nipecotic acid [Ligand Id: 4564] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL277498
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14]
ChEMBL Displacement of [3H]GABA from Gamma-aminobutyric acid A (GABA-A) receptor in rat brain membranes B 4 pIC50 >100000 nM IC50 J Med Chem (1985) 28: 1440-1446 [PMID:2995665]
ChEMBL Inhibition of [3H]GABA binding to Gamma-aminobutyric acid receptor of rat brain synaptosomal membranes B 4 pIC50 >100000 nM IC50 J Med Chem (1982) 25: 1157-1162 [PMID:6292417]
GABAB2/GABAB1/GABA B receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111474] [GtoPdb: 241, 240] [UniProtKB: O88871, Q9Z0U4]
ChEMBL Displacement of [3H]baclofen from Gamma-aminobutyric acid type B receptor in rat brain membranes B 4 pIC50 >100000 nM IC50 J Med Chem (1985) 28: 1440-1446 [PMID:2995665]
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 5.1 pIC50 8000 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 5.1 pIC50 8000 nM IC50 Bioorg Med Chem (2019) 27: 1232-1245 [PMID:30777661]
ChEMBL Percent inhibition against GABA transporter at a compound concentration of 1 uM B 8 pIC50 10.1 nM IC50 J Med Chem (2005) 48: 6887-6896 [PMID:16250647]
GAT1/GABA transporter 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5445] [GtoPdb: 929] [UniProtKB: P31648]
ChEMBL Displacement of NO 711 from mouse GAT1 expressed in HEK293 cell membranes after 40 mins by LC-ESI-MS-MS-based MS binding assay B 4.24 pKi 58210.32 nM Ki Bioorg Med Chem (2016) 24: 2072-2096 [PMID:27039250]
ChEMBL Inhibition of mouse GAT1 expressed in HEK293 cells assessed as [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA/unlabeled GABA addition measured after 4 mins by liquid scintillation counting analysis B 4.88 pIC50 13304.54 nM IC50 Bioorg Med Chem (2016) 24: 2072-2096 [PMID:27039250]
ChEMBL Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK cells B 4.88 pIC50 13182.57 nM IC50 Eur J Med Chem (2008) 43: 2404-2411 [PMID:18395300]
ChEMBL Inhibition of GABA uptake at murine GAT-1 expressed in HEK293 cells B 4.88 pIC50 13182.57 nM IC50 Eur J Med Chem (2013) 65: 487-499 [PMID:23770450]
ChEMBL Inhibition of mouse GAT1 expressed in HEK cells assessed as inhibition of [3H]-GABA uptake after 25 mins by liquid scintillation counting analysis B 5.07 pIC50 8511.38 nM IC50 Bioorg Med Chem (2013) 21: 3363-3378 [PMID:23598250]
ChEMBL Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis B 5.1 pIC50 8000 nM IC50 J Med Chem (2013) 56: 1323-1340 [PMID:23336362]
ChEMBL Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis B 5.1 pIC50 7943.28 nM IC50 J Med Chem (2013) 56: 1323-1340 [PMID:23336362]
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 4.41 pIC50 39000 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 [3H]GABA uptake at mouse GAT3 expressed in HEK cells B 4.64 pIC50 22908.68 nM IC50 Eur J Med Chem (2008) 43: 2404-2411 [PMID:18395300]
ChEMBL Inhibition of GABA uptake at murine GAT-2 expressed in HEK293 cells B 4.64 pIC50 22908.68 nM IC50 Eur J Med Chem (2013) 65: 487-499 [PMID:23770450]
GAT3/GABA transporter 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3699] [GtoPdb: 931] [UniProtKB: P31650]
ChEMBL Inhibition of mouse GAT3 expressed in HEK293 cells assessed as [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA/unlabeled GABA addition measured after 4 mins by liquid scintillation counting analysis B 4.64 pIC50 23014.42 nM IC50 Bioorg Med Chem (2016) 24: 2072-2096 [PMID:27039250]
ChEMBL Inhibition of [3H]GABA uptake at mouse GAT4 expressed in HEK cells B 4.7 pIC50 19952.62 nM IC50 Eur J Med Chem (2008) 43: 2404-2411 [PMID:18395300]
ChEMBL Inhibition of GABA uptake at murine GAT-3 expressed in HEK293 cells B 4.7 pIC50 19952.62 nM IC50 Eur J Med Chem (2013) 65: 487-499 [PMID:23770450]
ChEMBL Inhibition of mouse GAT4 expressed in HEK293 cells assessed as [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA/unlabeled GABA addition measured after 4 mins by liquid scintillation counting analysis B 4.7 pIC50 19769.7 nM IC50 Bioorg Med Chem (2016) 24: 2072-2096 [PMID:27039250]
ChEMBL Inhibition of mouse GAT3 expressed in HEK cells assessed as inhibition of [3H]-GABA uptake after 25 mins by liquid scintillation counting analysis B 4.71 pIC50 19498.45 nM IC50 Bioorg Med Chem (2013) 21: 3363-3378 [PMID:23598250]

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]