guvacine [Ligand Id: 4691] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL76768 (Guvacine)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GAT1/GABA transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1903] [GtoPdb: 929] [UniProtKB: P30531]
ChEMBL Inhibitory activity against human GABA transporter-1 (hGAT1) B 4.85 pIC50 14000 nM IC50 J. Med. Chem. (1994) 37: 2334-2342 [PMID:8057281]
GAT1/GABA transporter 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5445] [GtoPdb: 929] [UniProtKB: P31648]
ChEMBL Inhibition of mouse GAT1 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting B 4.68 pIC50 20900 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 417-423 [PMID:26706177]
ChEMBL Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis B 4.85 pIC50 14000 nM IC50 J. Med. Chem. (2013) 56: 1323-1340 [PMID:23336362]
ChEMBL Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK cells B 4.87 pIC50 13489.63 nM IC50 Eur. J. Med. Chem. (2008) 43: 2404-2411 [PMID:18395300]
ChEMBL Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis B 4.9 pIC50 12589.25 nM IC50 J. Med. Chem. (2013) 56: 1323-1340 [PMID:23336362]
GAT1/GABA transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4054] [GtoPdb: 929] [UniProtKB: P23978]
ChEMBL H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined B 5.54 pIC50 2900 nM IC50 J. Med. Chem. (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound B 5.55 pIC50 2790 nM IC50 J. Med. Chem. (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined B 5.56 pIC50 2770 nM IC50 J. Med. Chem. (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL H-bonding interaction between amino acid residue (Thr-89) of Sodium- and chloride-dependent GABA transporter 1TM2 and compound B 5.58 pIC50 2660 nM IC50 J. Med. Chem. (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined B 5.58 pIC50 2650 nM IC50 J. Med. Chem. (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined B 5.59 pIC50 2590 nM IC50 J. Med. Chem. (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound B 5.59 pIC50 2560 nM IC50 J. Med. Chem. (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined B 5.65 pIC50 2260 nM IC50 J. Med. Chem. (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound B 5.72 pIC50 1910 nM IC50 J. Med. Chem. (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined B 5.73 pIC50 1870 nM IC50 J. Med. Chem. (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined B 5.73 pIC50 1850 nM IC50 J. Med. Chem. (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL H-bonding interaction between amino acid residue (Thr-89) of Sodium- and chloride-dependent GABA transporter 1TM2 and compound B 5.75 pIC50 1760 nM IC50 J. Med. Chem. (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined B 5.77 pIC50 1680 nM IC50 J. Med. Chem. (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound B 5.77 pIC50 1680 nM IC50 J. Med. Chem. (2004) 47: 5620-5629 [PMID:15509161]
GAT2/GABA transporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4535] [GtoPdb: 930] [UniProtKB: Q9NSD5]
ChEMBL Binding affinity to GAT2 B 4.18 pIC50 66000 nM IC50 Eur. J. Med. Chem. (2010) 45: 2453-2466 [PMID:20219271]
GAT2/GABA transporter 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4889] [GtoPdb: 930] [UniProtKB: P31646]
ChEMBL Inhibitory activity against rat GABA transporter-2 (rGAT2) B 4.24 pIC50 58000 nM IC50 J. Med. Chem. (1994) 37: 2334-2342 [PMID:8057281]
GAT2/GABA transporter 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5205] [GtoPdb: 930] [UniProtKB: P31649]
ChEMBL Inhibition of mouse GAT2 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting B 4.14 pIC50 72400 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 417-423 [PMID:26706177]
ChEMBL Inhibition of [3H]GABA uptake at mouse GAT3 expressed in HEK cells B 4.59 pIC50 25703.96 nM IC50 Eur. J. Med. Chem. (2008) 43: 2404-2411 [PMID:18395300]
GAT3/GABA transporter 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3699] [GtoPdb: 931] [UniProtKB: P31650]
ChEMBL Inhibition of [3H]GABA uptake at mouse GAT4 expressed in HEK cells B 4.59 pIC50 25703.96 nM IC50 Eur. J. Med. Chem. (2008) 43: 2404-2411 [PMID:18395300]

ChEMBL data shown on this page come from version 25:

A.P. Bento, A. Gaulton, A. Hersey, et al. (2014). The ChEMBL bioactivity database: an update. Nucl. Acids Res. Database Issue. 42 D1083-D1090. [PMID:24214965]