
10.00	IC50	0.1	nM	CHEMBL569443
10.00	IC50	0.1	nM	CHEMBL565693
10.00	IC50	0.1	nM	CHEMBL79984
10.00	IC50	0.1	nM	CHEMBL82938
10.00	IC50	0.1	nM	CHEMBL298835
10.00	IC50	0.1	nM	CHEMBL56822
10.00	IC50	0.1	nM	CHEMBL292619
10.00	IC50	0.1	nM	CHEMBL296804
10.00	IC50	0.1	nM	CHEMBL56520
10.00	IC50	0.1	nM	CHEMBL352778
10.00	IC50	0.1	nM	CHEMBL29018
9.96	IC50	0.11	nM	CHEMBL91877
9.96	IC50	0.11	nM	CHEMBL305408
9.96	IC50	0.11	nM	CHEMBL569263

PubChem BioAssay actives

2898 with measured affinity, of 3624 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
(2S)-2-[[(2S)-1-(benzenesulfonyl)pyrrolidine-2-carbonyl]amino]-3-[4-[4-(diaminomethylideneamino)butanoylamino]phenyl]propanoic acid	1324385: Inhibition of integrin alphaVbeta1 (unknown origin)-mediated CHO cell adhesion to fibronectin preincubated for 15 to 30 mins followed by 60 min incubation for adhesion by crystal violet staining based cell adhesion assay	ic50	<0.0001	uM
(2S)-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonylpyrrolidine-2-carbonyl]amino]-3-[4-[(3,5-dichloropyridine-4-carbonyl)amino]phenyl]propanoic acid	241468: Inhibition of VLA-4 receptor of Jurkat cells in BURJ assay	ic50	<0.0001	uM
(2S)-2-[[(2S,4R)-1-(3-cyanophenyl)sulfonyl-4-(3,3-difluoropiperidin-1-yl)pyrrolidine-2-carbonyl]amino]-3-[4-[(3,5-dichloropyridine-4-carbonyl)amino]phenyl]propanoic acid	448164: Displacement of [35S]-labeled ligand from VLA4 in human Jurkat cells washed with buffer containing activating Mn2+ by competitive binding assay	ic50	<0.0001	uM
(5R)-6-[(1-carbamoylcyclohexyl)amino]-5-[[(2R)-2-[[4-[(2-methylphenyl)carbamoylamino]benzoyl]amino]-6-[[(E)-3-pyridin-3-ylprop-2-enoyl]amino]hexanoyl]amino]-6-oxohexanoic acid	303242: Inhibition of integrin alpha4beta1 receptor-mediated human Molt-4 cell adhesion to CS1 peptide	ic50	<0.0001	uM
(2S)-2-[[(2S,4R)-1-(3-cyanophenyl)sulfonyl-4-[cyclobutyl(2,2,2-trifluoroethyl)amino]pyrrolidine-2-carbonyl]amino]-3-[4-[(3,5-dichloropyridine-4-carbonyl)amino]phenyl]propanoic acid	448685: Displacement of [35S]-labeled ligand from VLA4 in human Jurkat cells washed with buffer containing non activating Ca2+ and Mg2+ by competitive binding assay	ic50	<0.0001	uM
(5S)-6-[[(2R)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[[(2S)-2-[[2-[4-[(2-methylphenyl)carbamoylamino]phenyl]acetyl]amino]-6-[[(E)-3-pyridin-3-ylprop-2-enoyl]amino]hexanoyl]amino]-6-oxohexanoic acid	513088: Inhibition of Integrin alpha-4-beta-1-mediated adhesion in human jurkat cells	ic50	<0.0001	uM
(5S)-6-[(1-carbamoylcyclohexyl)amino]-5-[[(2S)-2-[[2-[4-[(2-methylphenyl)carbamoylamino]phenyl]acetyl]amino]-6-[[(E)-3-pyridin-3-ylprop-2-enoyl]amino]hexanoyl]amino]-6-oxohexanoic acid	1797818: Competitive Cell Adhesion Assay from Article 10.1021/jm070790o: “Highly Potent, Water Soluble Benzimidazole Antagonist for Activated alpha(4)beta(1) Integrin.”	ic50	<0.0001	uM
(2S)-3-[4-[(2,6-dichlorobenzoyl)amino]phenyl]-2-[[1-[2-(methylcarbamoylamino)ethyl]cyclopentanecarbonyl]amino]propanoic acid	217051: Inhibitory binding concentration determined against VCAM/VLA-4 in ELISA	ic50	0.0001	uM
