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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 |
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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]