ITGA2B

Summary

ITGA2B (integrin subunit alpha 2b, HGNC:6138) is a protein-coding gene on chromosome 17q21.31, encoding Integrin alpha-IIb (P08514). Integrin alpha-IIb/beta-3 (ITGA2B:ITGB3) is a receptor for fibronectin, fibrinogen, plasminogen, prothrombin, thrombospondin and vitronectin.

This gene encodes a member of the integrin alpha chain family of proteins. The encoded preproprotein is proteolytically processed to generate light and heavy chains that associate through disulfide linkages to form a subunit of the alpha-IIb/beta-3 integrin cell adhesion receptor. This receptor plays a crucial role in the blood coagulation system, by mediating platelet aggregation. Mutations in this gene are associated with platelet-type bleeding disorders, which are characterized by a failure of platelet aggregation, including Glanzmann thrombasthenia.

Source: NCBI Gene 3674 — RefSeq curated summary.

At a glance

• Gene–disease (curated): platelet-type bleeding disorder 16 (Definitive, ClinGen) — +5 more curated relationships
• GWAS associations: 9
• Clinical variants (ClinVar): 992 total — 156 pathogenic, 100 likely-pathogenic
• Phenotypes (HPO): 52
• Druggable target: yes — 14 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_000419

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:6138
Approved symbol	ITGA2B
Name	integrin subunit alpha 2b
Location	17q21.31
Locus type	gene with protein product
Status	Approved
Aliases	CD41B, CD41, PPP1R93, GPIIb
Ensembl gene	ENSG00000005961
Ensembl biotype	protein_coding
OMIM	607759
Entrez	3674

Gene structure

Transcript identifiers

Ensembl transcripts: 13 — 7 retained_intron, 6 protein_coding

ENST00000262407, ENST00000587295, ENST00000589645, ENST00000591990, ENST00000592075, ENST00000592226, ENST00000592253, ENST00000592462, ENST00000592944, ENST00000648408, ENST00000901306, ENST00000901307, ENST00000949677

RefSeq mRNA: 1 — MANE Select: NM_000419 NM_000419

CCDS: CCDS32665

Canonical transcript exons

ENST00000262407 — 30 exons

Exon	Start	End
ENSE00000390828	44386010	44386131
ENSE00000732018	44385824	44385921
ENSE00000732019	44385551	44385716
ENSE00000732047	44375591	44375716
ENSE00000732049	44374998	44375111
ENSE00000854277	44374354	44374470
ENSE00000854286	44389286	44389649
ENSE00001321776	44374659	44374760
ENSE00001504857	44385286	44385335
ENSE00002793608	44372181	44372423
ENSE00003464623	44384311	44384354
ENSE00003473537	44380386	44380490
ENSE00003476888	44384948	44385076
ENSE00003484770	44383894	44383946
ENSE00003491331	44380246	44380301
ENSE00003506001	44380002	44380153
ENSE00003508572	44380600	44380645
ENSE00003512793	44380879	44381061
ENSE00003514103	44377009	44377088
ENSE00003515097	44385164	44385209
ENSE00003519044	44377698	44377790
ENSE00003530299	44376085	44376184
ENSE00003557061	44383493	44383704
ENSE00003561077	44384538	44384585
ENSE00003577648	44375833	44375985
ENSE00003590069	44376308	44376388
ENSE00003611358	44378362	44378509
ENSE00003624080	44378643	44378710
ENSE00003638103	44379689	44379814
ENSE00003677346	44384085	44384138

Expression profiles

Bgee: expression breadth ubiquitous, 182 present calls, max score 97.36.

FANTOM5 (CAGE): breadth broad, TPM avg 3.9836 / max 515.4776, expressed in 435 samples.

FANTOM5 promoters (7 alternative TSS)

Promoter ID	TPM avg	Samples expressed
166373	2.0095	126
166377	0.6846	82
166372	0.5787	308
166375	0.5223	52
166376	0.0743	24
166374	0.0648	26
166371	0.0495	30

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
monocyte	CL:0000576	97.36	gold quality
mononuclear cell	CL:0000842	97.03	gold quality
leukocyte	CL:0000738	96.45	gold quality
blood	UBERON:0000178	87.45	gold quality
trabecular bone tissue	UBERON:0002483	84.65	gold quality
granulocyte	CL:0000094	84.55	gold quality
pancreatic ductal cell	CL:0002079	83.26	silver quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	83.21	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	81.81	gold quality
right hemisphere of cerebellum	UBERON:0014890	81.48	gold quality
sperm	CL:0000019	81.29	gold quality
bone marrow cell	CL:0002092	81.29	gold quality
male germ cell	CL:0000015	80.68	gold quality
cerebellar cortex	UBERON:0002129	80.57	gold quality
cerebellar hemisphere	UBERON:0002245	80.53	gold quality
bone marrow	UBERON:0002371	80.15	gold quality
endometrium epithelium	UBERON:0004811	79.84	gold quality
cerebellum	UBERON:0002037	79.53	gold quality
right lung	UBERON:0002167	79.23	gold quality
triceps brachii	UBERON:0001509	77.81	gold quality
vena cava	UBERON:0004087	77.64	silver quality
cerebellar vermis	UBERON:0004720	77.10	silver quality
inferior olivary complex	UBERON:0002127	76.85	gold quality
right lobe of thyroid gland	UBERON:0001119	76.32	gold quality
gluteal muscle	UBERON:0002000	75.76	gold quality
spleen	UBERON:0002106	75.73	gold quality
thyroid gland	UBERON:0002046	75.64	gold quality
left lobe of thyroid gland	UBERON:0001120	75.47	gold quality
tendon of biceps brachii	UBERON:0008188	75.12	gold quality
right frontal lobe	UBERON:0002810	74.97	gold quality

Single-cell (SCXA)

Detected in 15 experiment(s), a significant marker in 14.

Experiment	Marker?	Max mean expression
E-MTAB-9067	yes	1548.02
E-CURD-112	yes	1307.93
E-MTAB-7407	yes	1036.51
E-MTAB-8884	yes	846.73
E-HCAD-6	yes	597.95
E-ANND-5	yes	500.93
E-MTAB-8205	yes	136.30
E-HCAD-4	yes	54.11
E-CURD-122	yes	22.66
E-MTAB-9221	yes	21.89
E-HCAD-10	yes	18.24
E-HCAD-1	yes	7.13
E-MTAB-9801	yes	4.56
E-CURD-6	no	133.34
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CTNNBL1, ETS1, ETV6, FLI1, FOSB, GATA1, HOXB4, IRF2, MBD2, RUNX1, SP1, SP3, SPI1, STAT6, TAL1, ZFPM1

miRNA regulators (miRDB)

13 targeting ITGA2B, 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-4753-3P	99.90	71.03	3786
HSA-MIR-4728-5P	99.85	69.39	4718
HSA-MIR-130B-5P	99.83	68.50	1888
HSA-MIR-6785-5P	99.82	68.68	4428
HSA-MIR-149-3P	99.72	68.22	3963
HSA-MIR-6883-5P	99.69	68.05	3785
HSA-MIR-4516	99.61	67.78	3390
HSA-MIR-3612	99.45	66.02	1333
HSA-MIR-650	99.45	65.77	1309
HSA-MIR-130A-5P	99.33	70.26	2623
HSA-MIR-4443	98.02	66.25	1928
HSA-MIR-4423-3P	97.98	69.66	912
HSA-MIR-711	96.60	65.75	528

Literature-anchored findings (GeneRIF, showing 40)

