[3H]AMPA [Ligand Id: 4077] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL13378
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  • GluN2C/Glutamate [NMDA] receptor subunit epsilon 3 in Rat [ChEMBL: CHEMBL401] [GtoPdb: 458] [UniProtKB: Q00961]
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  • GluN1/Glutamate (NMDA) receptor subunit zeta 1 in Rat [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439]
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  • GluA1/Glutamate receptor ionotropic, AMPA 1 in Human [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261]
  • GluA1/Glutamate receptor ionotropic, AMPA 1 in Mouse [ChEMBL: CHEMBL3502] [GtoPdb: 444] [UniProtKB: P23818]
  • GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490]
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  • GluA2/Glutamate receptor ionotropic, AMPA 2 in Human [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262]
  • GluA2/Glutamate receptor ionotropic, AMPA 2 in Rat [ChEMBL: CHEMBL3503] [GtoPdb: 445] [UniProtKB: P19491]
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  • GluA3/Glutamate receptor ionotropic, AMPA 3 in Human [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263]
  • GluA3/Glutamate receptor ionotropic, AMPA 3 in Rat [ChEMBL: CHEMBL3504] [GtoPdb: 446] [UniProtKB: P19492]
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  • GluA4/Glutamate receptor ionotropic, AMPA 4 in Human [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058]
  • GluA4/Glutamate receptor ionotropic, AMPA 4 in Rat [ChEMBL: CHEMBL3505] [GtoPdb: 447] [UniProtKB: P19493]
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  • GluK1/Glutamate receptor ionotropic kainate 1 in Human [ChEMBL: CHEMBL1918] [GtoPdb: 450] [UniProtKB: P39086]
  • GluK1/Glutamate receptor ionotropic kainate 1 in Rat [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756]
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  • GluK2/Glutamate receptor ionotropic kainate 2 in Human [ChEMBL: CHEMBL3683] [GtoPdb: 451] [UniProtKB: Q13002]
  • GluK2/Glutamate receptor ionotropic kainate 2 in Rat [ChEMBL: CHEMBL3607] [GtoPdb: 451] [UniProtKB: P42260]
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  • GluK3/Glutamate receptor ionotropic kainate 3 in Rat [ChEMBL: CHEMBL3744] [GtoPdb: 452] [UniProtKB: P42264]
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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: 459461455456457458460] [UniProtKB: O15399O60391Q05586Q12879Q13224Q14957Q8TCU5]
ChEMBL In vitro binding affinity against N-methyl-D-aspartate glutamate receptor using [3H]-CPG 39653 as radioligand B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1997) 40: 2831-2842 [PMID:9288165]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL Displacement of [3H]CGP 39653 from NMDA receptor in rat synaptosomes B 4 pKi >100000 nM Ki J. Med. Chem. (2007) 50: 2408-2414 [PMID:17455929]
ChEMBL Displacement of [3H]CGP39653 from NMDA receptor in Sprague-Dawley rat brain membranes B 4 pKi >100000 nM Ki J. Med. Chem. (2010) 53: 4110-4118 [PMID:20408529]
ChEMBL Binding affinity for N-methyl-D-aspartate glutamate receptor (NMDA) using [3H]- CPP B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2002) 45: 19-31 [PMID:11754576]
ChEMBL Compound was evaluated for the inhibition of binding of [3H]- CPP to NMDA receptor B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1994) 37: 878-884 [PMID:7512140]
ChEMBL Compound was evaluated for the inhibition of binding of [3H]- MK-801 to NMDA receptor B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1994) 37: 878-884 [PMID:7512140]
ChEMBL Binding affinity by measuring displacement of [3H]CPP from NMDA receptor in rat cortical slice preparation B 4 pIC50 >100000 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 1649-1654
