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ChEMBL ligand: CHEMBL916 (Aggrastat, Agrastat, L-700462, MK-383, Tirofiban) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 32:
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]