TCN-201 [Ligand Id: 7846] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2333945 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GluN1/GluN2A in Human [GtoPdb: 455, 456] [UniProtKB: Q05586, Q12879] | ||||||||
| GtoPdb | Inhibition of glycine-induced (1µM) NMDA receptor responses measured in Xenopus oocytes co-expressing hGluN1 and hGluN2A NMDA receptor subunits | - | 7 | pIC50 | 100 | nM | IC50 | J Neurosci (2012) 32: 6197-208 [PMID:22553026] |
| GluN1/GluN2A/Glutamate NMDA receptor; Grin1/Grin2a in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096680] [GtoPdb: 455, 456] [UniProtKB: P35439, Q00959] | ||||||||
| ChEMBL | Antagonist activity at rat GluN1A/GluN2A receptor expressed in Xenopus laevis oocytes assessed as inhibition of glutamate/glycine-induced channel current at -70 mV holding potential by two electrode voltage clamp method | B | 6.29 | pIC50 | 512 | nM | IC50 | Eur J Med Chem (2017) 129: 124-134 [PMID:28222314] |
| ChEMBL | Negative allosteric modulation of recombinant rat GluN1/GluN2A expressed in Xenopus laevis oocytes assessed as inhibition of glutamate/glycine-induced current response at -40 mV holding potential by two-electrode voltage clamp method | B | 6.77 | pIC50 | 170 | nM | IC50 | ACS Med Chem Lett (2019) 10: 248-254 [PMID:30891121] |
| GluN1/GluN2B/Glutamate NMDA receptor; GRIN1/GRIN2B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907603] [GtoPdb: 455, 457] [UniProtKB: Q05586, Q13224] | ||||||||
| ChEMBL | Negative allosteric modulation of human GluN1/GluN2A receptor expressed in xenopus laevis oocytes assessed as reduction in 3 uM glycine-induced channel current by two electrode voltage clamp method | B | 6.35 | pIC50 | 446 | nM | IC50 | J Med Chem (2018) 62: 3-23 [PMID:29446949] |
| ChEMBL | Inhibition of human recombinant GluN1/GluN2B receptor expressed in human osteosarcoma cells after 5 mins by FLIPR/Ca2+ assay | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2013) 56: 3121-3147 [PMID:23458846] |
| GluN2A/Glutamate [NMDA] receptor subunit epsilon 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1972] [GtoPdb: 456] [UniProtKB: Q12879] | ||||||||
| ChEMBL | Negative allosteric modulation of human GluN2A receptor expressed in HEK cells assessed as reduction in 3 uM glycine/glutamate-induced intracellular calcium flux preincubated for 10 mins followed by glycine/glutamate addition and measured for 3 mins by Fluo-8-AM dye based fluorescence assay | B | 6.47 | pIC50 | 340 | nM | IC50 | J Med Chem (2018) 62: 3-23 [PMID:29446949] |
| ChEMBL | Negative allosteric modulation of human GluN2A receptor expressed in xenopus laevis oocytes assessed as reduction in 3 uM glycine-induced channel current at -40 mV holding potential by two electrode voltage clamp method | B | 6.49 | pIC50 | 320 | nM | IC50 | J Med Chem (2018) 62: 3-23 [PMID:29446949] |
| ChEMBL | Negative allosteric modulation of human GluN2A receptor expressed in HEK cells assessed as reduction in glycine/glutamate-induced intracellular calcium flux preincubated for 5 mins followed by glycine/glutamate addition by Fluo-4-AM dye based FLIPR assay | B | 6.96 | pIC50 | 110 | nM | IC50 | J Med Chem (2018) 62: 3-23 [PMID:29446949] |
| ChEMBL | Negative allosteric modulation of eGFP-fused human GluN2A receptor expressed in HEK293T cells assessed as inhibition of NMDA-induced channel current at -60 mV holding potential measured for 5 secs every 60 secs in presence of glycine by whole cell patch clamp method | B | 6.96 | pIC50 | 109 | nM | IC50 | Eur J Med Chem (2017) 129: 124-134 [PMID:28222314] |
| GtoPdb | Inhibition of glycine-induced (1µM) NMDA receptor responses measured in Xenopus oocytes co-expressing hGluN1 and hGluN2A NMDA receptor subunits | - | 7 | pIC50 | 100 | nM | IC50 | J Neurosci (2012) 32: 6197-208 [PMID:22553026] |
| GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1904] [GtoPdb: 457] [UniProtKB: Q13224] | ||||||||
| ChEMBL | Negative allosteric modulation of human GluN2B receptor expressed in HEK cells assessed as reduction in glycine/glutamate-induced intracellular calcium flux preincubated for 5 mins followed by glycine/glutamate addition by Fluo-4-AM dye based FLIPR assay | B | 4.3 | pIC50 | 50000 | nM | IC50 | J Med Chem (2018) 62: 3-23 [PMID:29446949] |
| ChEMBL | Negative allosteric modulation of human GluN2B receptor expressed in xenopus laevis oocytes assessed as reduction in 3 uM glycine-induced channel current at -40 mV holding potential by two electrode voltage clamp method | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 62: 3-23 [PMID:29446949] |
| GluN2C/Glutamate [NMDA] receptor subunit epsilon 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4109] [GtoPdb: 458] [UniProtKB: Q14957] | ||||||||
| ChEMBL | Negative allosteric modulation of human GluN2C receptor expressed in xenopus laevis oocytes assessed as reduction in 3 uM glycine-induced channel current at -40 mV holding potential by two electrode voltage clamp method | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 62: 3-23 [PMID:29446949] |
| GluN2D/Glutamate [NMDA] receptor subunit epsilon 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2591] [GtoPdb: 459] [UniProtKB: O15399] | ||||||||
| ChEMBL | Negative allosteric modulation of human GluN2D receptor expressed in HEK cells assessed as reduction in glycine/glutamate-induced intracellular calcium flux preincubated for 5 mins followed by glycine/glutamate addition by Fluo-4-AM dye based FLIPR assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2018) 62: 3-23 [PMID:29446949] |
| ChEMBL | Negative allosteric modulation of human GluN2D receptor expressed in xenopus laevis oocytes assessed as reduction in 3 uM glycine-induced channel current at -40 mV holding potential by two electrode voltage clamp method | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 62: 3-23 [PMID:29446949] |
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]