• Reduction of disulfide bonds within the redox site of integrin alphaIIbbeta3 leads to transitions in the integrin’s activation state, which is the switch from “off” to “on” that regulates its ligand binding affinity. (PMID:11467947)
• Distinct domains of alphaIIbbeta3 support different aspects of outside-in signal transduction and platelet activation. (PMID:11583324)
• Lateral clustering of platelet GP Ib-IX complexes leads to up-regulation of the adhesive function of integrin alpha IIbbeta 3 (PMID:11812775)
• GPIIb-IIIa complexes are not in an activated conformational state after dissociation of abciximab unless there is an additional source of activation. (PMID:11858493)
• Relationships between Rap1b, affinity modulation of integrin alpha IIbbeta 3, and the actin cytoskeleton (integrin alpha(IIb)beta(3)) (PMID:11994301)
• describes regions within CIB and alpha(IIb) that interact with one another (PMID:12023286)
• Factor XIII mediates adhesion of platelets to endothelial cells through alpha(v)beta(3) and glycoprotein IIb/IIIa integrins. (PMID:12031826)
• binding of Aup1 plays a crucial role in the alpha(IIb)beta(3) inside-out signaling (PMID:12042322)
• collagen receptor glycoprotein VI and alphaIIbbeta3 trigger distinct patterns of receptor signalling in platelets, leading to tyrosine phosphorylation of PLCgamma2 (integrin alphaiibbeta3) (PMID:12049640)
• Integrin alpha IIbbeta 3 has agonist-specific activation states and causes intrasubunit and intersubunit allosteric effects (PMID:12140290)
• the effects of either the Cys5Ala or Cys435Ala substitution of GPIIIa on the ability to bind GPIIb and the adhesive properties of the resulting GPIIb-IIIa complex (PMID:12200372)
• co-stimulation of G(12/13) and G(i) pathways is sufficient to activate GPIIb/IIIa in human platelets in a mechanism that involves intracellular calcium (PMID:12297512)
• three-dimensional structure at 20-A resolution of the unliganded; low-affinity state of the human platelet integrin alpha(IIb)beta(3) derived by electron cryomicroscopy and single particle image reconstruction (PMID:12388784)
• Identification of distal regulatory regions in the human alpha IIb gene locus necessary for consistent, high-level megakaryocyte expression (PMID:12393463)
• patients with schizophrenia have increased platelet expression of alpha IIb, IIIa which may contribute to their increased risk of cardiovascular illness (PMID:12399140)
• Ligand binding promotes the entropy-driven oligomerization of this protein (PMID:12426312)
• A naturally occurring Tyr143His alpha IIb mutation abolishes alpha IIb beta 3 function for soluble ligands but retains its ability for mediating cell adhesion and clot retraction. The functional defect is likely caused by its allosteric effect. (PMID:12506038)
• Integrin alphaiibbeta3 plays a role in signal transduction that leads to a defect in leukocyte adhesion (PMID:12511588)
• possible association between the GPIIb/IIIa PIA1/A2 polymorphism and the occurrence of cryptogenic stroke in young patients (PMID:12586134)
• data suggest that despite partial disruption of calf-1 or calf-2 domain by mutation in Glanzmann thrombasthenia, glycoprotein IIb/IIIa complex is formed but its transport from the endoplasmic reticulum is impaired (PMID:12609844)
• Review. A signal is initiated at the cytoplasmic tail to transform the extracellular domain of alphaIIbbeta3 into a functional receptor for fibrinogen or von Willebrand factor to support platelet aggregation & thrombus formation. (PMID:12637342)
• Intercellular calcium communication is primarily mediated by a signaling mechanism operating between this protein, integrin beta 3 and the adenosine diphosphate purinergic receptor P2Y12. (PMID:12668663)
• binding of thrombin to GPIbalpha induces fibrin binding to resting alphaIIbbeta3 leading to fibrin-dependent platelet aggregation and clot retraction, that can be selectively inhibited by alphaIIbbeta3 antagonists (PMID:12719784)
• results suggest that homomeric associations involving transmembrane domains provide a driving force for integrin activation; results also suggest a structural basis for the coincidence of integrin activation and clustering (PMID:12730600)
• the extracellular Ig domain of IAP(CD47), when bound to thrombospondin, interacts with integrin alphaIIbbeta3 and can change alphaIIbbeta3 in a high affinity state without the requirement of intracellular signaling (PMID:12736272)
• identification of binding site in gamma C-domain of fibrinogen (PMID:12799374)
• Pathways dependent on the platelet alpha(2)beta(3) integrin physiology could be implicated in the pathogenesis of Type 2 diabetes. (PMID:12827240)
• Bidirectional signaling of ITGA2B requires the beta3 cytoplasmic domain. (PMID:12860973)
• reduced availability of GPIIb-mRNA associated with G188A mutation is due to inefficient RNA splicing or utilization of alternative intronic donor sites that generate an in-frame STOP codon resulting in activation of nonsense-mediated mRNA decay, or both (PMID:12871379)
• high prevalence of Glanzmann thrombasthenia patients homozygous for the so-called French gypsy mutation (IVS15[ + 1]G–>A) in alphaIIb (PMID:12871468)
• Glycoprotein IIb/IIIa has a role in platelet-activating factor-induced platelet activation with protein kinase C activity (PMID:12911597)
• the E749ATSTFTN756 region of the beta3-tail stabilizes the binding of soluble and surface-bound ligand to integrin alphaIIbbeta3 via a mechanism that involves the phosphorylation of FAK (PMID:14521607)
• proteins regulated by CBFA2 are required for inside-out signal transduction-dependent activation of GPIIb-IIIa (PMID:14525764)
• Substitution of conserved serine residues at position 1 in beta strand A of all seven repeats of alpha(IIb) similarly inhibited ligand binding to alpha(IIb)beta(3). (PMID:14597981)
• analysis of the three-dimensional model of integrin alphaIIbbeta3 (PMID:15056669)
• ERK promotes megakaryocyte differentiation by coordinate regulation of nuclear factors that synergize in GPIIb promoter regulation. (PMID:15121870)
• integrin alpha(IIb)beta3 adhesive function is regulated by platelet FXIII and calpain (PMID:15131115)
• This review discusses the major role played by glycoprotein IIb/IIIa (GPIIb/IIIa) in the regulation of platelet adhesion and aggregation during hemostasis. (PMID:15134555)
• alpha IIb beta 3 signaling in platelets is regulated by SHIP1 and Lyn kinase (PMID:15166241)
• studies reveal a previously unrecognized role for integrin alpha 2b whereby the alpha subunit cytoplasmic tail localizes the machinery for initiating and temporally maintaining the regulatory signaling activity of protein phosphatase 1 (PMID:15205468)

Cross-species orthologs

10 orthologs

Organism	Symbol	Gene ID
danio_rerio	itga2b	ENSDARG00000018687
mus_musculus	Itga2b	ENSMUSG00000034664
rattus_norvegicus	Itga2b	ENSRNOG00000022071
drosophila_melanogaster	if	FBGN0001250
drosophila_melanogaster	mew	FBGN0004456
drosophila_melanogaster	ItgaPS4	FBGN0034005
drosophila_melanogaster	ItgaPS5	FBGN0034880
drosophila_melanogaster	scb	FBGN0286785
caenorhabditis_elegans		WBGENE00002081
caenorhabditis_elegans		WBGENE00003929

Paralogs (17): ITGAL (ENSG00000005844), ITGA3 (ENSG00000005884), ITGA8 (ENSG00000077943), ITGAE (ENSG00000083457), ITGA6 (ENSG00000091409), ITGA4 (ENSG00000115232), ITGA7 (ENSG00000135424), ITGA11 (ENSG00000137809), ITGAV (ENSG00000138448), ITGAX (ENSG00000140678), ITGA10 (ENSG00000143127), ITGA9 (ENSG00000144668), ITGAD (ENSG00000156886), ITGA5 (ENSG00000161638), ITGA2 (ENSG00000164171), ITGAM (ENSG00000169896), ITGA1 (ENSG00000213949)

Protein

Protein identifiers

Integrin alpha-IIb — P08514 (reviewed: P08514)

Alternative names: GPalpha IIb, Platelet membrane glycoprotein IIb

All UniProt accessions (3): P08514, A0A3B3IU79, K7EP83

UniProt curated annotations — full annotation on UniProt →

Function. Integrin alpha-IIb/beta-3 (ITGA2B:ITGB3) is a receptor for fibronectin, fibrinogen, plasminogen, prothrombin, thrombospondin and vitronectin. It recognizes the sequence R-G-D in a wide array of ligands. It recognizes the sequence H-H-L-G-G-G-A-K-Q-A-G-D-V in fibrinogen gamma chain. Following activation integrin alpha-IIb/beta-3 brings about platelet/platelet interaction through binding of soluble fibrinogen. This step leads to rapid platelet aggregation which physically plugs ruptured endothelial cell surface. Integrin ITGA2B:ITGB3 is also the receptor of erythrocyte-specific ICAM4 ligand involved in heterotypic cell-cell adhesion between erythrocytes and activated platelets.

Subunit / interactions. Heterodimer of an alpha and a beta subunit. The alpha subunit is composed of a heavy and a light chain linked by a disulfide bond. Alpha-IIb associates with beta-3. Directly interacts with RNF181. Interacts (via C-terminus cytoplasmic tail region) with CIB1; the interaction is direct and calcium-dependent. Interacts (via C-terminus cytoplasmic tail region) with CIB2, CIB3 and CIB4; the interactions are stabilized/increased in a calcium and magnesium-dependent manner. ITGA2B:ITGB3 interacts with PPIA/CYPA; the interaction is ROS and PPIase activity-dependent and is increased in the presence of thrombin. ITGA2B:ITGB3 interacts with SELP (via C-type lectin domain); the interaction mediates cell-cell interaction and adhesion.

Subcellular location. Cell membrane.

Tissue specificity. Isoform 1 and isoform 2 are expressed in platelets and megakaryocytes, but not in reticulocytes. Not detected in Jurkat, nor in U937 cell lines. Isoform 3 is expressed in prostate adenocarcinoma, as well as in several erythroleukemia, prostate adenocarcinoma and melanoma cell lines, including PC-3, DU-145, HEL, WM983A, WM983B and WM35. Not detected in platelets, nor in normal prostate (at protein level).

Post-translational modifications. Cleaved by ELANE; the cleavage promotes activation of platelet fibrinogen receptor integrin alpha-IIb/beta-3.

