ChEMBL ligand: CHEMBL916 (Aggrastat, Agrastat, L-700462, MK-383, Tirofiban)
integrin, beta 3 subunit (platelet glycoprotein IIIa, antigen CD61)/integrin, alpha IIb subunit (platelet glycoprotein IIb of IIb/IIIa complex, antigen CD41)/Integrin alpha-IIb/beta-3 in Human [ChEMBL: CHEMBL2093869] [GtoPdb: 2457, 2441] [UniProtKB: P05106, P08514] There should be some charts here, you may need to enable JavaScript!
integrin, beta 3 subunit (platelet glycoprotein IIIa, antigen CD61)/integrin, alpha V subunit/Integrin alpha-V/beta-3 in Human [ChEMBL: CHEMBL1907598] [GtoPdb: 2457, 2453] [UniProtKB: P05106, P06756] There should be some charts here, you may need to enable JavaScript!
Integrin subunit alpha 2b/beta-3 in Rat [ChEMBL: CHEMBL4296069] [UniProtKB: D3ZAC0, Q8R2H2] There should be some charts here, you may need to enable JavaScript!
integrin αIIbβ3 in Human [GtoPdb: 2579] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
integrin, beta 3 subunit (platelet glycoprotein IIIa, antigen CD61)/integrin, alpha IIb subunit (platelet glycoprotein IIb of IIb/IIIa complex, antigen CD41)/Integrin alpha-IIb/beta-3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2093869] [GtoPdb: 2457, 2441] [UniProtKB: P05106, P08514]
ChEMBL	Equilibrium dissociation constant was measured from displacement of L-762,745 from Fibrinogen receptor of human platelets by flow cytometry	B	7.82	pKd	15	nM	Kd	J Med Chem (1999) 42: 2409-2421 [PMID:10395482]
ChEMBL	Binding affinity against alpha IIb beta-3 integrin in the presence of L-736622.	B	7.89	pKd	13	nM	Kd	Bioorg Med Chem Lett (1996) 6: 2519-2524
ChEMBL	Binding affinity to resting form of alpha IIb/beta3 integrin by flow cytometry using fluorescein ligand L-726,745 displacement from human platelets.	B	7.89	pKd	13	nM	Kd	Bioorg Med Chem Lett (2000) 10: 1943-1948 [PMID:10987423]
ChEMBL	Competition with [1251]L-692,884 for binding to purified alpha IIb/beta3 integrin, activated by coating onto yttrium silicate scintillation proximity assay fluomicrospheres.	B	8.72	pKd	1.9	nM	Kd	Bioorg Med Chem Lett (2000) 10: 1943-1948 [PMID:10987423]
ChEMBL	Inhibition of fibrinogen binding to human alpha2b/beta3 integrin after 1 hr by ELISA	B	5.62	pIC50	2400	nM	IC50	J Med Chem (2014) 57: 5829-5834 [PMID:24949551]
ChEMBL	Binding affinity to alpha2b/beta3 integrin (unknown origin)	B	6.22	pIC50	600	nM	IC50	J Med Chem (2014) 57: 5829-5834 [PMID:24949551]
ChEMBL	Antagonist activity at GP2b/GP3a receptor in human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 1 min followed by ADP addition by aggregometric method	B	7.05	pIC50	90	nM	IC50	Eur J Med Chem (2017) 125: 197-209 [PMID:27662032]
ChEMBL	Displacement of fibrinogen from human platelet GP2b/GP3a receptor after 2 hrs by ELISA	B	7.4	pIC50	40	nM	IC50	Eur J Med Chem (2017) 125: 197-209 [PMID:27662032]
ChEMBL	Inhibition of platelet aggregation	F	7.45	pIC50	35.7	nM	IC50	J Med Chem (2000) 43: 3453-3473 [PMID:10999999]
ChEMBL	Antagonist activity against integrin alpha2bbeta3 closed form in human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation	B	7.49	pIC50	32	nM	IC50	J Med Chem (2015) 58: 7681-7694 [PMID:26367138]
ChEMBL	Antagonist activity against integrin alpha2bbeta3 open form in human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation	B	7.49	pIC50	32	nM	IC50	J Med Chem (2015) 58: 7681-7694 [PMID:26367138]
ChEMBL	Inhibition of aggregation of human gel-filtered platelets measured by light transmittance method at 37 degrees C.	F	7.82	pIC50	15	nM	IC50	Bioorg Med Chem Lett (2000) 10: 1943-1948 [PMID:10987423]
ChEMBL	Inhibition of human alphaIIb-beta3 integrin in platelet aggregation assay	B	7.82	pIC50	15	nM	IC50	J Med Chem (2003) 46: 5316-5325 [PMID:14640540]
ChEMBL	The compound was tested in vivo for the inhibition of aggregation of human gel-filtered platelets(GFP)	F	7.96	pIC50	11	nM	IC50	J Med Chem (1999) 42: 2409-2421 [PMID:10395482]
ChEMBL	In vitro inhibition of ADP-mediated human gel filtered platelet aggregation.	F	7.96	pIC50	11	nM	IC50	J Med Chem (1992) 35: 4640-4642 [PMID:1469694]
ChEMBL	Inhibition of ADP-mediated platelet aggregation in human gel-filtered platelets	F	8	pIC50	10	nM	IC50	Bioorg Med Chem Lett (1994) 4: 1835-1840