ChEMBL Concentration required for 50% inhibition of [3H]-CPP binding to N-methyl-D-aspartate glutamate receptor in rat cortical slice preparation B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1992) 35: 3512-3519 [PMID:1383544]
ChEMBL Concentration required for 50% inhibition of [3H]-MK-801 binding to N-methyl-D-aspartate glutamate receptor in rat cortical slice preparation B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1992) 35: 3512-3519 [PMID:1383544]
GluN2C/Glutamate [NMDA] receptor subunit epsilon 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL401] [GtoPdb: 458] [UniProtKB: Q00961]
ChEMBL Binding affinity of compound was determined against N-methyl-D-aspartate glutamate receptor, using radioligand [3H]- CGP-39653 B 4 pKi >100000 nM Ki J. Med. Chem. (2003) 46: 2246-2249 [PMID:12747796]
GluN1/Glutamate (NMDA) receptor subunit zeta 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439]
ChEMBL Compound was evaluated for the inhibition of binding of [3H]glycine to NMDA receptor B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1994) 37: 878-884 [PMID:7512140]
GluA1/GluA2/Glutamate receptor AMPA 1/2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3883294] [GtoPdb: 444445] [UniProtKB: P42261P42262]
ChEMBL Agonist activity at recombinant GluA1A2 receptor flip isoform expressed in Xenopus oocytes F 5.48 pEC50 3310 nM EC50 Bioorg. Med. Chem. (2010) 18: 1381-1387 [PMID:20096591]
GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic AMPA in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2096670] [GtoPdb: 444445446447] [UniProtKB: P42261P42262P42263P48058]
ChEMBL Inhibition of the binding of radioligand [3H]AMPA in the presence at low-affinity AMPA receptor sites. B 6.44 pIC50 364 nM IC50 J. Med. Chem. (1991) 34: 123-130 [PMID:1825114]
ChEMBL In vitro binding affinity against Ionotropic glutamate receptor AMPA using [3H]AMPA as radioligand B 7.64 pIC50 23 nM IC50 J. Med. Chem. (1997) 40: 2831-2842 [PMID:9288165]
ChEMBL Inhibition of the binding of radioligand [3H]AMPA in the presence at high-affinity AMPA receptor sites. B 7.72 pIC50 19 nM IC50 J. Med. Chem. (1991) 34: 123-130 [PMID:1825114]
GluA1/GluA2/GluA4/GluA3/Glutamate receptor ionotropic, AMPA in Mouse (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2096617] [GtoPdb: 444445447446] [UniProtKB: P23818P23819Q9Z2W8Q9Z2W9]
ChEMBL Compound was tested for in vitro binding affinity against Ionotropic glutamate receptor AMPA using [3H]AMPA ligand B 7.4 pIC50 40 nM IC50 J. Med. Chem. (1998) 41: 930-939 [PMID:9526567]
GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic, AMPA in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093871] [GtoPdb: 444445446447] [UniProtKB: P19490P19491P19492P19493]
ChEMBL Concentration required for 50% inhibition of [3H]Glu binding to AMPA receptor in rat cortical slice preparation in the presence of 2.5 mM CaCl2 B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1992) 35: 3512-3519 [PMID:1383544]
ChEMBL Tested for inhibition of Specific DL-[H]Ionotropic glutamate receptor AMPA binding to rat brain membranes B 6.1 pIC50 800 nM IC50 J. Med. Chem. (1983) 26: 901-903 [PMID:6133955]
ChEMBL Binding affinity at Ionotropic glutamate receptor AMPA, using [3H]AMPA receptor binding assay. B 7.1 pIC50 79 nM IC50 J. Med. Chem. (1992) 35: 107-111 [PMID:1370693]
ChEMBL Concentration required for 50% inhibition of [3H]AMPA binding to AMPA receptor in rat cortical slice preparation B 7.22 pIC50 60 nM IC50 J. Med. Chem. (1992) 35: 3512-3519 [PMID:1383544]
ChEMBL Binding affinity by measuring displacement of [3H]AMPA from Ionotropic glutamate receptor AMPA in rat cortical slice preparation B 7.4 pIC50 40 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 1649-1654
