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 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]
