selfotel [Ligand Id: 4155] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL39664 (CGS 19755, CGS-19755, CPDD-0027, GNF-PF-157, Selfotel) |
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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 | Tested in vitro for the affinity against NMDA receptor in a cortical wedge assay | B | 5.8 | pIC50 | 1600 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 43-48 |
| ChEMBL | Tested in vitro for the affinity against NMDA receptor by examining its ability to inhibit [3H]-CGS-19,755 binding | B | 7.27 | pIC50 | 54 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 43-48 |
| 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 | Compound was evaluated for its ability to displace [3H]CPP or [3H]-CGS- 19755 ligand from N-methyl-D-aspartate (NMDA) receptor | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1992) 35: 1509-1514 [PMID:1533680] |
| ChEMBL | Compound was tested in vitro for N-methyl-D-aspartate glutamate receptor binding using [3H]L-glutamate | B | 6.8 | pKi | 160 | nM | Ki | J Med Chem (1991) 34: 161-168 [PMID:1671413] |
| ChEMBL | Compound was evaluated for its ability to displace [3H]CPP or [3H]-CGS- 19755 ligand from N-methyl-D-aspartate (NMDA) receptor | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (1992) 35: 1509-1514 [PMID:1533680] |
| ChEMBL | The compound was tested for NMDA antagonist activity against [3H]-CGS- 19755 binding in rat cortex preparation | B | 7.4 | pKi | 40 | nM | Ki | Bioorg Med Chem Lett (1992) 2: 1247-1250 |
| ChEMBL | Binding affinity to the glutamate site of the NMDA receptor was measured by competitive inhibition of binding of [3H]-CGP- 39653 to rat or porcine cerebral cortex membranes | B | 7.54 | pKi | 29 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 1635-1640 |
| ChEMBL | Tested for binding affinity against NMDA receptor, from rat synaptic membrane, using [3H]glycine as the radioligand. | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1993) 36: 331-342 [PMID:8093907] |
| ChEMBL | Tested for binding affinity against NMDA receptor, from rat synaptic membrane, using [3H]TCP as the radioligand. | B | 4.65 | pIC50 | 22400 | nM | IC50 | J Med Chem (1993) 36: 331-342 [PMID:8093907] |
| ChEMBL | Affinity for the NMDA receptor site was assessed by its ability to displace [3H]TCP from its binding site in rat brain | B | 4.65 | pIC50 | 22400 | nM | IC50 | J Med Chem (2001) 44: 1516-1529 [PMID:11334562] |
| ChEMBL | Compound was evaluated in vitro in a cortical-wedge preparation for the antagonism of N-methyl-D-aspartate-induced responses | F | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (1991) 34: 90-97 [PMID:1825117] |
| ChEMBL | Inhibition of rat NMDA receptor | B | 5.79 | pIC50 | 1620 | nM | IC50 | Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743] |
| ChEMBL | Compound was tested in vitro for its inhibitory activity against N-methyl-D-aspartate glutamate receptor using [3H]MK-801 | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (1991) 34: 161-168 [PMID:1671413] |
| ChEMBL | Tested for the ability to inhibit the specific binding of [3H]-CGS- 19755 to NMDA recognition sites on rat brain membranes | B | 7.06 | pIC50 | 87 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 33-38 |
| ChEMBL | Inhibition of N-methyl-D-aspartate glutamate receptor by using [3H]CPP as a radioligand from the rat cortical membranes. | B | 7.19 | pIC50 | 65 | nM | IC50 | J Med Chem (1990) 33: 2916-2924 [PMID:2145436] |
| ChEMBL | In vitro binding affinity against N-methyl-D-aspartate glutamate receptor using [3H]CGS-19,755 ligand | B | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (1991) 34: 90-97 [PMID:1825117] |
| ChEMBL | In vitro compound's ability to displace [3H]-CGS-19,755 binding as a measure of its affinity for the glutamate recognition site on the NMDA receptor complex. | B | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (1992) 35: 3547-3560 [PMID:1404235] |
| ChEMBL | Ability to displace [3H]CPP from NMDA receptor in rat brain membrane | B | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (1992) 35: 1345-1370 [PMID:1533422] |
| ChEMBL | Inhibition of [3H]-CGS- 19755 binding to N-methyl-D-aspartic acid receptors in rat crude synaptic membranes | B | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (1989) 32: 2171-2178 [PMID:2549246] |
| ChEMBL | Tested for binding affinity against NMDA receptor, from rat synaptic membrane, using [3H]-CPP as the radioligand. | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (1993) 36: 331-342 [PMID:8093907] |
| ChEMBL | Displacement of [3H]CPP from rat synaptic membrane glutamate NMDA receptor | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2001) 44: 1516-1529 [PMID:11334562] |
| ChEMBL | Displacement of [3H]CPP from rat brain synaptic membrane N-methyl-D-aspartate glutamate receptor | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (1998) 41: 236-246 [PMID:9457246] |
| ChEMBL | Compound was evaluated for its ability to displace [3H]CCP binding for NMDA receptor | B | 7.62 | pIC50 | 24 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 207-212 |
| ChEMBL | Tested in vitro for antagonistic activity at N-methyl-D-aspartate glutamate receptor by measuring displacement of [3H]TCP from crude synaptic membrane preparations obtained from rat brain | F | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (1998) 41: 236-246 [PMID:9457246] |
| GluN2A/Glutamate [NMDA] receptor subunit epsilon 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL310] [GtoPdb: 456] [UniProtKB: Q00959] | ||||||||
| ChEMBL | Inhibition of [3H]Glu binding to rat N-methyl-D-aspartic acid receptor 2A | B | 6.08 | pIC50 | 840 | nM | IC50 | J Med Chem (2005) 48: 5489-5494 [PMID:16107147] |
| ChEMBL | Inhibition of [3H]CPP binding to rat N-methyl-D-aspartic acid receptor 2A | B | 7.02 | pIC50 | 95 | nM | IC50 | J Med Chem (2005) 48: 5489-5494 [PMID:16107147] |
| GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic AMPA in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2096670] [GtoPdb: 444, 445, 446, 447] [UniProtKB: P42261, P42262, P42263, P48058] | ||||||||
| ChEMBL | Percent inhibition against AMPA receptor at 1 uM | B | 6.01 | pIC50 | 967 | nM | IC50 | J Med Chem (2005) 48: 6887-6896 [PMID:16250647] |
| GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490] | ||||||||
| ChEMBL | Binding affinity towards AMPA receptor using [3H]AMPA as radioligand; Inactive | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (1990) 33: 2961-2963 [PMID:1977908] |
| GluK3/Glutamate receptor ionotropic kainate 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3744] [GtoPdb: 452] [UniProtKB: P42264] | ||||||||
| ChEMBL | Binding affinity towards Ionotropic glutamate receptor kainate using [3H]-kainic acid as radioligand; Inactive | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (1990) 33: 2961-2963 [PMID:1977908] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay | F | 5.88 | pEC50 | 1317 | nM | EC50 | Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783] |
| ChEMBL | NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay | F | 5.92 | pEC50 | >1208 | nM | EC50 | Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783] |
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]
