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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]