(2S)-3-[4-[(2,6-dichlorobenzoyl)amino]phenyl]-2-[[1-(4-methylsulfonylbutyl)cyclobutanecarbonyl]amino]propanoic acid	216088: Inhibition of Very late antigen 4/vascular cell adhesion molecule 1 interaction in ELISA	ic50	0.0001	uM
(2S)-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonylpyrrolidine-2-carbonyl]amino]-3-[4-(pyrrolidine-1-carbonyloxy)phenyl]propanoic acid	219967: Alpha4-beta1 integrin binding affinity was assessed by measuring the reduction in binding of [125I]VCAM-Ig to a suspension of Jurkat cells (a human T cell line alpha-4-beta-1-beta-7)	ic50	0.0001	uM
(2S)-2-[[C-[(2S)-1-(benzenesulfonyl)azetidin-2-yl]-N-(2,2,2-trifluoroethyl)carbonimidoyl]amino]-3-[4-(2,6-dimethoxyphenyl)phenyl]propanoic acid	1727046: Displacement of 125I-VCAM-Ig from VLA4 in human Jurkat cells incubated for 30 mins by scintillation counting method	ic50	0.0001	uM
(2S)-2-[[3-(benzenesulfonyl)piperidine-3-carbonyl]amino]-3-[4-(2,6-dimethoxyphenyl)phenyl]propanoic acid	216052: Binding affinity towards VLA-4 (alpha4 beta-1) receptor in human Jurkat cells using [125I]VCAM-Ig as radioligand	ic50	0.0001	uM
(2S)-2-[[3-(2-bromophenyl)sulfonylpiperidine-3-carbonyl]amino]-3-[4-(2,6-dimethoxyphenyl)phenyl]propanoic acid	216052: Binding affinity towards VLA-4 (alpha4 beta-1) receptor in human Jurkat cells using [125I]VCAM-Ig as radioligand	ic50	0.0001	uM
(2S)-3-[4-[(2,6-dichlorobenzoyl)amino]phenyl]-2-[[1-[2-(methylcarbamothioylamino)ethyl]cyclopentanecarbonyl]amino]propanoic acid	217051: Inhibitory binding concentration determined against VCAM/VLA-4 in ELISA	ic50	0.0001	uM
(2S)-3-[4-(2,6-dimethoxyphenyl)phenyl]-2-[[3-(3-methylimidazol-4-yl)sulfonylpiperidine-3-carbonyl]amino]propanoic acid	216052: Binding affinity towards VLA-4 (alpha4 beta-1) receptor in human Jurkat cells using [125I]VCAM-Ig as radioligand	ic50	0.0001	uM
3-[4-[(3,5-dichloropyridine-4-carbonyl)amino]phenyl]-2-[3-[2,2-dimethylpropanoyl(2-methylpropyl)amino]-4-ethylphenyl]propanoic acid	242815: Inhibition of Very late antigen-4 (VLA-4) expressing human leukemia cells (HL-60) aggregation with human Vascular cell adhesion molecule-1 (VCAM-1) expressing chinese hamster ovary (CHO) cells	ic50	0.0001	uM
(2S)-2-[[(2S)-1-(benzenesulfonyl)pyrrolidine-2-carbonyl]amino]-3-[4-(pyrrolidine-1-carbonyloxy)phenyl]propanoic acid	219967: Alpha4-beta1 integrin binding affinity was assessed by measuring the reduction in binding of [125I]VCAM-Ig to a suspension of Jurkat cells (a human T cell line alpha-4-beta-1-beta-7)	ic50	0.0001	uM
(2S)-2-[[3-(3-bromophenyl)sulfonylpiperidine-3-carbonyl]amino]-3-[4-(2,6-dimethoxyphenyl)phenyl]propanoic acid	216052: Binding affinity towards VLA-4 (alpha4 beta-1) receptor in human Jurkat cells using [125I]VCAM-Ig as radioligand	ic50	0.0001	uM
(2S)-3-[4-[(2,6-dichlorobenzoyl)amino]phenyl]-2-[[1-(4-methylsulfonylbutyl)cyclopentanecarbonyl]amino]propanoic acid	216088: Inhibition of Very late antigen 4/vascular cell adhesion molecule 1 interaction in ELISA	ic50	0.0001	uM
(2S)-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonyl-2-methylazetidine-2-carbonyl]amino]-3-[4-(2,6-dimethoxyphenyl)phenyl]propanoic acid	216083: Inhibition of Mn2+ activated state of very late antigen 4 (VLA-4)	ic50	0.0001	uM
