BIO1211 [Ligand Id: 6589] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL88478 (BIO-1211) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| integrin, beta 1 subunit (fibronectin receptor, beta polypeptide, antigen CD29 includes MDF2, MSK12)/integrin, alpha 4 subunit (antigen CD49D, alpha 4 subunit of VLA-4 receptor)/Integrin alpha-4/beta-1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907599] [GtoPdb: 2455, 2443] [UniProtKB: P05556, P13612] | ||||||||
| ChEMBL | Displacement of [125I]-FN from human alpha4beta1 integrin expressed in human Jurkat cells by scintillation proximity assay | B | 8.82 | pKi | 1.5 | nM | Ki | Eur J Med Chem (2014) 73: 225-232 [PMID:24412498] |
| ChEMBL | Antagonist activity at alpha4beta1 in human Jurkat E6.1 cells assessed as reduction in cell adhesion to VCAM1 pre-incubated for 30 mins before VCAM1 and further incubated for 30 mins by nitrophenyl-N-acetyl-beta-D-glucosaminide substrate based chromogenic assay | B | 8.07 | pIC50 | 8.6 | nM | IC50 | J Med Chem (2016) 59: 9721-9742 [PMID:27726366] |
| ChEMBL | Inhibition of human alpha4beta1 integrin expressed in human Jurkat cells assessed as inhibition of cell adhesion to VCAM-1 | B | 8.12 | pIC50 | 7.6 | nM | IC50 | ACS Med Chem Lett (2015) 6: 701-706 [PMID:26101577] |
| ChEMBL | Inhibition of human alpha4beta1 integrin expressed in human Jurkat cells assessed as inhibition of cell adhesion to VCAM-1 | B | 8.12 | pIC50 | 7.6 | nM | IC50 | Eur J Med Chem (2014) 73: 225-232 [PMID:24412498] |
| ChEMBL | Displacement of [125I]-FN from human alpha4beta1 integrin expressed in human Jurkat cells by scintillation proximity assay | B | 8.32 | pIC50 | 4.8 | nM | IC50 | Eur J Med Chem (2014) 73: 225-232 [PMID:24412498] |
| ChEMBL | Inhibition of integrin alpha4-beta1 adhesion to Jurkat cells | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (1999) 42: 920-934 [PMID:10072689] |
| ChEMBL | Inhibition of integrin alpha4-beta1 binding to VCAM-Ig | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (1999) 42: 920-934 [PMID:10072689] |
| ChEMBL | Inhibition of VLA-4 receptor expressed in CHO cells | B | 9.3 | pIC50 | <0.5 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 41-45 [PMID:15582407] |
| ChEMBL | Inhibition of Integrin alpha-4-beta-1-mediated adhesion in human jurkat cells | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Nat Chem Biol (2006) 2: 381-389 [PMID:16767086] |
| ChEMBL | Inhibition of [125I]VCAM-Ig binding to Alpha-4 beta-1 (VLA-4) of Jurkat cells | B | 9.89 | pIC50 | 0.13 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 685-688 [PMID:11844701] |
| ChEMBL | Antagonistic activity against VLA-4 integrin of human jurkat cells using [125I]VCAM-Ig as radioligand | F | 9.89 | pIC50 | 0.13 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2709-2713 [PMID:11591507] |
| integrin, alpha 4 subunit (antigen CD49D, alpha 4 subunit of VLA-4 receptor)/integrin, beta 7 subunit/Integrin alpha-4/beta-7 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095184] [GtoPdb: 2443, 2461] [UniProtKB: P13612, P26010] | ||||||||
| ChEMBL | Inhibition of integrin alpha4-beta7 adhesion to JY cells | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (1999) 42: 920-934 [PMID:10072689] |
| ChEMBL | Inhibition of [125I]MAdCAM-Ig binding to alpha4-beta7 integrin of human RPMI-8866 cells | B | 6.06 | pIC50 | 862 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2709-2713 [PMID:11591507] |
| ChEMBL | Inhibition of [125I]VCAM-Ig binding to alpha4-beta7 integrin of human RPMI-8866 cells | B | 6.36 | pIC50 | 433 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2709-2713 [PMID:11591507] |
| 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 | Inhibition of integrin alpha5-beta1 adhesion to K562 cells | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 920-934 [PMID:10072689] |
| 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 integrin alphaIIb-beta3 adhesion to human citreated platelets | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 920-934 [PMID:10072689] |
| integrin, beta 2 subunit (complement component 3 receptor 3 and 4 subunit)/integrin, alpha L subunit (antigen CD11A (p180), lymphocyte function-associated antigen 1; alpha polypeptide)/Integrin alpha-L/beta-2 (LFA-1) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2364172] [GtoPdb: 2456, 2451] [UniProtKB: P05107, P20701] | ||||||||
| ChEMBL | Antagonist activity at alphaLbeta2 in human Jurkat E6.1 cells assessed as reduction in cell adhesion to ICAM1 pre-incubated for 30 mins before ICAM1 and further incubated for 30 mins by nitrophenyl-N-acetyl-beta-D-glucosaminide substrate based chromogenic assay | B | 9.08 | pIC50 | 0.84 | nM | IC50 | J Med Chem (2016) 59: 9721-9742 [PMID:27726366] |
| integrin, beta 2 subunit (complement component 3 receptor 3 and 4 subunit)/integrin, alpha L subunit (antigen CD11A (p180), lymphocyte function-associated antigen 1; alpha polypeptide)/Intercellular adhesion molecule (ICAM-1), Integrin alpha-L/beta-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096661] [GtoPdb: 2456, 2451] [UniProtKB: P05107, P05362, P20701] | ||||||||
| ChEMBL | Inhibition of ICAM-1 transfected CHO cell adhesion to integrin alphaL-beta2 of human JY cells | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 920-934 [PMID:10072689] |
| integrin α4β1 in Human [GtoPdb: 2580] | ||||||||
| GtoPdb | - | - | 9 | pIC50 | - | - | - | J Med Chem (1999) 42: 920-34 [PMID:10072689] |
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]
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