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 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]
