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] |
| ChEMBL | Inhibition of human GAT1 expressed in COS cells assessed as decrease in [3H]GABA uptake after 10 mins by scintillation counting analysis | B | 4.85 | pIC50 | 14000 | nM | IC50 | Bioorg Med Chem (2019) 27: 1232-1245 [PMID:30777661] |
| 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 33:
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]
