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 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]
