NMDA [Ligand Id: 4268] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL291278 (2-Methylamino-Succinic Acid, Nmda, N-Methyl-Daspartate, N-methyl-d-aspartic acid (nmda), (R)-2-(Methylamino)Succinic Acid)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 Displacement of [3H]CGP39653 from NMDA receptor in Sprague-Dawley rat brain membranes B 5.21 pKi 6200 nM Ki J Med Chem (2010) 53: 4110-4118 [PMID:20408529]
ChEMBL Displacement of [3H]CGP39653 from NMDA receptor in rat brain synaptic cortical membranes after 60 mins by scintillation counting method B 5.21 pKi 6200 nM Ki J Med Chem (2019) 62: 4467-4482 [PMID:30943028]
ChEMBL Inhibitory activity against N-methyl-D-aspartate glutamate receptor using [3H]CPP as radioligand B 4.46 pIC50 35000 nM IC50 J Med Chem (1996) 39: 183-190 [PMID:8568805]
ChEMBL Inhibition of [3H]CPP binding to N-methyl-D-aspartate glutamate receptor of rat cortical or hippocampal membranes B 5.22 pIC50 6000 nM IC50 J Med Chem (1990) 33: 2772-2777 [PMID:2170646]
ChEMBL Compound was evaluated for the inhibition of [3H]CGS-19,755 binding to NMDA receptor from rat brain synaptic membrane. B 5.26 pIC50 5500 nM IC50 Bioorg Med Chem Lett (1996) 6: 2381-2386
ChEMBL Compound was tested for inhibition of [3H]CPP binding from N-methyl-D-aspartate glutamate receptor in the rat cortical membranes. B 5.34 pIC50 4550 nM IC50 J Med Chem (1990) 33: 2916-2924 [PMID:2145436]
ChEMBL Compound was evaluated for the inhibition of [3H]-CGS-19,755 binding at N-methyl-D-aspartate glutamate receptor B 5.38 pIC50 4150 nM IC50 J Med Chem (1992) 35: 4608-4612 [PMID:1361579]
ChEMBL Compound was evaluated for the inhibition of [3H]norepinephrine binding at N-methyl-D-aspartate glutamate receptor B 4.12 pEC50 75000 nM EC50 J Med Chem (1992) 35: 4608-4612 [PMID:1361579]
ChEMBL Compound was evaluated for the inhibition of [3H]MK-801 binding at N-methyl-D-aspartate glutamate receptor B 5.16 pEC50 6860 nM EC50 J Med Chem (1992) 35: 4608-4612 [PMID:1361579]
GluN1/GluN2A/Glutamate NMDA receptor; Grin1/Grin2a in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096680] [GtoPdb: 455, 456] [UniProtKB: P35439, Q00959]
ChEMBL Activity at rat recombinant NR1/NR2A receptor expressed in Xenopus oocytes assessed as effect on glutamate-induced current by two voltage clamp electrophysiology B 4.12 pEC50 75000 nM EC50 J Med Chem (2008) 51: 4179-4187 [PMID:18578474]
GluN1/GluN2B/Glutamate NMDA receptor; Grin1/Grin2b in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096666] [GtoPdb: 455, 457] [UniProtKB: P35439, Q00960]
ChEMBL Activity at rat recombinant NR1/NR2B receptor expressed in Xenopus oocytes assessed as effect on glutamate-induced current by two voltage clamp electrophysiology B 4.66 pEC50 22000 nM EC50 J Med Chem (2008) 51: 4179-4187 [PMID:18578474]
GluN1/GluN2C/Glutamate NMDA receptor; Grin1/Grin2c in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096911] [GtoPdb: 455, 458] [UniProtKB: P35439, Q00961]
ChEMBL Activity at rat recombinant NR1/NR2C receptor expressed in Xenopus oocytes assessed as effect on glutamate-induced current by two voltage clamp electrophysiology B 4.64 pEC50 23000 nM EC50 J Med Chem (2008) 51: 4179-4187 [PMID:18578474]
GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic, AMPA in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093871] [GtoPdb: 444, 445, 446, 447] [UniProtKB: P19490, P19491, P19492, P19493]
ChEMBL Inhibitory activity against Ionotropic glutamate receptor AMPA using [3H]AMPA as radioligand B 4 pIC50 >100000 nM IC50 J Med Chem (1996) 39: 183-190 [PMID:8568805]
ChEMBL Compound was evaluated for the inhibition of [3H]AMPA binding to Ionotropic glutamate receptor AMPA from rat brain synaptic membrane. B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (1996) 6: 2381-2386
