lifitegrast [Ligand Id: 7533] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2048028 (Lifitegrast, SAR 1118, SAR-1118, SHP-606, SHP606, Xiidra)
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  • Intercellular adhesion molecule-1 in Human [ChEMBL: CHEMBL3070] [UniProtKB: P05362]
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  • 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 [ChEMBL: CHEMBL2096661] [GtoPdb: 2456, 2451] [UniProtKB: P05107, P05362, P20701]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 4.7 pIC50 >20000 nM IC50 ACS Med Chem Lett (2012) 3: 203-206 [PMID:24900456]
Intercellular adhesion molecule-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3070] [UniProtKB: P05362]
ChEMBL Inhibition of human recombinant ICAM-1 adhesion into human Jurkat cells after 1 hr B 8.53 pIC50 2.98 nM IC50 ACS Med Chem Lett (2012) 3: 203-206 [PMID:24900456]
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 Antagonist activity at LFA-1/ICAM-1 in human HuT-78 T-cells assessed as inhibition of cell adhesion after 1 hr by p-nitrophenyl n-acetyl-beta-D-glucosaminide method in presence of 10% human serum F 7.13 pIC50 74 nM IC50 ACS Med Chem Lett (2012) 3: 203-206 [PMID:24900456]
ChEMBL Antagonist activity at LFA-1/ICAM-1 in human HuT-78 T-cells assessed as inhibition of cell adhesion after 1 hr by p-nitrophenyl n-acetyl-beta-D-glucosaminide method F 8.05 pIC50 9 nM IC50 ACS Med Chem Lett (2012) 3: 203-206 [PMID:24900456]

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]