Disease relevance. Fetomaternal alloimmune thrombocytopenia 2 (FMAIT2) [MIM:621266] A form of fetomaternal alloimmune thrombocytopenia, a bleeding disorder caused by maternal/fetal incompatibility for platelet alloantigens and arising when a fetus inherits a paternal platelet alloantigen that the mother does not possess. During pregnancy, as well as parturition, maternal alloantibodies against paternally-inherited platelet antigens cause destruction of fetal platelets and fetal/neonatal thrombocytopenia. Disease severity and clinical features in the fetus or neonate are heterogeneous. While most fetuses remain asymptomatic, others develop skin bleedings (petechiae) or internal organ bleedings. The most severe symptom is intracranial hemorrhage that is mostly discovered postnatally and can result in neurological complications or even death. Mothers with circulating platelet alloantibodies may experience miscarriage. FMAIT2 transmission pattern is consistent with autosomal dominant paternal inheritance. Disease susceptibility is associated with variants affecting the gene represented in this entry. Glanzmann thrombasthenia 1 (GT1) [MIM:273800] A form of Glanzmann thrombasthenia, a disorder characterized by failure of platelet aggregation, absent or diminished clot retraction, and mucocutaneous bleeding of mild-to-moderate severity. Glanzmann thrombasthenia has been classified into clinical types I and II. In type I, platelets show absence of glycoprotein IIb-IIIa complexes at their surface and lack fibrinogen and clot retraction capability. In type II, the platelets express glycoprotein IIb-IIIa complexes at reduced levels, have detectable amounts of fibrinogen, and have low or moderate clot retraction capability. GT1 inheritance is autosomal recessive. The disease is caused by variants affecting the gene represented in this entry. Bleeding disorder, platelet-type, 16 (BDPLT16) [MIM:187800] An autosomal dominant form of congenital macrothrombocytopenia associated with platelet anisocytosis. It is a disorder of platelet production. Affected individuals may have no or only mildly increased bleeding tendency. In vitro studies show mild platelet functional abnormalities. The disease is caused by variants affecting the gene represented in this entry.

Polymorphism. Genetic variants in ITGA2B define different platelet-specific alloantigen systems that are involved in fetomaternal alloimmune thromobocytopenia. Alloantigen system Bak, also known as HPA-3 or Lek, is characterized by variant p.Ser874Ile (alloantigen Bak(a) or Lek(a) or HPA-3a) and variant p.Ile874Ser (alloantigen Bak(b) or Lek(b) or HPA-3b). Additional platelet-specific alloantigens involved in fetomaternal alloimmune thromobocytopenia are known.

Similarity. Belongs to the integrin alpha chain family.

Isoforms (3)

UniProt ID	Names	Canonical?
P08514-1	1	yes
P08514-2	2
P08514-3	3, tr-alpha-IIb

RefSeq proteins (1): NP_000410* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000413	Integrin_alpha	Family
IPR013517	FG-GAP	Repeat
IPR013519	Int_alpha_beta-p	Repeat
IPR013649	Integrin_alpha_Ig-like_1	Domain
IPR018184	Integrin_alpha_C_CS	Conserved_site
IPR028994	Integrin_alpha_N	Homologous_superfamily
IPR032695	Integrin_dom_sf	Homologous_superfamily
IPR048285	Integrin_alpha_Ig-like_2	Domain
IPR048286	Integrin_alpha_Ig-like_3	Domain

Pfam: PF00357, PF01839, PF08441, PF20805, PF20806

UniProt features (215 total): strand 81, sequence variant 43, binding site 20, helix 13, sequence conflict 11, turn 11, disulfide bond 9, repeat 7, glycosylation site 7, chain 4, topological domain 2, splice variant 2, signal peptide 1, short sequence motif 1, modified residue 1, transmembrane region 1, mutagenesis site 1

Structure

Experimental structures (PDB)

78 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
7SC4	X-RAY DIFFRACTION	1.85
7UDH	X-RAY DIFFRACTION	2
7UBR	X-RAY DIFFRACTION	2.05
3T3P	X-RAY DIFFRACTION	2.2
7TMZ	X-RAY DIFFRACTION	2.2
3NIG	X-RAY DIFFRACTION	2.25
7U9V	X-RAY DIFFRACTION	2.25
3NID	X-RAY DIFFRACTION	2.3
7L8P	X-RAY DIFFRACTION	2.35
7UCY	X-RAY DIFFRACTION	2.35
3ZE2	X-RAY DIFFRACTION	2.35
7UKT	X-RAY DIFFRACTION	2.37
2VDR	X-RAY DIFFRACTION	2.4
3NIF	X-RAY DIFFRACTION	2.4
7UJK	X-RAY DIFFRACTION	2.43
3ZDX	X-RAY DIFFRACTION	2.45
3ZDY	X-RAY DIFFRACTION	2.45
7UJE	X-RAY DIFFRACTION	2.5
7TCT	X-RAY DIFFRACTION	2.5
2VDO	X-RAY DIFFRACTION	2.51
3FCS	X-RAY DIFFRACTION	2.55
7U60	X-RAY DIFFRACTION	2.55
2VDQ	X-RAY DIFFRACTION	2.59
4Z7N	X-RAY DIFFRACTION	2.6
3T3M	X-RAY DIFFRACTION	2.6
7TD8	X-RAY DIFFRACTION	2.6
7TPD	X-RAY DIFFRACTION	2.6
7UK9	X-RAY DIFFRACTION	2.6
7UKO	X-RAY DIFFRACTION	2.6
9E8B	ELECTRON MICROSCOPY	2.67

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P08514-F1	88.00	0.71

Antibody-complex structures (SAbDab): 50 — 2VC2, 2VDK, 2VDL, 2VDM, 2VDN, 2VDO, 2VDP, 2VDQ, 2VDR, 3NID, 3NIF, 3NIG, 3T3M, 3T3P, 3ZDX, 3ZDY, 3ZDZ, 3ZE0, 3ZE1, 3ZE2, 4Z7N, 4Z7O, 4Z7Q, 5HDB, 6V4P (+25 more)

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 (20): 274; 276; 278; 281; 283; 328; 330; 332; 334; 336; 396; 398 …

Post-translational modifications (1): 891

Disulfide bonds (9): 87–96, 138–161, 177–198, 504–515, 521–576, 633–639, 705–718, 857–921, 911–916

Glycosylation sites (7): 46, 280, 601, 711, 874, 878, 962

Mutagenesis-validated functional residues (1):

Position	Phenotype
1029–1030	imparts constitutive activity (ligand-binding) to alpha-iib/beta-3.

Function

Pathways and Gene Ontology

Reactome pathways

37 pathways

ID	Pathway
R-HSA-114608	Platelet degranulation
R-HSA-216083	Integrin cell surface interactions
R-HSA-3000178	ECM proteoglycans
R-HSA-354192	Integrin signaling
R-HSA-354194	GRB2:SOS provides linkage to MAPK signaling for Integrins
R-HSA-372708	p130Cas linkage to MAPK signaling for integrins
R-HSA-445144	Signal transduction by L1
R-HSA-5674135	MAP2K and MAPK activation
R-HSA-6802946	Signaling by moderate kinase activity BRAF mutants
R-HSA-6802948	Signaling by high-kinase activity BRAF mutants
R-HSA-6802952	Signaling by BRAF and RAF1 fusions
R-HSA-6802955	Paradoxical activation of RAF signaling by kinase inactive BRAF
R-HSA-8936459	RUNX1 regulates genes involved in megakaryocyte differentiation and platelet function
R-HSA-9649948	Signaling downstream of RAS mutants
R-HSA-9656223	Signaling by RAF1 mutants
R-HSA-9769733	Fibrin formation
R-HSA-109582	Hemostasis
R-HSA-1266738	Developmental Biology
R-HSA-1474244	Extracellular matrix organization
R-HSA-162582	Signal Transduction
R-HSA-1643685	Disease
R-HSA-212436	Generic Transcription Pathway
R-HSA-373760	L1CAM interactions
R-HSA-422475	Axon guidance
R-HSA-5663202	Diseases of signal transduction by growth factor receptors and second messengers
R-HSA-5673001	RAF/MAP kinase cascade
R-HSA-5683057	MAPK family signaling cascades
R-HSA-5684996	MAPK1/MAPK3 signaling
R-HSA-6802949	Signaling by RAS mutants
R-HSA-6802957	Oncogenic MAPK signaling

MSigDB gene sets: 309 (showing top): GOCC_SECRETORY_GRANULE, REACTOME_PLATELET_AGGREGATION_PLUG_FORMATION, REACTOME_PLATELET_ACTIVATION_SIGNALING_AND_AGGREGATION, MODULE_45, MODULE_64, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_UP, GOCC_CELL_SURFACE, MODULE_16, GOBP_REGULATION_OF_LEUKOCYTE_MIGRATION, GOBP_CELL_CELL_ADHESION, REACTOME_P130CAS_LINKAGE_TO_MAPK_SIGNALING_FOR_INTEGRINS, GOBP_LEUKOCYTE_MIGRATION, REACTOME_GRB2_SOS_PROVIDES_LINKAGE_TO_MAPK_SIGNALING_FOR_INTEGRINS, GOBP_POSITIVE_REGULATION_OF_LEUKOCYTE_MIGRATION

GO Biological Process (6): angiogenesis (GO:0001525), positive regulation of leukocyte migration (GO:0002687), cell-matrix adhesion (GO:0007160), integrin-mediated signaling pathway (GO:0007229), cell-cell adhesion (GO:0098609), cell adhesion (GO:0007155)