ChEMBL Displacement of [3H]AMPA from AMPA receptor in rat brain synaptic cortical membranes after 30 mins by scintillation counting method B 4 pIC50 >100000 nM IC50 J Med Chem (2019) 62: 4467-4482 [PMID:30943028]
GluK1/GluK2/GluK3/GluK4/GluK5/Glutamate receptor ionotropic, kainate in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094119] [GtoPdb: 450, 451, 452, 453, 454] [UniProtKB: P22756, P42260, P42264, Q01812, Q63273]
ChEMBL Inhibitory activity against Ionotropic glutamate receptor kainate using [3H]-kainic acid as radioligand B 4 pIC50 >100000 nM IC50 J Med Chem (1996) 39: 183-190 [PMID:8568805]
ChEMBL Compound was evaluated for the inhibition of [3H]-KA binding to Ionotropic glutamate receptor kainate from rat brain synaptic membrane. B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (1996) 6: 2381-2386
GluN1/GluN2D/Ionotropic glutamate receptor NMDA 1/2D in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038506] [GtoPdb: 455, 459] [UniProtKB: P35439, Q62645]
ChEMBL Activity at rat NR1/NR2D receptor expressed in Xenopus oocytes assessed as effect on glutamate-induced current by two voltage clamp electrophysiology B 5.08 pEC50 8300 nM EC50 J Med Chem (2008) 51: 4179-4187 [PMID:18578474]
Serine protease hepsin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2079849] [UniProtKB: P05981]
ChEMBL High-Throughput Screening Assay: To identify novel inhibitors of hepsin, the Chembridge DIVERSet 10,000 compound high-diversity library was screened using an assay based on the cleavage of the chromogenic peptide. In addition, the NINDS II library of 1040 compounds (MicroSource Discovery) was screened to identify hepsin inhibitors among established drugs and known bioactive molecules. Screens were performed in a 96-well format at a final compound concentration of 2 uM. To minimize false positives, positions 1 and 12 of each row contained DMSO/buffer controls. As a measure of reproducibility, the Z' score for this assay was 0.78 (Zhang et al., 1999 J Biomol Screen 4:67). B 6.12 pIC50 750 nM IC50 US-9182402-B2. Hepsin inhibitors (2015)
Thrombin in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4471] [UniProtKB: P00735]
ChEMBL High-Throughput Screening Assay: To identify novel inhibitors of hepsin, the Chembridge DIVERSet 10,000 compound high-diversity library was screened using an assay based on the cleavage of the chromogenic peptide. In addition, the NINDS II library of 1040 compounds (MicroSource Discovery) was screened to identify hepsin inhibitors among established drugs and known bioactive molecules. Screens were performed in a 96-well format at a final compound concentration of 2 uM. To minimize false positives, positions 1 and 12 of each row contained DMSO/buffer controls. As a measure of reproducibility, the Z' score for this assay was 0.78 (Zhang et al., 1999 J Biomol Screen 4:67). B 4.7 pIC50 >20000 nM IC50 US-9182402-B2. Hepsin inhibitors (2015)
Trypsin in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366] [UniProtKB: P00761]
ChEMBL High-Throughput Screening Assay: To identify novel inhibitors of hepsin, the Chembridge DIVERSet 10,000 compound high-diversity library was screened using an assay based on the cleavage of the chromogenic peptide. In addition, the NINDS II library of 1040 compounds (MicroSource Discovery) was screened to identify hepsin inhibitors among established drugs and known bioactive molecules. Screens were performed in a 96-well format at a final compound concentration of 2 uM. To minimize false positives, positions 1 and 12 of each row contained DMSO/buffer controls. As a measure of reproducibility, the Z' score for this assay was 0.78 (Zhang et al., 1999 J Biomol Screen 4:67). B 5.62 pIC50 2420 nM IC50 US-9182402-B2. Hepsin inhibitors (2015)

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]