(2S)-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonyl-2-methylpyrrolidine-2-carbonyl]amino]-3-[4-(2,6-dimethoxyphenyl)phenyl]propanoic acid	216069: Inhibition of [125I]VCAM-Ig binding to VLA-4 of Jurkat cells in the presence of [Ca2+]	ic50	0.0001	uM
3-[4-[(2,6-dichlorobenzoyl)amino]phenyl]-2-[3-[2,2-dimethylpropanoyl(2-methylpropyl)amino]-4-propoxyphenyl]propanoic acid	242815: Inhibition of Very late antigen-4 (VLA-4) expressing human leukemia cells (HL-60) aggregation with human Vascular cell adhesion molecule-1 (VCAM-1) expressing chinese hamster ovary (CHO) cells	ic50	0.0001	uM
(2S)-2-[[amino-[(2S)-1-(benzenesulfonyl)azetidin-2-yl]methylidene]amino]-3-[4-(2,6-dimethoxyphenyl)phenyl]propanoic acid	1727046: Displacement of 125I-VCAM-Ig from VLA4 in human Jurkat cells incubated for 30 mins by scintillation counting method	ic50	0.0001	uM
(2S)-2-[[(2S,4R)-1-(3-cyanophenyl)sulfonyl-4-(cyclobutylamino)pyrrolidine-2-carbonyl]amino]-3-[4-[(3,5-dichloropyridine-4-carbonyl)amino]phenyl]propanoic acid	448685: Displacement of [35S]-labeled ligand from VLA4 in human Jurkat cells washed with buffer containing non activating Ca2+ and Mg2+ by competitive binding assay	ic50	0.0001	uM
(2S)-2-[[(2S)-1-(benzenesulfonyl)pyrrolidine-2-carbonyl]amino]-3-[4-[[3-(diaminomethylideneamino)benzoyl]amino]phenyl]propanoic acid	1324385: Inhibition of integrin alphaVbeta1 (unknown origin)-mediated CHO cell adhesion to fibronectin preincubated for 15 to 30 mins followed by 60 min incubation for adhesion by crystal violet staining based cell adhesion assay	ic50	0.0001	uM
(2S)-2-[[(2S)-1-(benzenesulfonyl)pyrrolidine-2-carbonyl]amino]-3-[4-[4-(4,5-dihydro-1H-imidazol-2-ylamino)butanoylamino]phenyl]propanoic acid	1324385: Inhibition of integrin alphaVbeta1 (unknown origin)-mediated CHO cell adhesion to fibronectin preincubated for 15 to 30 mins followed by 60 min incubation for adhesion by crystal violet staining based cell adhesion assay	ic50	0.0001	uM
(2S)-3-[[2-[[3-[4-(adamantane-1-carbonylamino)butanoylamino]-5-(diaminomethylideneamino)benzoyl]amino]acetyl]amino]-2-[[(2S)-1-(benzenesulfonyl)pyrrolidine-2-carbonyl]amino]propanoic acid	1698264: Inhibition of alphavbeta1 integrin (unknown origin) by solid phase binding assay	ic50	0.0001	uM
(2S)-3-[[2-[[3-[3-(adamantane-1-carbonylamino)propanoylamino]-5-(diaminomethylideneamino)benzoyl]amino]acetyl]amino]-2-[[(2S)-1-(benzenesulfonyl)pyrrolidine-2-carbonyl]amino]propanoic acid	1698264: Inhibition of alphavbeta1 integrin (unknown origin) by solid phase binding assay	ic50	0.0001	uM
(2S)-3-[[2-[[3-[[2-(adamantane-1-carbonylamino)acetyl]amino]-5-(diaminomethylideneamino)benzoyl]amino]acetyl]amino]-2-[[(2S)-1-(benzenesulfonyl)pyrrolidine-2-carbonyl]amino]propanoic acid	1698264: Inhibition of alphavbeta1 integrin (unknown origin) by solid phase binding assay	ic50	0.0001	uM
(2S)-3-[[2-[[3-[5-(adamantane-1-carbonylamino)pentanoylamino]-5-(diaminomethylideneamino)benzoyl]amino]acetyl]amino]-2-[[(2S)-1-(benzenesulfonyl)pyrrolidine-2-carbonyl]amino]propanoic acid	1698264: Inhibition of alphavbeta1 integrin (unknown origin) by solid phase binding assay	ic50	0.0001	uM