GO Molecular Function (7): signaling receptor activity (GO:0038023), identical protein binding (GO:0042802), metal ion binding (GO:0046872), extracellular matrix binding (GO:0050840), molecular adaptor activity (GO:0060090), fibrinogen binding (GO:0070051), protein binding (GO:0005515)

GO Cellular Component (10): plasma membrane (GO:0005886), focal adhesion (GO:0005925), external side of plasma membrane (GO:0009897), cell surface (GO:0009986), platelet alpha granule membrane (GO:0031092), extracellular exosome (GO:0070062), integrin alphaIIb-beta3 complex (GO:0070442), blood microparticle (GO:0072562), integrin complex (GO:0008305), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-11 pathways:

Category	Pathways
Oncogenic MAPK signaling	5
Extracellular matrix organization	2
Integrin signaling	2
Response to elevated platelet cytosolic Ca2+	1
Signal Transduction	1
Platelet Aggregation (Plug Formation)	1
L1CAM interactions	1
RAF/MAP kinase cascade	1
Transcriptional regulation by RUNX1	1
Signaling by RAS mutants	1
Coagulation pathway	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
binding	3
cellular anatomical structure	3
blood vessel morphogenesis	1
anatomical structure formation involved in morphogenesis	1
positive regulation of immune system process	1
regulation of leukocyte migration	1
positive regulation of cell migration	1
leukocyte migration	1
cell-substrate adhesion	1
cell surface receptor signaling pathway	1
cell adhesion	1
cellular process	1
molecular transducer activity	1
protein binding	1
cation binding	1
molecular_function	1
protein-containing complex binding	1
membrane	1
cell periphery	1
cell-substrate junction	1
plasma membrane	1
cell surface	1
side of membrane	1
secretory granule membrane	1
platelet alpha granule	1
extracellular vesicle	1
integrin complex	1
extracellular region	1
protein complex involved in cell adhesion	1
plasma membrane signaling receptor complex	1

Protein interactions and networks

STRING

2422 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
ITGA2B	VWF	P04275	999
ITGA2B	ITGB3	P05106	999
ITGA2B	FN1	P02751	995
ITGA2B	VTN	P01141	994
ITGA2B	ITGB2	P05107	968
ITGA2B	CIB1	Q99828	968
ITGA2B	GP1BA	P07359	948
ITGA2B	ICAM1	P05362	936
ITGA2B	CD40LG	P29965	933
ITGA2B	SELP	P16109	929
ITGA2B	GP9	P14770	914
ITGA2B	GP6	Q9HCN6	893
ITGA2B	CD36	P16671	892
ITGA2B	CD34	P28906	850
ITGA2B	ITGAM	P11215	813

IntAct

23 interactions, top by confidence:

A	B	Type	Score
ITGA2B	ITGB3	psi-mi:“MI:0407”(direct interaction)	0.810
ITGB3	ITGA2B	psi-mi:“MI:0915”(physical association)	0.810
ITGA2B	ITGB3	psi-mi:“MI:0915”(physical association)	0.810
ITGA2B	ITGA2B	psi-mi:“MI:0915”(physical association)	0.800
ITGA2B	ITGA2B	psi-mi:“MI:0407”(direct interaction)	0.800
ITGA2B	VWF	psi-mi:“MI:0407”(direct interaction)	0.440
	FN1	psi-mi:“MI:0914”(association)	0.350
CD177	MYO1G	psi-mi:“MI:0914”(association)	0.350
BMI1	HMGB1P1	psi-mi:“MI:0914”(association)	0.350
ITGA2B	ITGA2B	psi-mi:“MI:0915”(physical association)	0.000
ITGB3	ITGA2B	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (41): CIB1 (Two-hybrid), CIB1 (Reconstituted Complex), PLA2G4A (Reconstituted Complex), ITGB3 (Reconstituted Complex), ITGA2B (Affinity Capture-Western), ITGA2B (Reconstituted Complex), ITGB3 (Reconstituted Complex), ITGA2B (Affinity Capture-Western), ITGB3 (Co-crystal Structure), ITGB3 (Reconstituted Complex), GCN4 (Reconstituted Complex), GCN4 (Co-crystal Structure), ITGB3 (Affinity Capture-Western), ITGA2B (Affinity Capture-Western), ITGB3 (Reconstituted Complex)

ESM2 similar proteins: A0JND9, E1BPW0, O14773, O18956, O35795, O55026, O75173, O75355, O75356, O75578, O89023, O93295, P08514, P08648, P11688, P17405, P49961, P55772, P56201, P79784, P97687, Q04519, Q0VD19, Q12794, Q32M88, Q49HH9, Q49KI5, Q5DRK1, Q5IS74, Q5MY95, Q5RFL1, Q5RFQ8, Q60HH1, Q6P3E7, Q6P6S9, Q717C1, Q717C2, Q7RTX0, Q8BFW6, Q8BNJ2

Diamond homologs: A2ARA8, O70362, P06756, P08514, P08648, P11688, P12080, P26008, P26009, P34446, P43406, P53708, P53711, P80108, P80109, P80746, Q06274, Q27977, Q61739, Q86AV9, Q8R2H5, Q9QUM0, F1MMS9, O75578, P20701, P23229, P26006, P26007, P38570, Q00651, Q13683, Q13797, Q24247, Q60677, Q61738, Q63258, Q91687, Q9W1M8, A8X3A7, P17852

SIGNOR signaling

4 interactions.

A	Effect	B	Mechanism
GATA1	“up-regulates quantity by expression”	ITGA2B	“transcriptional regulation”
RUNX1	“up-regulates quantity by expression”	ITGA2B	“transcriptional regulation”
ITGA2B	“form complex”	“AIIB/b3 integrin”	binding
CIB1	“up-regulates activity”	ITGA2B	binding

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	156
Likely pathogenic	100
Uncertain significance	438
Likely benign	232
Benign	38

Top pathogenic / likely-pathogenic (30)

Variant ID	HGVS	Classification
1074062	NM_000419.5(ITGA2B):c.1253del (p.Gly418fs)	Pathogenic
1210178	NM_000419.5(ITGA2B):c.1232dup (p.Tyr411Ter)	Pathogenic
1210179	NM_000419.5(ITGA2B):c.2348+5G>C	Pathogenic
1210184	NM_000419.5(ITGA2B):c.1051C>T (p.Arg351Ter)	Pathogenic
1210189	NM_000419.5(ITGA2B):c.245dup (p.Gly83fs)	Pathogenic
1210190	NM_000419.5(ITGA2B):c.2015del (p.Gly672fs)	Pathogenic
1210196	NM_000419.5(ITGA2B):c.1608del (p.Asn536fs)	Pathogenic
1210197	NM_000419.5(ITGA2B):c.1460_1461insAGGT (p.Ser488fs)	Pathogenic
1210205	NM_000419.5(ITGA2B):c.1233C>A (p.Tyr411Ter)	Pathogenic
1210207	NM_000419.5(ITGA2B):c.2459del (p.Asn820fs)	Pathogenic
1330319	NM_000419.5(ITGA2B):c.2444_2445del (p.Thr814_Tyr815insTer)	Pathogenic
1330320	NM_000419.5(ITGA2B):c.2953C>T (p.Gln985Ter)	Pathogenic
1330328	NM_000419.5(ITGA2B):c.1993C>T (p.Gln665Ter)	Pathogenic
1330329	NM_000419.5(ITGA2B):c.727del (p.Leu243fs)	Pathogenic
1330330	NM_000419.5(ITGA2B):c.432G>A (p.Trp144Ter)	Pathogenic
1330342	NM_000419.5(ITGA2B):c.574+1G>A	Pathogenic
1330346	NM_000419.5(ITGA2B):c.625-1G>A	Pathogenic
1330347	NM_000419.5(ITGA2B):c.2421G>A (p.Trp807Ter)	Pathogenic
1684324	NM_000419.5(ITGA2B):c.138dup (p.Gly47fs)	Pathogenic
1687215	NM_000419.5(ITGA2B):c.21_22del (p.Leu8fs)	Pathogenic
1691463	NM_000419.5(ITGA2B):c.957T>A (p.Tyr319Ter)	Pathogenic
1691468	NM_000419.5(ITGA2B):c.2338del (p.Glu780fs)	Pathogenic
1691469	NM_000419.5(ITGA2B):c.1919_1920del (p.Val640fs)	Pathogenic
1691471	NM_000419.5(ITGA2B):c.3060G>A (p.Lys1020=)	Pathogenic
1691473	NM_000419.5(ITGA2B):c.2673_2674dup (p.Ile892fs)	Pathogenic
1691475	NM_000419.5(ITGA2B):c.2770C>T (p.Gln924Ter)	Pathogenic
1691485	NM_000419.5(ITGA2B):c.2902del (p.Tyr968fs)	Pathogenic
1691486	NM_000419.5(ITGA2B):c.2578C>T (p.Gln860Ter)	Pathogenic
1691491	NM_000419.5(ITGA2B):c.224del (p.Gly75fs)	Pathogenic
1703867	NM_000419.5(ITGA2B):c.337C>T (p.Gln113Ter)	Pathogenic

