MK-0429 [Ligand Id: 9689] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL145085 (Alpha-V Beta-3 Antagonist) |
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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, beta 1 subunit (fibronectin receptor, beta polypeptide, antigen CD29 includes MDF2, MSK12)/integrin, alpha V subunit/integrin, alpha 5 subunit (fibronectin receptor, alpha polypeptide)/Fibronectin receptor (Integrin alpha-5/beta-1 and alpha-V/beta-3) in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2111425] [GtoPdb: 2457, 2455, 2453, 2444] [UniProtKB: P05106, P05556, P06756, P08648] | ||||||||
| ChEMBL | Antagonist activity at integrin alphavbeta3alpha5beta1 in human A375M cells assessed as inhibition of cell adhesion to fibronectin in presence of Mg2+ | F | 6.09 | pIC50 | 810 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4117-4121 [PMID:22572578] |
| GtoPdb | Binding to the αvβ3 integrin using a scintillation-proximity assay (SPAV3). | - | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (2003) 46: 4790-8 [PMID:14561098] |
| integrin, beta 1 subunit (fibronectin receptor, beta polypeptide, antigen CD29 includes MDF2, MSK12)/integrin, alpha 5 subunit (fibronectin receptor, alpha polypeptide)/Integrin alpha-5/beta-1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095226] [GtoPdb: 2455, 2444] [UniProtKB: P05556, P08648] | ||||||||
| ChEMBL | Antagonist activity at integrin alpha5beta1 in human K562 cells assessed as inhibition of cell adhesion | F | 5.34 | pIC50 | 4600 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4117-4121 [PMID:22572578] |
| ChEMBL | Antagonist activity at integrin alpha5beta1 in human A375M cells assessed as inhibition of cell adhesion in presence of Mg2+ and MK-0429 | F | 5.66 | pIC50 | 2200 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4117-4121 [PMID:22572578] |
| 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 | Inhibition of alphaIIb-beta3 integrin mediated platelet aggregation | B | 4.46 | pIC50 | 34700 | nM | IC50 | J Med Chem (2003) 46: 4790-4798 [PMID:14561098] |
| 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] | ||||||||
| GtoPdb | Binding to the αvβ3 integrin using a scintillation-proximity assay (SPAV3). | - | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (2003) 46: 4790-8 [PMID:14561098] |
| ChEMBL | Inhibition of human integrin alphavbeta3 expressed in HEK293 cells assessed as reduction in cell adhesion to fibrinogen preincubated for 20 mins followed by phosphatase substrate addition and measured after 1 hr by spectrophotometry | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2020) 63: 5675-5696 [PMID:31999923] |
| ChEMBL | Antagonist activity at integrin alphaVbeta3 in human A375M cells assessed as cell adhesion to fibrinogen in presence of Mg2+ | F | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4117-4121 [PMID:22572578] |
| ChEMBL | Inhibition of alphaV-beta3 integrin binding | B | 10.1 | pIC50 | 0.08 | nM | IC50 | J Med Chem (2003) 46: 4790-4798 [PMID:14561098] |
| ChEMBL | Inhibition of integrin alphaVbeta3 | B | 10.1 | pIC50 | 0.08 | nM | IC50 | J Med Chem (2010) 53: 4332-4353 [PMID:20218623] |
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]