(2S)-2-[[(2S)-1-(benzenesulfonyl)-2-ethylazetidine-2-carbonyl]amino]-3-[4-(2,6-dimethoxyphenyl)phenyl]propanoic acid	1727046: Displacement of 125I-VCAM-Ig from VLA4 in human Jurkat cells incubated for 30 mins by scintillation counting method	ic50	0.0001	uM
(2S)-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonylpyrrolidine-2-carbonyl]amino]-3-[4-[2-(dimethylcarbamoyl)phenyl]phenyl]propanoic acid	217347: Antagonistic activity against VLA-4 integrin of human jurkat cells using [125I]VCAM-Ig as radioligand	ic50	0.0001	uM
(2S)-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonylpyrrolidine-2-carbonyl]amino]-3-[4-[2-(methylcarbamoyl)phenyl]phenyl]propanoic acid	217347: Antagonistic activity against VLA-4 integrin of human jurkat cells using [125I]VCAM-Ig as radioligand	ic50	0.0001	uM
(2S)-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonylpyrrolidine-2-carbonyl]amino]-3-[4-(2-methylsulfonylphenyl)phenyl]propanoic acid	217347: Antagonistic activity against VLA-4 integrin of human jurkat cells using [125I]VCAM-Ig as radioligand	ic50	0.0001	uM
(2S)-3-[4-(2-carbamoylphenyl)phenyl]-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonylpyrrolidine-2-carbonyl]amino]propanoic acid	217347: Antagonistic activity against VLA-4 integrin of human jurkat cells using [125I]VCAM-Ig as radioligand	ic50	0.0001	uM
(5R)-5-[[(2R)-2-[[2-[4-(1,3-benzothiazol-2-ylamino)phenyl]acetyl]amino]-6-[[(E)-3-pyridin-3-ylprop-2-enoyl]amino]hexanoyl]amino]-6-[(1-carbamoylcyclohexyl)amino]-6-oxohexanoic acid	410577: Inhibition of human integrin alpha-4-beta-1-mediated MOLT4 cell adhesion to biotin-conjugated CS-1 peptide	ic50	0.0001	uM
(2S)-3-[4-(2-cyanophenyl)phenyl]-2-[[(2S,3S)-1-(3,5-dichlorophenyl)sulfonyl-3-hydroxypyrrolidine-2-carbonyl]amino]propanoic acid	219966: Inhibition of integrin alpha4-beta1 of human Jurkat cells	ic50	0.0001	uM
(2S)-2-[[(2S,3S)-1-(3,5-dichlorophenyl)sulfonyl-3-hydroxypyrrolidine-2-carbonyl]amino]-3-[4-(2-methoxyphenyl)phenyl]propanoic acid	219966: Inhibition of integrin alpha4-beta1 of human Jurkat cells	ic50	0.0001	uM
(2S)-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonyl-2-methylpyrrolidine-2-carbonyl]amino]-3-[4-(morpholine-4-carbonyloxy)phenyl]propanoic acid	219967: Alpha4-beta1 integrin binding affinity was assessed by measuring the reduction in binding of [125I]VCAM-Ig to a suspension of Jurkat cells (a human T cell line alpha-4-beta-1-beta-7)	ic50	0.0001	uM
(2S)-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonylpyrrolidine-2-carbonyl]amino]-3-[4-[2-[(2-methylpropan-2-yl)oxy]-2-oxoethoxy]phenyl]propanoic acid	219967: Alpha4-beta1 integrin binding affinity was assessed by measuring the reduction in binding of [125I]VCAM-Ig to a suspension of Jurkat cells (a human T cell line alpha-4-beta-1-beta-7)	ic50	0.0001	uM
(2S)-3-[4-[(2,6-dichlorobenzoyl)amino]phenyl]-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonyl-2-methylpyrrolidine-2-carbonyl]amino]propanoic acid	216069: Inhibition of [125I]VCAM-Ig binding to VLA-4 of Jurkat cells in the presence of [Ca2+]	ic50	0.0001	uM
