tirofiban [Ligand Id: 6586] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL916 (L-700462, Aggrastat, Tirofiban, MK-383)
  • 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: 24572441] [UniProtKB: P05106P08514]
  • This target only has 0 pki data point
  • 0
1 CHEMBL916_lig_chart_1 Integrin alpha-IIb/beta-3 Human
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  • integrin, beta 3 subunit (platelet glycoprotein IIIa, antigen CD61)/integrin, alpha V subunit/Integrin alpha-V/beta-3 in Human [ChEMBL: CHEMBL1907598] [GtoPdb: 24572453] [UniProtKB: P05106P06756]
  • This target only has 0 pki data point
  • 0
2 CHEMBL916_lig_chart_2 Integrin alpha-V/beta-3 Human
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  • integrin αIIbβ3 in Human [GtoPdb: 2579]
  • This target only has 0 pki data point
  • 0
3 CHEMBL916_lig_chart_3 integrin αIIbβ3 Human
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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: 24572441] [UniProtKB: P05106P08514]
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 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 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 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 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 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 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 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 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 [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 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-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-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 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 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 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 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: 24572453] [UniProtKB: P05106P06756]
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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]