SpliceAI

4138 predictions. Top by Δscore:

Variant	Effect	Δscore
17:44375589:A:AC	donor_gain	1.0000
17:44375590:C:CC	donor_gain	1.0000
17:44375590:CTA:C	donor_gain	1.0000
17:44375827:TCTTA:T	donor_loss	1.0000
17:44375828:CTTA:C	donor_loss	1.0000
17:44375829:TTAC:T	donor_loss	1.0000
17:44375830:TA:T	donor_loss	1.0000
17:44375831:A:AC	donor_gain	1.0000
17:44375831:AC:A	donor_gain	1.0000
17:44375831:ACCT:A	donor_loss	1.0000
17:44375832:C:CC	donor_gain	1.0000
17:44375832:C:CT	donor_loss	1.0000
17:44375832:CC:C	donor_gain	1.0000
17:44375986:C:CC	acceptor_gain	1.0000
17:44376306:AC:A	donor_gain	1.0000
17:44376307:CC:C	donor_gain	1.0000
17:44377010:T:TA	donor_gain	1.0000
17:44377692:CCTCA:C	donor_loss	1.0000
17:44377693:CTCA:C	donor_loss	1.0000
17:44377694:TCACC:T	donor_loss	1.0000
17:44377695:CACC:C	donor_loss	1.0000
17:44377697:C:A	donor_loss	1.0000
17:44377802:C:CT	acceptor_gain	1.0000
17:44377803:A:T	acceptor_gain	1.0000
17:44377808:C:CT	acceptor_gain	1.0000
17:44377808:C:T	acceptor_gain	1.0000
17:44377809:A:T	acceptor_gain	1.0000
17:44378356:CCATA:C	donor_loss	1.0000
17:44378357:CATA:C	donor_loss	1.0000
17:44378358:ATACC:A	donor_loss	1.0000

AlphaMissense

6702 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
17:44378673:C:G	C639S	0.995
17:44378674:A:T	C639S	0.995
17:44377732:C:G	C718S	0.994
17:44377733:A:T	C718S	0.994
17:44378691:C:G	C633S	0.994
17:44378692:A:T	C633S	0.994
17:44380642:A:G	L466P	0.994
17:44377771:C:G	C705S	0.993
17:44377772:A:T	C705S	0.993
17:44378673:C:T	C639Y	0.992
17:44378674:A:G	C639R	0.992
17:44379795:T:G	D591A	0.991
17:44378691:C:T	C633Y	0.990
17:44385849:A:T	V128D	0.990
17:44377733:A:G	C718R	0.989
17:44377771:C:T	C705Y	0.989
17:44383930:C:T	G321E	0.989
17:44377772:A:G	C705R	0.988
17:44378417:A:G	L680P	0.988
17:44381055:G:T	A406E	0.988
17:44389322:C:T	G51E	0.988
17:44376382:G:C	N758K	0.987
17:44376382:G:T	N758K	0.987
17:44378672:A:C	C639W	0.987
17:44379796:C:G	D591H	0.987
17:44383634:C:A	G357W	0.987
17:44384348:A:T	V285D	0.987
17:44376090:A:C	Y815D	0.986
17:44377732:C:T	C718Y	0.986
17:44380928:A:C	F448L	0.986

dbSNP variants (sampled 300 via entrez): RS1000132610 (17:44384412 C>T), RS1000151886 (17:44385063 C>A,T), RS1000163641 (17:44384059 C>A,G), RS1000213828 (17:44372677 G>A), RS1000365515 (17:44382212 A>C,G), RS1000372157 (17:44377515 C>T), RS1000525625 (17:44388902 T>C), RS1000567414 (17:44372525 C>A,T), RS1000576229 (17:44388639 C>T), RS1000888535 (17:44377146 C>A,T), RS1001011632 (17:44377172 C>T), RS1001216412 (17:44374207 A>C), RS1001704288 (17:44388569 A>G), RS1001715074 (17:44373924 G>A,T), RS1001811356 (17:44386077 C>A,G,T)

Disease associations

OMIM: gene MIM:607759 | disease phenotypes: MIM:273800, MIM:187800, MIM:621266

GenCC curated gene-disease

Disease	Classification	Inheritance
Glanzmann’s thrombasthenia	Definitive	Autosomal recessive
platelet-type bleeding disorder 16	Strong	Autosomal dominant
Glanzmann thrombasthenia 1	Strong	Autosomal recessive
fetomaternal alloimmune thrombocytopenia 2	Strong	Autosomal dominant
autosomal dominant macrothrombocytopenia	Supportive	Autosomal dominant

ClinGen Gene-Disease Validity (2)

Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.

Disease	Classification	Inheritance
platelet-type bleeding disorder 16	Definitive	AD
Glanzmann thrombasthenia	Definitive	AR

Mondo (7): Glanzmann thrombasthenia (MONDO:0100326), platelet-type bleeding disorder 16 (MONDO:0008552), Glanzmann thrombasthenia 1 (MONDO:0031332), fetomaternal alloimmune thrombocytopenia 2 (MONDO:0980724), thrombocytopenia (MONDO:0002049), (MONDO:0010119), autosomal dominant macrothrombocytopenia (MONDO:0015372)

Orphanet (2): Glanzmann thrombasthenia (Orphanet:849), Autosomal dominant macrothrombocytopenia (Orphanet:140957)

HPO phenotypes

52 total (30 of 52 shown, HPO-id order):

HPO	Term
HP:0000006	Autosomal dominant inheritance
HP:0000007	Autosomal recessive inheritance
HP:0000132	Menorrhagia
HP:0000225	Gingival bleeding
HP:0000421	Epistaxis
HP:0000618	Blindness
HP:0000707	Abnormality of the nervous system
HP:0000790	Hematuria
HP:0000967	Petechiae
HP:0000978	Bruising susceptibility
HP:0000979	Purpura
HP:0001263	Global developmental delay
HP:0001873	Thrombocytopenia
HP:0001892	Abnormal bleeding
HP:0001902	Giant platelets
HP:0001903	Anemia
HP:0001975	Decreased platelet glycoprotein IIb-IIIa
HP:0002138	Subarachnoid hemorrhage
HP:0002170	Intracranial hemorrhage
HP:0002239	Gastrointestinal hemorrhage
HP:0002249	Melena
HP:0003010	Prolonged bleeding time
HP:0003540	Impaired platelet aggregation
HP:0003623	Neonatal onset
HP:0004406	Spontaneous, recurrent epistaxis
HP:0004809	Neonatal alloimmune thrombocytopenia
HP:0004846	Prolonged bleeding after surgery
HP:0004866	Impaired ADP-induced platelet aggregation
HP:0006298	Prolonged bleeding after dental extraction
HP:0007420	Spontaneous hematomas

GWAS associations

9 associations (top):

Study	Trait	p-value
GCST001337_52	Platelet count	2.000000e-08
GCST004599_124	Mean platelet volume	2.000000e-37
GCST004603_182	Platelet count	3.000000e-20
GCST004616_31	Platelet distribution width	2.000000e-16
GCST010703_292	Brain morphology (MOSTest)	1.000000e-14
GCST90002395_258	Mean platelet volume	6.000000e-76
GCST90002395_259	Mean platelet volume	3.000000e-20
GCST90002400_213	Plateletcrit	8.000000e-12
GCST90002402_454	Platelet count	7.000000e-53

EFO canonical traits (4, from GWAS)

EFO ID	Trait name
EFO:0004309	platelet count
EFO:0007984	platelet component distribution width
EFO:0004346	neuroimaging measurement
EFO:0007985	platelet crit

MeSH disease descriptors (3)

Descriptor	Name	Tree numbers
D013915	Thrombasthenia	C15.378.100.100.820; C15.378.140.810; C15.378.463.810; C16.320.099.820
D013921	Thrombocytopenia	C15.378.140.855; C15.378.243.937
C566061	Glanzmann Thrombasthenia, Autosomal Dominant (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (3): CHEMBL2093869 (PROTEIN COMPLEX), CHEMBL2111443 (SELECTIVITY GROUP), CHEMBL212 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

14 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 753,857 (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
CHEMBL1174	EPTIFIBATIDE	4	17,269
CHEMBL25	ASPIRIN	4	694,602
CHEMBL916	TIROFIBAN	4	16,908
CHEMBL273264	NAFAMOSTAT	3	7,063
CHEMBL429876	CILENGITIDE	3	10,123
CHEMBL108111	LAMIFIBAN	2	2,653
CHEMBL18301	ROXIFIBAN	2	822
CHEMBL3085474	FRADAFIBAN	2	925
CHEMBL356301	LOTRAFIBAN	2	964
CHEMBL435176	SIBRAFIBAN	2	1,159
CHEMBL64706	ORBOFIBAN	2	16
CHEMBL76098	XEMILOFIBAN	2	1,312
CHEMBL78871	GANTOFIBAN	2	11
CHEMBL87728	ELAROFIBAN	2	30

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

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs3760364	ITGA2B		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: catalytic receptor — Integrins

Binding affinities (BindingDB)

