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 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]