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 2 subunit (complement component 3 receptor 3 and 4 subunit)/integrin, alpha 1 subunit/Integrin alpha1/beta2 complex in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL5465394] [GtoPdb: 2456, 2437] [UniProtKB: P05107, P56199] | ||||||||
| ChEMBL | Antagonist activity at alpha1beta2 integrin receptor in human Jurkat E6.1 cells assessed as inhibition of ICAM-1-induced cell adhesion pre-incubated for 30 mins followed by 30 mins incubation in ICAM-1 coated wells by fluorescence based assay | B | 8.08 | pIC50 | 8.4 | nM | IC50 | J Med Chem (2023) 66: 5021-5040 [PMID:36976921] |
| ChEMBL | Binding affinity to alpha1beta2 integrin receptor (unknown origin) preincubated for 30 mins followed by 30 mins incubation in ICAM-1 coated wells by fluorescence based assay | B | 8.28 | pIC50 | 5.2 | nM | IC50 | J Med Chem (2023) 66: 5021-5040 [PMID:36976921] |
| 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 | Binding affinity to alpha4beta1 integrin receptor (unknown origin) preincubated for 30 mins followed by 30 mins incubation in vascular cell adhesion molecule 1-induced cell adhesion coated wells by fluorescence based assay | B | 8.05 | pIC50 | 8.9 | nM | IC50 | J Med Chem (2023) 66: 5021-5040 [PMID:36976921] |
| ChEMBL | Binding affinity to alpha4beta1 integrin receptor (unknown origin) preincubated for 30 mins followed by 30 mins incubation in fibronectin coated wells by fluorescence based assay | B | 8.07 | pIC50 | 8.6 | nM | IC50 | J Med Chem (2023) 66: 5021-5040 [PMID:36976921] |
| 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 | Eur J Med Chem (2014) 73: 225-232 [PMID:24412498] |
| 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 | Antagonist activity at alpha4beta1 integrin receptor in human Jurkat E6.1 cells assessed as inhibition of fibronectin-induced cell adhesion | B | 8.26 | pIC50 | 5.5 | nM | IC50 | J Med Chem (2023) 66: 5021-5040 [PMID:36976921] |
| 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 | Antagonist activity at alpha4beta1 integrin receptor in human Jurkat E6.1 cells assessed as inhibition of vascular cell adhesion molecule 1-induced cell adhesion | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2023) 66: 5021-5040 [PMID:36976921] |
| 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 | 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] |
| 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] |
| 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 7 subunit/GABAA receptor α4 subunit/Integrin alpha4/beta7 complex in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL5465395] [GtoPdb: 2461, 407] [UniProtKB: P26010, P48169] | ||||||||
| ChEMBL | Binding affinity to alpha4beta7 integrin receptor (unknown origin) preincubated for 30 mins followed by 30 mins incubation in mucosal vascular add-ressin cell adhesion molecule 1 coated wells by fluorescence based assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2023) 66: 5021-5040 [PMID:36976921] |
| 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] |
| ChEMBL | Binding affinity to alpha5beta1 integrin receptor (unknown origin) preincubated for 30 mins followed by 30 mins incubation in fibronectin coated wells by fluorescence based assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2023) 66: 5021-5040 [PMID:36976921] |
| ChEMBL | Agonist activity at alpha5beta1 integrin receptor in human K562 cells assessed as inhibition of fibronectin-induced cell adhesion pre-incubated for 30 mins followed by 1 hr incubation in fibronectin coated wells by fluorescence plate reader assay | B | 5.3 | pEC50 | >5000 | nM | EC50 | J Med Chem (2023) 66: 5021-5040 [PMID:36976921] |
| 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 M subunit (complement component 3 receptor 3 subunit)/Integrin alpha-M/beta-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111362] [GtoPdb: 2456, 2452] [UniProtKB: P05107, P11215] | ||||||||
| ChEMBL | Binding affinity to alphaMbeta2 integrin receptor (unknown origin) preincubated for 30 mins followed by 30 mins incubation in fibrinogen coated wells by fluorescence based assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2023) 66: 5021-5040 [PMID:36976921] |
| 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 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]