(2S)-2-[[(2S)-1-(3-chlorophenyl)sulfonylpyrrolidine-2-carbonyl]amino]-3-[4-[(3,5-dichloropyridine-4-carbonyl)amino]phenyl]propanoic acid	216069: Inhibition of [125I]VCAM-Ig binding to VLA-4 of Jurkat cells in the presence of [Ca2+]	ic50	0.0001	uM
(2S)-3-[4-[(3,5-dichloro-1-methylpyridin-1-ium-4-carbonyl)amino]phenyl]-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonyl-2-methylpyrrolidine-2-carbonyl]amino]propanoic acid	216069: Inhibition of [125I]VCAM-Ig binding to VLA-4 of Jurkat cells in the presence of [Ca2+]	ic50	0.0001	uM
(2S)-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonyl-2-methylpyrrolidine-2-carbonyl]amino]-3-[4-[(2,4-dichloropyridine-3-carbonyl)amino]phenyl]propanoic acid	216069: Inhibition of [125I]VCAM-Ig binding to VLA-4 of Jurkat cells in the presence of [Ca2+]	ic50	0.0001	uM
(2S)-3-[4-[(4-chloropyridine-3-carbonyl)amino]phenyl]-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonyl-2-methylpyrrolidine-2-carbonyl]amino]propanoic acid	216070: Inhibition of [125I]VCAM-Ig binding to VLA-4 of Jurkat cells in the presence of Mn2+	ic50	0.0001	uM
(2S)-3-[4-[(2-chloro-4-methoxypyridine-3-carbonyl)amino]phenyl]-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonyl-2-methylpyrrolidine-2-carbonyl]amino]propanoic acid	216069: Inhibition of [125I]VCAM-Ig binding to VLA-4 of Jurkat cells in the presence of [Ca2+]	ic50	0.0001	uM
(2S)-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonyl-2-methylpyrrolidine-2-carbonyl]amino]-3-[4-[2,6-dimethoxy-4-(pyrrolidin-1-ylmethyl)phenyl]phenyl]propanoic acid	216069: Inhibition of [125I]VCAM-Ig binding to VLA-4 of Jurkat cells in the presence of [Ca2+]	ic50	0.0001	uM
(2S)-3-[4-[(4,6-dichloro-2-oxo-3H-pyridine-5-carbonyl)amino]phenyl]-2-[[(2S)-1-(3,5-dichlorophenyl)sulfonyl-2-methylpyrrolidine-2-carbonyl]amino]propanoic acid	216069: Inhibition of [125I]VCAM-Ig binding to VLA-4 of Jurkat cells in the presence of [Ca2+]	ic50	0.0001	uM
(2S)-2-[[(2S)-1-(benzenesulfonyl)pyrrolidine-2-carbonyl]amino]-3-[4-[(3,5-dichloropyridine-4-carbonyl)amino]phenyl]propanoic acid	216069: Inhibition of [125I]VCAM-Ig binding to VLA-4 of Jurkat cells in the presence of [Ca2+]	ic50	0.0001	uM
2-[[1-(benzenesulfonyl)pyrrolidine-2-carbonyl]amino]-3-[4-(2,6-dimethoxyphenyl)phenyl]propanoic acid	218412: Inhibition of [125I]VCAM-Ig binding to human integrin alpha4-beta1 (VLA-4) of Jurkat cells	ic50	0.0001	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
bisphenol A	decreases expression, increases reaction, decreases reaction, increases expression, affects expression (+1 more)	5
sodium arsenite	decreases expression, increases abundance, increases expression, increases stability	5
Cisplatin	increases expression, affects response to substance, decreases response to substance, increases activity	4
Cadmium Chloride	affects expression, increases abundance, increases expression, affects reaction	4
Fulvestrant	decreases reaction, increases expression, increases reaction	3
Arsenic	decreases expression, increases methylation, increases abundance	3
Benzo(a)pyrene	affects reaction, decreases expression, decreases methylation, increases methylation, affects expression	3