32 measured of 44 human assays (44 total across all organisms); most potent 32 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(S)-3-(3-Adamantan-1-yl-propionylamino)-6-[2-(4-carbamimidoyl-phenyl)-acetylamino]-hexanoic acid	IC50	0.37 nM
(S)-N-((S)-Adamantan-1-yl-carboxy-methyl)-3-{(S)-3-[2-(4-carbamimidoyl-phenyl)-acetylamino]-2-oxo-pyrrolidin-1-yl}-succinamic acid; TFA	IC50	2 nM
(S)-3-(2-Adamantan-1-yl-acetylamino)-6-[2-(4-carbamimidoyl-phenyl)-acetylamino]-hexanoic acid	IC50	2.2 nM
(3S)-3-[5-[2-[4-(2-fluoroethoxy)phenyl]ethyl]-3-pyridinyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	3 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(3S)-3-[5-[2-[3-(2-fluoroethoxy)phenyl]ethyl]-3-pyridinyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	3 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(3S)-3-[5-[2-[4-(2-fluoroethoxy)phenyl]ethynyl]-3-pyridinyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	5 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(S)-N-((S)-2-Adamantan-1-yl-1-carboxy-ethyl)-3-{(S)-3-[2-(4-carbamimidoyl-phenyl)-acetylamino]-2-oxo-pyrrolidin-1-yl}-succinamic acid; TFA	IC50	5 nM
(3S)-3-[5-[2-[3-(2-fluoroethoxy)phenyl]ethynyl]-3-pyridinyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	6 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(3S)-3-[5-[(4-cyano-3-fluorophenyl)methoxy]-3-pyridinyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	7 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(3S)-3-[5-[(E)-2-[3-(2-fluoroethoxy)phenyl]ethenyl]-3-pyridinyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	7 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(3S)-3-[5-[(3-cyano-4-fluorophenyl)methoxy]-3-pyridinyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	8 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(3S)-3-[5-[4-(2-fluoroethoxy)phenyl]-3-pyridinyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	11 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
RP-444	IC50	13 nM
(3S)-3-[5-[2-(2-fluoroethoxy)phenyl]-3-pyridinyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	14 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(3S)-3-[5-(4-fluoro-3-nitrophenyl)-3-pyridinyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	14 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(3S)-3-[5-(4-cyano-3-fluorophenyl)-3-pyridinyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	15 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(3S)-3-(4-cyano-3-fluorophenyl)-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	15 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(3S)-3-[5-[2-[2-(2-fluoroethoxy)ethoxy]ethoxy]-3-pyridinyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	16 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(3S)-3-[5-[3-(2-fluoroethoxy)phenyl]-3-pyridinyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	16 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(3S)-3-[5-(2-fluoroethoxy)-3-pyridinyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	20 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(S)-N-((S)-2-Adamantan-1-yl-1-methoxycarbonyl-ethyl)-3-{(S)-3-[2-(4-carbamimidoyl-phenyl)-acetylamino]-2-oxo-pyrrolidin-1-yl}-succinamic acid; TFA	IC50	20 nM
(3S)-3-[5-(3-cyano-4-fluorophenyl)-3-pyridinyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	21 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(3S)-3-[4-(2-fluoroethoxy)phenyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	29 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(3S)-3-[3-fluoro-5-[4-(2-fluoroethoxy)phenyl]phenyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	35 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(3S)-3-[3-[2-[2-(2-fluoroethoxy)ethoxy]ethoxy]phenyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	84 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(S)-N-Adamantan-1-ylmethyl-3-{2-[3-(4-carbamimidoyl-phenyl)-4,5-dihydro-isoxazol-5-yl]-acetylamino}-succinamic acid; TFA	IC50	95 nM
(3S)-3-[3-(2-fluoroethoxy)phenyl]-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	IC50	101 nM	US-9744252: Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
(S)-N-Adamantan-2-yl-3-{2-[3-(4-carbamimidoyl-phenyl)-4,5-dihydro-isoxazol-5-yl]-acetylamino}-succinamic acid; TFA	IC50	140 nM
2-((S)-(1R,7S)-7,7-Dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-3-{4-[2-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-ethyl]-benzoylamino}-propionic acid	IC50	157 nM
(S)-2-(Adamantan-1-ylmethoxycarbonylamino)-3-{[5-(3-guanidino-3-oxo-propyl)-thiophene-2-carbonyl]-amino}-propionic acid	IC50	480 nM
(S)-N-((S)-2-Adamantan-1-yl-1-methoxycarbonyl-ethyl)-3-[(S)-3-((S)-2-benzyloxycarbonylamino-5-guanidino-pentanoylamino)-2-oxo-pyrrolidin-1-yl]-succinamic acid; TFA	IC50	510 nM
[3-(2-tert-Butoxycarbonylamino-6-isopropylamino-hexanoylamino)-adamantan-1-ylamino]-acetic acid	IC50	29900 nM

ChEMBL bioactivities

2424 potent at pChembl≥5 of 2773 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.80	IC50	0.016	nM	CHEMBL315008
10.64	IC50	0.023	nM	CHEMBL1782661
10.64	Kd	0.023	nM	CHEMBL293601
10.59	Kd	0.026	nM	CHEMBL80432
10.57	IC50	0.027	nM	CHEMBL421547
10.52	ED50	0.03	nM	CHEMBL293601
10.40	ED50	0.04	nM	CHEMBL94393
10.40	ED50	0.04	nM	CHEMBL78503
10.40	ED50	0.04	nM	CHEMBL78517
10.39	IC50	0.041	nM	CHEMBL329015
10.37	IC50	0.043	nM	CHEMBL329871
10.33	ED50	0.047	nM	CHEMBL78760
10.33	Ki	0.0465	nM	CHEMBL8572
10.25	ED50	0.056	nM	CHEMBL57040
10.25	Kd	0.056	nM	CHEMBL57040
10.24	IC50	0.057	nM	CHEMBL88944
10.22	ED50	0.06	nM	CHEMBL327216
10.22	IC50	0.06	nM	ELAROFIBAN
10.21	IC50	0.061	nM	CHEMBL328528
10.17	IC50	0.068	nM	CHEMBL88826
10.15	ED50	0.07	nM	CHEMBL92091
10.15	ED50	0.07	nM	CHEMBL96788
10.15	ED50	0.07	nM	CHEMBL310964
10.15	Kd	0.07	nM	CHEMBL78760
10.14	IC50	0.073	nM	CHEMBL128906
10.10	ED50	0.08	nM	CHEMBL298655
10.10	Kd	0.08	nM	CHEMBL298655
10.10	ED50	0.08	nM	CHEMBL78570
10.10	Kd	0.08	nM	CHEMBL311048
10.05	Kd	0.09	nM	CHEMBL293601
10.05	ED50	0.09	nM	CHEMBL80432
10.05	IC50	0.09	nM	CHEMBL8501
10.05	IC50	0.09	nM	CHEMBL8572
10.04	Kd	0.092	nM	CHEMBL78517
10.01	IC50	0.098	nM	CHEMBL129877
10.00	IC50	0.1	nM	CHEMBL80623
10.00	IC50	0.1	nM	CHEMBL79087
10.00	ED50	0.099	nM	CHEMBL96097
10.00	IC50	0.1	nM	CHEMBL146766
10.00	IC50	0.1	nM	CHEMBL358487
10.00	Ki	0.1	nM	CHEMBL2370493
9.96	ED50	0.11	nM	CHEMBL311048
9.92	ED50	0.12	nM	CHEMBL40502
9.92	ED50	0.12	nM	CHEMBL300525
9.92	IC50	0.12	nM	CHEMBL89424
9.92	IC50	0.12	nM	CHEMBL323649
9.92	IC50	0.12	nM	CHEMBL131823
9.92	ED50	0.12	nM	CHEMBL80381
9.92	IC50	0.12	nM	CHEMBL7997
9.89	ED50	0.13	nM	CHEMBL96174