ChEMBL	Antagonist activity at alpha2bbeta3 in human HEL cells assessed as reduction in cell adhesion to fibrinogen pre-incubated for 30 mins before fibrinogen and further incubated for 1 hr by nitrophenyl-N-acetyl-beta-D-glucosaminide substrate based chromogenic assay	B	8.03	pIC50	9.4	nM	IC50	J Med Chem (2016) 59: 9721-9742 [PMID:27726366]
ChEMBL	Compound was evaluated for inhibition against Fibrinogen Receptor.	B	8.05	pIC50	9	nM	IC50	J Med Chem (1998) 41: 2068-2075 [PMID:9622548]
ChEMBL	Inhibition of platelet aggregation as the concentration necessary to inhibit the change in light.	F	8.05	pIC50	9	nM	IC50	J Med Chem (1994) 37: 2537-2551 [PMID:8057299]
ChEMBL	Inhibition of fibrinogen binding to alpha2bbeta3 isolated from human HEL cells incubated for 1 hr by scintillation-proximity assay based competitive solid-phase binding assay	B	8.14	pIC50	7.3	nM	IC50	J Med Chem (2016) 59: 9721-9742 [PMID:27726366]
ChEMBL	Inhibition of [125I]fibrinogen binding to fibrinogen receptor	B	8.3	pIC50	5	nM	IC50	J Med Chem (1992) 35: 4640-4642 [PMID:1469694]
ChEMBL	Inhibition of FITC-labeled fibrinogen binding to integrin alpha2bbeta3 open form in human washed platelets	B	8.62	pIC50	2.4	nM	IC50	J Med Chem (2015) 58: 7681-7694 [PMID:26367138]
ChEMBL	Inhibition of FITC-labeled fibrinogen binding to integrin alpha2bbeta3 receptor in human platelets by flow cytometry	B	8.62	pIC50	2.4	nM	IC50	Bioorg Med Chem (2013) 21: 4646-4661 [PMID:23757209]
ChEMBL	Inhibition of FITC-labeled fibrinogen binding to integrin alpha2bbeta3 closed form in human washed platelets	B	8.62	pIC50	2.4	nM	IC50	J Med Chem (2015) 58: 7681-7694 [PMID:26367138]
ChEMBL	Inhibition of FITC-labelled fibrinogen binding to integrin alpha2b beta3 receptor in human platelet cells	B	8.72	pIC50	1.9	nM	IC50	Bioorg Med Chem Lett (2016) 26: 1839-1843 [PMID:26912112]
ChEMBL	Inhibition of fibrinogen binding to human platelet integrin alpha2b beta3 by ELISA based solid phase binding assay	B	8.92	pIC50	1.2	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127039-127039 [PMID:32094009]
ChEMBL	Displacement of extracellular matrix protein fibrinogen from human integrin alpha2bbeta3 after 1 hr by competitive ELISA	B	9.02	pIC50	0.95	nM	IC50	J Med Chem (2012) 55: 871-882 [PMID:22185640]
ChEMBL	Inhibition of fibrinogen binding to Integrin alpha2bbeta3 receptor (unknown origin) by competitive ELISA	B	9.02	pIC50	0.95	nM	IC50	J Med Chem (2013) 56: 1509-1519 [PMID:23362923]
ChEMBL	Displacement of biotinylated fibrinogen from human alpha2b-beta3 receptor after 2 hrs by chemiluminescence assay	B	9.43	pIC50	0.37	nM	IC50	Eur J Med Chem (2012) 50: 255-263 [PMID:22365562]
ChEMBL	Displacement of biotinylated fibrinogen from human glycoprotein 2b/3a receptor after 2 hrs by chemiluminescence assay	B	9.43	pIC50	0.37	nM	IC50	Eur J Med Chem (2013) 64: 302-313 [PMID:23644213]
ChEMBL	Inhibition of integrin alpha2bbeta3-mediated platelet aggregation in human TRAP-6-activated whole blood for 6 mins by impedence-based aggregometry	B	7.87	pEC50	13.6	nM	EC50	J Med Chem (2012) 55: 871-882 [PMID:22185640]
integrin, beta 3 subunit (platelet glycoprotein IIIa, antigen CD61)/integrin, alpha V subunit/Integrin alpha-V/beta-3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907598] [GtoPdb: 2457, 2453] [UniProtKB: P05106, P06756]
ChEMBL	Inhibition of HUVEC attachment to human vitronectin	F	4	pIC50	100000	nM	IC50	J Med Chem (1992) 35: 4640-4642 [PMID:1469694]
ChEMBL	Inhibition of human umbilical vein endothelial cell adhesion to vitronectin	F	4.21	pIC50	62000	nM	IC50	J Med Chem (1994) 37: 2537-2551 [PMID:8057299]
ChEMBL	Inhibition of binding to human Vitronectin receptor (integrin alphaV-beta3)	B	6	pIC50	>1000	nM	IC50	J Med Chem (2003) 46: 5316-5325 [PMID:14640540]
ChEMBL	Inhibition of human integrin alphavbeta3 (unknown origin)	B	7.96	pIC50	11	nM	IC50	J Med Chem (2020) 63: 5675-5696 [PMID:31999923]
Integrin subunit alpha 2b/beta-3 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296069] [UniProtKB: D3ZAC0, Q8R2H2]
ChEMBL	Inhibition of fibrinogen binding to rat platelet integrin alpha2b beta3 by ELISA based solid phase binding assay	B	6.89	pIC50	130	nM	IC50	J Nat Prod (2021) 84: 466-473 [PMID:33491454]
integrin αIIbβ3 in Human [GtoPdb: 2579]
GtoPdb	Displacement of biotinylated fibrinogen from human integrin αIIbβ3.	-	9.43	pIC50	0.37	nM	IC50	Eur J Med Chem (2013) 64: 302-13 [PMID:23644213]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]