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 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]