PubChem BioAssay actives

2056 with measured affinity, of 3151 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-(phenylmethoxycarbonylamino)-3-[[3-[(E)-2-piperidin-4-ylethenyl]-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridine-8-carbonyl]amino]propanoic acid	92831: Inhibition of thrombin-induced human gel-filtered platelet aggregation	ic50	<0.0001	uM
(2S)-2-[(4-chlorophenyl)sulfonylamino]-3-[[2-(2-piperidin-4-ylethyl)thieno[2,3-b]thiophene-5-carbonyl]amino]propanoic acid	73144: Equilibrium dissociation constant was measured from displacement of L-762,745 from Fibrinogen receptor of human platelets by flow cytometry	kd	<0.0001	uM
(2S)-2-(phenylmethoxycarbonylamino)-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	92831: Inhibition of thrombin-induced human gel-filtered platelet aggregation	ic50	<0.0001	uM
(2S)-2-(benzylsulfonylamino)-3-[[3-[(E)-2-piperidin-4-ylethenyl]-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridine-8-carbonyl]amino]propanoic acid	92831: Inhibition of thrombin-induced human gel-filtered platelet aggregation	ic50	<0.0001	uM
(2S)-2-(benzenesulfonamido)-3-[[5-[4-(diaminomethylideneamino)phenyl]thiophene-2-carbonyl]amino]propanoic acid;2,2,2-trifluoroacetic acid	218638: Inhibition of fibrinogen binding to integrin alphaIIb-beta3	ic50	<0.0001	uM
(2S)-2-(benzenesulfonamido)-3-[[5-[2-[(diaminomethylideneamino)methyl]phenyl]thiophene-2-carbonyl]amino]propanoic acid;2,2,2-trifluoroacetic acid	218638: Inhibition of fibrinogen binding to integrin alphaIIb-beta3	ic50	<0.0001	uM
(2S)-2-(benzenesulfonamido)-3-[[3-chloro-4-[4-(1,4,5,6-tetrahydropyrimidin-2-ylamino)piperidin-1-yl]benzoyl]amino]propanoic acid	600450: Antagonist activity at alpha2bbeta3 integrin receptor	ic50	<0.0001	uM
3-[2-(4-carbamimidoylbenzoyl)imino-3,4-dimethyl-1,3-thiazol-5-yl]propanoic acid	219096: Affinity for purified activated GPIIb/IIIa fibrinogen receptor by ELISA	ki	<0.0001	uM
(3S)-3-[[3-(2-piperidin-4-ylethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridine-8-carbonyl]amino]-3-pyridin-3-ylpropanoic acid	92831: Inhibition of thrombin-induced human gel-filtered platelet aggregation	ic50	<0.0001	uM
(2S)-2-(benzenesulfonamido)-3-[[2-(2-piperidin-4-ylethyl)thieno[2,3-b]thiophene-5-carbonyl]amino]propanoic acid	73144: Equilibrium dissociation constant was measured from displacement of L-762,745 from Fibrinogen receptor of human platelets by flow cytometry	kd	<0.0001	uM
2-[(3S)-6-[[4-(morpholine-4-carboximidoyl)benzoyl]amino]-3,4-dihydro-2H-chromen-3-yl]acetic acid	73134: Inhibition of Fibrinogen binding to Immobilized Human Fibrinogen Receptor.	ic50	0.0001	uM
(3S)-3-[[3-[(E)-2-piperidin-4-ylethenyl]-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridine-8-carbonyl]amino]-3-pyridin-3-ylpropanoic acid	92831: Inhibition of thrombin-induced human gel-filtered platelet aggregation	ic50	0.0001	uM
(2S)-2-(benzenesulfonamido)-3-[[2-(2-piperidin-4-ylethyl)thieno[3,2-b]thiophene-5-carbonyl]amino]propanoic acid	33000: Dissociation constant for alpha IIb beta-3 integrin rested platelets	kd	0.0001	uM
2-[(5S,11S,14S)-11-[3-(diaminomethylideneamino)propyl]-14-ethyl-12-methyl-4,7,10,13,16-pentaoxo-3,6,9,12,15-pentazabicyclo[15.3.1]henicosa-1(21),17,19-trien-5-yl]acetic acid	33003: Dissociation constant for [3H]-DMP728 binding to alphaIIb beta III integrin	ki	0.0001	uM
2-[7-[(4-carbamimidoylbenzoyl)amino]-1,2,3,4-tetrahydronaphthalen-2-yl]acetic acid	73134: Inhibition of Fibrinogen binding to Immobilized Human Fibrinogen Receptor.	ic50	0.0001	uM
2-[6-[[4-(N’-prop-2-ynylcarbamimidoyl)benzoyl]amino]-3,4-dihydro-2H-chromen-3-yl]acetic acid	73134: Inhibition of Fibrinogen binding to Immobilized Human Fibrinogen Receptor.	ic50	0.0001	uM
(3S)-3-(6-chloro-3-pyridinyl)-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	73015: In vitro inhibition of biotinylated fibrinogen binding to immobilized fibrinogen receptor.	ic50	0.0001	uM
(2S)-3-[[2-(2-piperidin-4-ylethyl)thieno[2,3-b]thiophene-5-carbonyl]amino]-2-(thiophen-2-ylsulfonylamino)propanoic acid	73144: Equilibrium dissociation constant was measured from displacement of L-762,745 from Fibrinogen receptor of human platelets by flow cytometry	kd	0.0001	uM
(3S)-3-(6-methyl-3-pyridinyl)-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	73015: In vitro inhibition of biotinylated fibrinogen binding to immobilized fibrinogen receptor.	ic50	0.0001	uM
2-[7-[[4-(morpholine-4-carboximidoyl)benzoyl]amino]-1,2,3,4-tetrahydronaphthalen-2-yl]acetic acid	73134: Inhibition of Fibrinogen binding to Immobilized Human Fibrinogen Receptor.	ic50	0.0001	uM
(2S)-3-[[2-(2-piperidin-4-ylethyl)thieno[3,2-b]thiophene-5-carbonyl]amino]-2-(pyridin-3-ylsulfonylamino)propanoic acid	73148: Displacement of L-762,745 from Fibrinogen Receptor of human platelets by flow cytometry	kd	0.0001	uM
2-[6-[(4-carbamimidoylbenzoyl)amino]-3,4-dihydro-2H-chromen-3-yl]acetic acid	73134: Inhibition of Fibrinogen binding to Immobilized Human Fibrinogen Receptor.	ic50	0.0001	uM
2-[7-[[4-(N’-propylcarbamimidoyl)benzoyl]amino]-1,2,3,4-tetrahydronaphthalen-2-yl]acetic acid	73134: Inhibition of Fibrinogen binding to Immobilized Human Fibrinogen Receptor.	ic50	0.0001	uM
(2S)-3-[[2-(2-piperidin-4-ylethyl)thieno[3,2-b]thiophene-5-carbonyl]amino]-2-(thiophen-2-ylsulfonylamino)propanoic acid	73144: Equilibrium dissociation constant was measured from displacement of L-762,745 from Fibrinogen receptor of human platelets by flow cytometry	kd	0.0001	uM
3-[[3-benzyl-2-(4-carbamimidoylbenzoyl)imino-4-methyl-1,3-thiazole-5-carbonyl]amino]propanoic acid	219092: Affinity for purified activated GPIIb/IIIa fibrinogen receptor in ELISA	ic50	0.0001	uM
3-[[3-butyl-2-(4-carbamimidoylbenzoyl)imino-4-methyl-1,3-thiazole-5-carbonyl]amino]propanoic acid	219092: Affinity for purified activated GPIIb/IIIa fibrinogen receptor in ELISA	ic50	0.0001	uM
(2S)-2-[(4-methylphenyl)sulfonylamino]-3-[[4-oxo-5-(2-piperidin-4-ylethyl)-7,8-dihydro-6H-pyrazolo[1,5-a][1,4]diazepine-2-carbonyl]amino]propanoic acid	220879: Competition with [1251]L-692,884 for binding to purified alpha IIb/beta3 integrin, activated by coating onto yttrium silicate scintillation proximity assay fluomicrospheres.	kd	0.0001	uM
(2S)-2-(benzenesulfonamido)-3-[[5-(2-piperidin-4-ylethoxy)-1H-indole-2-carbonyl]amino]propanoic acid	220879: Competition with [1251]L-692,884 for binding to purified alpha IIb/beta3 integrin, activated by coating onto yttrium silicate scintillation proximity assay fluomicrospheres.	kd	0.0001	uM
2-[6-[[4-(morpholine-4-carboximidoyl)benzoyl]amino]-3,4-dihydro-2H-chromen-3-yl]acetic acid	73134: Inhibition of Fibrinogen binding to Immobilized Human Fibrinogen Receptor.	ic50	0.0001	uM
(3S)-3-[[3-[(E)-2-piperidin-4-ylethenyl]-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridine-8-carbonyl]amino]-3-quinolin-3-ylpropanoic acid	92831: Inhibition of thrombin-induced human gel-filtered platelet aggregation	ic50	0.0001	uM
(3S)-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]-3-pyridin-3-ylpropanoic acid	241901: Inhibition of human Biotinylated Fg binding to immobilized Alpha II beta-3	ic50	0.0001	uM
3-[[2-(4-carbamimidoylbenzoyl)imino-3-ethyl-4-methyl-1,3-thiazole-5-carbonyl]amino]propanoic acid	219092: Affinity for purified activated GPIIb/IIIa fibrinogen receptor in ELISA	ic50	0.0001	uM
(2S)-3-[[3-[(E)-2-piperidin-4-ylethenyl]-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridine-8-carbonyl]amino]-2-[(2-pyridin-3-ylacetyl)amino]propanoic acid	92831: Inhibition of thrombin-induced human gel-filtered platelet aggregation	ic50	0.0001	uM
(3R)-3-(5-chlorothiophen-2-yl)-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	73015: In vitro inhibition of biotinylated fibrinogen binding to immobilized fibrinogen receptor.	ic50	0.0001	uM
(3R)-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]-3-thiophen-2-ylpropanoic acid	73015: In vitro inhibition of biotinylated fibrinogen binding to immobilized fibrinogen receptor.	ic50	0.0001	uM
(2S)-2-(phenylmethoxycarbonylamino)-3-[[3-(2-piperidin-4-ylethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridine-8-carbonyl]amino]propanoic acid	92831: Inhibition of thrombin-induced human gel-filtered platelet aggregation	ic50	0.0001	uM
(2S)-3-[[2-(2-piperidin-4-ylethyl)thieno[2,3-b]thiophene-5-carbonyl]amino]-2-(pyridin-3-ylsulfonylamino)propanoic acid	33000: Dissociation constant for alpha IIb beta-3 integrin rested platelets	kd	0.0001	uM
(2S)-3-[[3-fluoro-4-[4-(1,4,5,6-tetrahydropyrimidin-2-ylamino)piperidin-1-yl]benzoyl]amino]-2-[(4-hydroxyphenyl)sulfonylamino]propanoic acid	600450: Antagonist activity at alpha2bbeta3 integrin receptor	ic50	0.0002	uM
2-[7-[[4-[N’-(furan-2-ylmethyl)carbamimidoyl]benzoyl]amino]-1,2,3,4-tetrahydronaphthalen-2-yl]acetic acid	73134: Inhibition of Fibrinogen binding to Immobilized Human Fibrinogen Receptor.	ic50	0.0002	uM
3-[(2S)-1-[2-[(4-carbamimidoylbenzoyl)amino]acetyl]-4-(carboxymethyl)-3-oxopiperazin-2-yl]propanoic acid	73008: Ability to inhibit binding of biotin-labeled human fibrinogen to immobilized fibrinogen receptor purified from human erythroleukemia (HEL) cells.	ic50	0.0002	uM
(3R)-5-phenyl-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]pent-4-ynoic acid	73015: In vitro inhibition of biotinylated fibrinogen binding to immobilized fibrinogen receptor.	ic50	0.0002	uM
(3R)-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]-3-quinolin-3-ylpropanoic acid	73015: In vitro inhibition of biotinylated fibrinogen binding to immobilized fibrinogen receptor.	ic50	0.0002	uM
2-[7-[[4-(N’-prop-2-ynylcarbamimidoyl)benzoyl]amino]-1,2,3,4-tetrahydronaphthalen-2-yl]acetic acid	73134: Inhibition of Fibrinogen binding to Immobilized Human Fibrinogen Receptor.	ic50	0.0002	uM
(3S)-3-(5-ethynyl-3-pyridinyl)-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	73015: In vitro inhibition of biotinylated fibrinogen binding to immobilized fibrinogen receptor.	ic50	0.0002	uM
(3S)-3-(5-bromo-3-pyridinyl)-3-[[(3R)-1-(3-piperidin-4-ylpropanoyl)piperidine-3-carbonyl]amino]propanoic acid	73015: In vitro inhibition of biotinylated fibrinogen binding to immobilized fibrinogen receptor.	ic50	0.0002	uM
3-(1,3-benzodioxol-5-yl)-3-[[4-(2,3-dihydro-1H-isoindol-5-ylamino)-4-oxobutanoyl]amino]propanoic acid	493882: Antagonist activity at FITC-tagged alpha3beta3 integrin in human platelet assessed as reduction of ADP-induced platelet aggregation	ic50	0.0002	uM
(2S)-2-(benzenesulfonamido)-3-[3-(1,2,3,4-tetrahydroisoquinoline-7-carbonylamino)propanoylamino]propanoic acid;hydrochloride	1251257: Inhibition of FITC-labeled fibrinogen binding to integrin alpha2bbeta3 open form in human washed platelets	ic50	0.0002	uM
(2S)-3-[[5-[3-[(diaminomethylideneamino)methyl]phenyl]thiophene-2-carbonyl]amino]-2-[(2,4,6-trimethylphenyl)sulfonylamino]propanoic acid;2,2,2-trifluoroacetic acid	218638: Inhibition of fibrinogen binding to integrin alphaIIb-beta3	ic50	0.0002	uM
(3R)-3-(1,3-benzodioxol-5-yl)-3-[[(3R)-1-[3-(1-methylpiperidin-4-yl)propanoyl]piperidine-3-carbonyl]amino]propanoic acid	73015: In vitro inhibition of biotinylated fibrinogen binding to immobilized fibrinogen receptor.	ic50	0.0002	uM
(2S)-2-(benzenesulfonamido)-3-[[4-(2-piperidin-4-ylethoxy)benzoyl]amino]propanoic acid	220879: Competition with [1251]L-692,884 for binding to purified alpha IIb/beta3 integrin, activated by coating onto yttrium silicate scintillation proximity assay fluomicrospheres.	kd	0.0002	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Aspirin	decreases reaction, increases expression, decreases expression, affects binding	3
(+)-JQ1 compound	decreases expression	2
Benzo(a)pyrene	affects methylation, decreases expression	2
Dactinomycin	affects cotreatment, increases expression	2
Tetradecanoylphorbol Acetate	decreases reaction, increases expression, increases reaction	2
aristolochic acid I	increases expression	1
triphenyl phosphate	affects expression	1
diphenyleneiodonium	decreases reaction, increases expression	1
6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid	decreases reaction, increases expression	1
hydroxyhydroquinone	increases expression	1
11-nor-delta(9)-tetrahydrocannabinol-9-carboxylic acid	affects methylation, increases abundance	1
anagrelide	decreases reaction, increases expression	1
benzo(e)pyrene	increases methylation	1
aflatoxin B2	decreases methylation, increases methylation	1
2,3,4,7,8-pentachlorodibenzofuran	decreases expression	1
methyllycaconitine	affects binding, decreases activity, decreases expression	1
acetovanillone	decreases reaction, increases expression	1
di-n-butylphosphoric acid	affects expression	1
alpha-cyano-(3,4-dihydroxy)-N-benzylcinnamide	decreases reaction, increases expression	1
SR 121566	decreases activity, affects binding	1
N(6)-methyl-2’-deoxyadenosine 3’,5’-diphosphate	affects binding, decreases reaction, increases expression, increases reaction	1
U 0126	decreases reaction, increases expression	1
cangrelor	increases expression, increases reaction, affects binding, decreases reaction	1
pyrazolanthrone	increases expression, increases reaction	1
nutlin 3	affects cotreatment, increases expression	1
abrine	decreases expression	1
3-hydrogenkwadaphnin	increases expression	1
jinfukang	affects cotreatment, increases expression	1
10-(4’-(N-diethylamino)butyl)-2-chlorophenoxazine	increases expression, decreases reaction	1
tablysin-15, Tabanus yao	affects binding	1

