rebamipide [Ligand Id: 871] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1697771 (Mucosta, NSC-758955, OPC-12759, Proamipide, Rebamipida, Rebamipide, Rebator)
  • Ubiquitin-associated and SH3 domain-containing protein B in Human [ChEMBL: CHEMBL5725045] [UniProtKB: Q8TF42]
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  • CCK1 receptor in Rat [GtoPdb: 76] [UniProtKB: P30551]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Ubiquitin-associated and SH3 domain-containing protein B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5725045] [UniProtKB: Q8TF42]
ChEMBL Competitive inhibition of human STS-1 HP domain (369 to 636 residues) phosphatase activity expressed in Escherichia coli BL21 (DE3) using pNPP as substrate assessed as inhibition constant preincubated for 20 mins followed by substrate addition by Lineweaver-Burk plot analysis B 5.7 pKi 2000 nM Ki J Med Chem (2024) 67: 1949-1960 [PMID:38252624]
ChEMBL Competitive inhibition of human STS-1 HP domain (369 to 636 residues) phosphatase activity expressed in Escherichia coli BL21 (DE3) using DiFMUP as substrate assessed as inhibition constant preincubated for 20 mins followed by substrate addition by Lineweaver-Burk plot analysis B 5.7 pKi 2000 nM Ki J Med Chem (2024) 67: 1949-1960 [PMID:38252624]
ChEMBL Inhibition of human STS-1 HP domain (369 to 636 residues) phosphatase activity expressed in Escherichia coli BL21 (DE3) using OMFP as substrate preincubated for 20 mins followed by substrate addition by fluorescence based spectrophotometric analysis B 5.43 pIC50 3700 nM IC50 J Med Chem (2024) 67: 1949-1960 [PMID:38252624]
ChEMBL Inhibition of human STS-1 HP domain (369 to 636 residues) phosphatase activity expressed in Escherichia coli BL21 (DE3) using DiFMUP as substrate preincubated for 20 mins followed by substrate addition by fluorescence based spectrophotometric analysis B 5.43 pIC50 3700 nM IC50 J Med Chem (2024) 67: 1949-1960 [PMID:38252624]
ChEMBL Inhibition of human STS-1 HP domain (369 to 636 residues) phosphatase activity expressed in Escherichia coli BL21 (DE3) using pNPP as substrate preincubated for 20 mins followed by substrate addition by absorbance based spectrophotometric analysis B 5.52 pIC50 3000 nM IC50 J Med Chem (2024) 67: 1949-1960 [PMID:38252624]
CCK1 receptor in Rat [GtoPdb: 76] [UniProtKB: P30551]
GtoPdb - - 4.4 pIC50 - - - Eur J Pharmacol (2004) 505: 61-6 [PMID:15556137]

ChEMBL data shown on this page come from version 36:

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]