traxoprodil [Ligand Id: 4163] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL17350 (Cp-101,606, CP-101,606, CP-101606, Traxoprodil) |
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| 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] |
| ChEMBL | Antagonist activity at NMDA receptor NR2B subunit (unknown origin) | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2023) 85: 129213-129213 [PMID:36870623] |
| 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 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]
