traxoprodil [Ligand Id: 4163] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL17350 (Cp-101,606, CP-101,606, CP-101606, Traxoprodil)
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Human [ChEMBL: CHEMBL1904] [GtoPdb: 457] [UniProtKB: Q13224]
  • GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Rat [ChEMBL: CHEMBL311] [GtoPdb: 457] [UniProtKB: Q00960]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: O15399, O60391, Q05586, Q12879, Q13224, Q14957, Q8TCU5]
ChEMBL Binding affinity against NMDA receptor by displacement of [3H]Ro-256981 B 7.96 pKi 11 nM Ki Bioorg Med Chem Lett (2003) 13: 829-832 [PMID:12617901]
ChEMBL Inhibition of [3H]-Ro-25-6981 binding to NMDA receptor B 8.15 pIC50 7 nM IC50 Bioorg Med Chem Lett (2004) 14: 3953-3956 [PMID:15225705]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7]
ChEMBL In vitro inhibition of glutamate induced neuronal death in primary cultures of rat hippocampal neurons. F 7.96 pIC50 11 nM IC50 J Med Chem (1995) 38: 3138-3145 [PMID:7636876]
ChEMBL In vitro inhibition of glutamate induced neuronal death in primary cultures of rat hippocampal neurons. F 7.99 pIC50 10.2 nM IC50 J Med Chem (1995) 38: 3138-3145 [PMID:7636876]
GluN1/GluN2A/Glutamate NMDA receptor; Grin1/Grin2a in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096680] [GtoPdb: 455, 456] [UniProtKB: P35439, Q00959]
ChEMBL Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2A. F 4 pIC50 >100000 nM IC50 J Med Chem (1999) 42: 3412-3420 [PMID:10464027]
GluN1/GluN2B/Glutamate NMDA receptor; GRIN1/GRIN2B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907603] [GtoPdb: 455, 457] [UniProtKB: Q05586, Q13224]
ChEMBL Displacement of [3H]ifenprodil binding to recombinant human NR1a/NR2B receptors expressed in L(tk-) cells B 7.96 pKi 11 nM Ki Bioorg Med Chem Lett (2003) 13: 693-696 [PMID:12639560]
ChEMBL Inhibition of NMDA-evoked increased intracellular [Ca2+] in cells expressing NR1/NR2B receptor B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (2004) 14: 3953-3956 [PMID:15225705]
GluN1/GluN2B/Glutamate NMDA receptor; Grin1/Grin2b in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096666] [GtoPdb: 455, 457] [UniProtKB: P35439, Q00960]
ChEMBL Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2B. F 7.14 pIC50 73 nM IC50 J Med Chem (1999) 42: 3412-3420 [PMID:10464027]
GluN1/GluN2C/Glutamate NMDA receptor; Grin1/Grin2c in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096911] [GtoPdb: 455, 458] [UniProtKB: P35439, Q00961]
ChEMBL Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2C. F 4 pIC50 >100000 nM IC50 J Med Chem (1999) 42: 3412-3420 [PMID:10464027]
GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1904] [GtoPdb: 457] [UniProtKB: Q13224]
ChEMBL Antagonist activity at human NR2B expressed in HEK293 cells assessed as glutamate-induced changes in intracellular calcium concentration F 7.13 pIC50 74 nM IC50 Bioorg Med Chem Lett (2011) 21: 3399-3403 [PMID:21524576]
GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL311] [GtoPdb: 457] [UniProtKB: Q00960]
ChEMBL Displacement of [3H]CP101606 from NR2B in rat brain minus cerebellum membrane B 8.34 pKi 4.6 nM Ki Bioorg Med Chem Lett (2011) 21: 3399-3403 [PMID:21524576]
ChEMBL Antagonist activity at NR2B NMDA receptor in Wistar rat neocortical cells assessed as inhibition of NMDA-evoked elevation of intracellular calcium concentration F 7.39 pIC50 41 nM IC50 J Med Chem (2007) 50: 901-914 [PMID:17290978]
ChEMBL Displacement of [3H]racemic CP-101606 from rat NR2B receptor in P2 membrane B 7.85 pIC50 14 nM IC50 Bioorg Med Chem Lett (2007) 17: 5558-5562 [PMID:17766106]
ChEMBL Displacement of [3H]Ro 25,6981 from NR2B NMDA receptor in rat forebrain B 8.15 pIC50 7 nM IC50 J Med Chem (2007) 50: 901-914 [PMID:17290978]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Displacement of [3H]bufuralol from hERG channel expressed in HEK293 cells B 5 pIC50 10000 nM IC50 Bioorg Med Chem Lett (2007) 17: 5558-5562 [PMID:17766106]

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]