Cadmium	increases expression, affects reaction, affects expression, increases abundance	3
Cannabidiol	affects cotreatment, decreases expression, increases expression	3
Estradiol	increases expression, affects cotreatment, decreases expression	3
Methotrexate	decreases expression, increases expression	3
Tobacco Smoke Pollution	increases expression, affects expression, decreases expression	3
Tretinoin	affects binding, increases cleavage, increases expression	3
Valproic Acid	decreases methylation, increases expression	3
arsenic disulfide	affects expression, decreases expression	2
ML 7	decreases activity, affects binding, affects localization	2
chloropicrin	decreases expression, increases expression	2
(+)-JQ1 compound	decreases expression, decreases reaction, increases expression	2
Arsenic Trioxide	decreases expression	2
Dibutyl Phthalate	increases expression, decreases expression	2
Hydrogen Peroxide	affects expression, decreases expression	2
Oxygen	increases expression, affects expression, affects reaction	2
Tetrachlorodibenzodioxin	decreases expression, increases expression	2
Cyclosporine	decreases expression	2
Antirheumatic Agents	decreases expression, increases expression	2
Simvastatin	decreases expression	2
Raloxifene Hydrochloride	increases expression	2
aristolochic acid I	decreases expression	1
p-carboxymethylphenyl 1,1-bis(3’-indolyl)-1-(p-carboxymethylphenyl)methane	increases response to substance, decreases expression	1
moringin	affects cotreatment, decreases expression	1

ChEMBL screening assays

409 unique, capped per target: 376 binding, 32 functional, 1 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2092376	Binding	Inhibition of integrin beta1 phosphorylation in human MB-MDA-231 cells at 1 to 10 uM incubated for 24 hrs by Western blot	Alkaloids from Pachysandra terminalis inhibit breast cancer invasion and have potential for development as antimetastasis therapeutic agents. — J Nat Prod
CHEMBL823926	Functional	Inhibition of alpha4-beta1 interaction to vascular cell adhesion molecule-1 (VCAM-1) was determined	Synthesis and structure-activity relationship of mannose-based peptidomimetics selectively blocking integrin alpha4beta7 binding to mucosal addressin cell adhesion molecule-1. — J Med Chem
CHEMBL4709538	ADMET	Inhibition of integrin alphavbeta1 (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

8 cell lines: 7 cancer cell line, 1 factor-dependent cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B1DR	Abcam HCT 116 ITGB1 KO	Cancer cell line	Male
CVCL_B8XR	Abcam MCF-7 ITGB1 KO	Cancer cell line	Female
CVCL_B9L6	Abcam A-549 ITGB1 KO	Cancer cell line	Male
CVCL_C8H4	FDCP1-P4C10	Factor-dependent cell line
CVCL_E0FJ	Ubigene HeLa ITGB1 KO	Cancer cell line	Female
CVCL_ST43	HAP1 ITGB1 (-) 1	Cancer cell line	Male
CVCL_ST44	HAP1 ITGB1 (-) 2	Cancer cell line	Male
CVCL_ST45	HAP1 ITGB1 (-) 3	Cancer cell line	Male

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00556283	PHASE4	COMPLETED	RCT: STARR vs Biofeedback
NCT00226044	PHASE3	COMPLETED	Rectal and Oral Omeprazole Treatment of Reflux Disease in Infants.