ChEMBL screening assays

407 unique, capped per target: 246 binding, 159 functional, 2 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1029026	Binding	Binding affinity to human integrin alpha2beta3 receptor by TRF assay	Synthesis and initial evaluation of novel, non-peptidic antagonists of the alpha(v)-integrins alpha(v)beta(3) and alpha(v)beta(5). — Bioorg Med Chem Lett
CHEMBL1211820	Functional	Antagonist activity at FITC-tagged alpha3beta3 integrin in human platelet rich plasma	Derivatives of tetrahydroisoquinoline: synthesis and initial evaluation of novel non-peptide antagonists of the alpha(IIb)beta(3)-integrin. — Bioorg Med Chem Lett
CHEMBL4375068	ADMET	Inhibition of human fibronectin binding to human Integrin alpha2b beta3 receptor incubated for 1 hr by ELISA	Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling. — J Med Chem

Cellosaurus cell lines

10 cell lines: 10 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_D8NH	Ubigene HCT 116 ITGA2B KO	Cancer cell line	Male
CVCL_E2T9	HP-alphaIIbbeta3	Cancer cell line	Female
CVCL_E2TE	HP-1b	Cancer cell line	Female
CVCL_E2TF	HP-3b	Cancer cell line	Female
CVCL_E2TG	HP-4b	Cancer cell line	Female
CVCL_E2TI	HP-6b	Cancer cell line	Female
CVCL_E2TJ	HP-7 variant	Cancer cell line	Female
CVCL_E2TK	HP-7b	Cancer cell line	Female
CVCL_ST23	HAP1 ITGA2B (-) 1	Cancer cell line	Male
CVCL_ST24	HAP1 ITGA2B (-) 2	Cancer cell line	Male

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00039858	PHASE4	COMPLETED	Evaluation of Argatroban Injection in Pediatric Patients Requiring Anticoagulant Alternatives to Heparin
NCT00239733	PHASE4	TERMINATED	Anti-D for Treating Thrombocytopenia in Adults Infected With Hepatitis C Virus With or Without HIV Co-Infection
NCT00907478	PHASE4	COMPLETED	Study on Bone Marrow Morphology in Adults Receiving Romiplostim for Treatment of Thrombocytopenia Associated With Immune Thrombocytopenia Purpura (ITP)
NCT01727401	PHASE4	TERMINATED	Thromboprophylaxis of Venous Thromboembolism in Acutely-ill Medical Inpatients With Thrombocytopenia
NCT02032134	PHASE4	TERMINATED	Protocol for the Infusion of Buffy Coat-derived Cryopreserved Platelets in Patients With Severe Thrombocytopenia
NCT02267993	PHASE4	COMPLETED	Efficacy and Safety of rhTPO for the Treatment of Thrombocytopenia After Chemotherapy in AML Patients
NCT03633019	PHASE4	UNKNOWN	High-dose Use of rhTPO in CIT Patients
NCT03688191	PHASE4	UNKNOWN	Study of Sirolimus in CTD-TP in China
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