NCT03127345	PHASE2	WITHDRAWN	Omega 3 Fatty Acid Treatment for Pediatric Musculoskeletal Health
NCT02230072	PHASE1	COMPLETED	Fetoscopic Meningomyelocele Repair Study
NCT00060606	Not specified	COMPLETED	Management of Myelomeningocele Study (MOMS)
NCT00966927	Not specified	ACTIVE_NOT_RECRUITING	Assessment of Functional Independence and Quality of Life in Adolescents With Spina Bifid
NCT00975338	Not specified	COMPLETED	The LETS Study: A Longitudinal Evaluation of Transition Services
NCT02592291	Not specified	RECRUITING	Mobile Health Self-Management and Support System for Chronic and Complex Health Conditions
NCT03044821	Not specified	TERMINATED	Open Myelomeningocele Repair With High Maternal BMI
NCT03090633	Not specified	ACTIVE_NOT_RECRUITING	Fetoscopic Repair of Isolated Fetal Spina Bifida
NCT03544970	Not specified	COMPLETED	An Audit of the Posterior Fossa Characterization in Open Spina Bifida Based on Tertiary Center Experience
NCT04763382	Not specified	UNKNOWN	The Effect of Nursing Interventions for Clean Intermittent Catheterization Caregivers and Child
NCT05718440	Not specified	RECRUITING	Uronephrological Complications Risk Factors in Spinal Dysraphism
NCT05962086	Not specified	UNKNOWN	Determining Developmental and Clinical Markers Affecting Urinary Function of Children With Spinal Dysraphism
NCT06907732	Not specified	NOT_YET_RECRUITING	Fetoscopic Robotic Open Spina Bifida Treatment
NCT02033772	Not specified	COMPLETED	Prospective Data Collection of Patients < 6 Months of Age Undergoing Thoracoscopic Surgery
NCT02466451	Not specified	COMPLETED	Study in Children With the Diagnosis of Congenital Diaphragmatic Hernia (CDH) and Oesophageal Atresia (EA)
NCT02525705	Not specified	COMPLETED	Dumping Syndrome After Operation of Esophageal Atresia Type III
NCT02883725	Not specified	COMPLETED	National Register of Oesophageal Atresia
NCT03023865	Not specified	UNKNOWN	Individualized Management for Long Gap Esophageal Atresia
NCT03415893	Not specified	COMPLETED	High-resolution Esophageal Manometry
NCT03455881	Not specified	UNKNOWN	Phenotypic and Genetic Assessment of Tracheal and Esophageal Birth Defects in Patients
NCT03615495	Not specified	COMPLETED	Flourish™ Pediatric Esophageal Atresia
NCT03619408	Not specified	UNKNOWN	Management of Esophagitis Following Repair of Esophageal Atresia
NCT03666767	Not specified	COMPLETED	Management and Outcomes of Congenital Anomalies in Low-, Middle- and High-Income Countries
NCT03730454	Not specified	ACTIVE_NOT_RECRUITING	Transanastomotic Tube for Proximal Esophageal Atresia With Distal Tracheoesophageal Fistula Repair
NCT03767673	Not specified	UNKNOWN	Cardiorespiratory Performance and Pulmonary Microbiome in Patients After Repair of Esophageal Atresia
NCT03999008	Not specified	UNKNOWN	Oral Viscous Budesonide in Anastomotic Stricture After Esophageal Atresia Repair (OVB in EA)
NCT04072419	Not specified	UNKNOWN	Application of Enhanced Recovery After Surgery for Congenital Esophageal Atresia During Perioperative Period
NCT04136795	Not specified	UNKNOWN	Evaluation of the Respiratory Impact After Conventional or Minimally Invasive Esophageal Atresia Surgery
NCT04259528	Not specified	UNKNOWN	Endoscopic Ultrasound Findings in Esophageal Atresia Following Surgical Repair
NCT04522193	Not specified	RECRUITING	Dumping Syndrome and Esophageal Atresia
NCT04901546	Not specified	COMPLETED	Esophageal Atresia: a Natural Experiment of the Effects of Oral Inoculation on the Gut Microbiome
NCT04932746	Not specified	COMPLETED	The Effect of Dexmedetomidine on Oxygen During One Lung Ventilation in Pediatric Surgery.
NCT05129930	Not specified	COMPLETED	Fluid Overload and Pulmonary Function
NCT05527873	Not specified	COMPLETED	Respiratory Complications of Operated Esophageal Atresia in Children
NCT05995171	Not specified	RECRUITING	Long Term Outcome of Easophageal Atresia : Transmics Profiles in Adolescence
NCT06073158	Not specified	COMPLETED	Molecular Signatures of Esophageal Atresia
NCT06208449	Not specified	UNKNOWN	Robotic Versus Thoracoscopy Versus Thoracotomy Repair for Congenital Esophageal Atresia
NCT06335862	Not specified	ENROLLING_BY_INVITATION	Primary Posterior Tracheopexy Prevents Tracheal Collapse