ChEMBL Binding affinity for Ionotropic glutamate receptor AMPA using [3H]- AMPA B 7.4 pIC50 40 nM IC50 J. Med. Chem. (2002) 45: 19-31 [PMID:11754576]
ChEMBL Compound was evaluated for the inhibition of binding of [3H]AMPA to the AMPA receptor B 7.4 pIC50 40 nM IC50 J. Med. Chem. (1994) 37: 878-884 [PMID:7512140]
ChEMBL In vitro binding affinity for Ionotropic glutamate receptor AMPA site was determined using [3H]AMPA as radioligand in rat cortex B 7.4 pIC50 40 nM IC50 J. Med. Chem. (1997) 40: 520-527 [PMID:9046343]
ChEMBL Compound was evaluated for the agonist activity on AMPA receptor in rat cortical wedge preparation F 5.46 pEC50 3500 nM EC50 J. Med. Chem. (1994) 37: 878-884 [PMID:7512140]
GluA1/Glutamate receptor ionotropic, AMPA 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261]
ChEMBL Binding affinity of compound was determined towards cloned Ionotropic glutamate receptor AMPA 1 (GluR1) expressed in Sf 9 insect cells B 7.66 pKi 22 nM Ki J. Med. Chem. (2003) 46: 2246-2249 [PMID:12747796]
GluA1/Glutamate receptor ionotropic, AMPA 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3502] [GtoPdb: 444] [UniProtKB: P23818]
ChEMBL Effective concentration of compound was determined for electrophysiological properties on Ionotropic glutamate receptor AMPA 1 using rat cortical slice model in Xenopus laevis oocytes F 5.06 pEC50 8700 nM EC50 J. Med. Chem. (2003) 46: 2246-2249 [PMID:12747796]
GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490]
ChEMBL Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR1 expressed in Sf9 cells B 7.66 pKi 21.9 nM Ki J. Med. Chem. (2008) 51: 6614-6618 [PMID:18811139]
ChEMBL Displacement of [3H]AMPA from rat recombinant GluR1 expressed in Sf9 cells B 10.66 pKi 0.02 nM Ki J. Med. Chem. (2007) 50: 2408-2414 [PMID:17455929]
ChEMBL Binding affinity of compound was determined against Ionotropic glutamate receptor AMPA receptor, using radioligand [3H]- AMPA B 7.4 pIC50 40 nM IC50 J. Med. Chem. (2003) 46: 2246-2249 [PMID:12747796]
ChEMBL Agonist activity at rat recombinant GluA1 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay F 4.28 pEC50 53000 nM EC50 Bioorg. Med. Chem. (2010) 18: 1381-1387 [PMID:20096591]
ChEMBL Agonist activity at rat recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes F 5.06 pEC50 8700 nM EC50 Bioorg. Med. Chem. (2010) 18: 1381-1387 [PMID:20096591]
GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262]
ChEMBL Binding affinity of compound was determined towards cloned Ionotropic glutamate receptor AMPA 2 (GluR2) expressed in Sf 9 insect cells B 7.77 pKi 17 nM Ki J. Med. Chem. (2003) 46: 2246-2249 [PMID:12747796]
GluA2/Glutamate receptor ionotropic, AMPA 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3503] [GtoPdb: 445] [UniProtKB: P19491]
ChEMBL Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR2(R) expressed in Sf9 cells B 7.77 pKi 16.8 nM Ki J. Med. Chem. (2008) 51: 6614-6618 [PMID:18811139]
ChEMBL Displacement of [3H]AMPA from rat recombinant GluR2 expressed in Sf9 cells B 10.77 pKi 0.02 nM Ki J. Med. Chem. (2007) 50: 2408-2414 [PMID:17455929]
ChEMBL Agonist activity at rat recombinant GluA2 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay F 4.17 pEC50 67000 nM EC50 Bioorg. Med. Chem. (2010) 18: 1381-1387 [PMID:20096591]
GluA3/Glutamate receptor ionotropic, AMPA 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263]
ChEMBL Binding affinity of compound was determined towards cloned Ionotropic glutamate receptor AMPA 3 (GluR3) expressed in Sf 9 insect cells B 7.68 pKi 21 nM Ki J. Med. Chem. (2003) 46: 2246-2249 [PMID:12747796]
GluA3/Glutamate receptor ionotropic, AMPA 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3504] [GtoPdb: 446] [UniProtKB: P19492]
ChEMBL Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR3 expressed in Sf9 cells B 7.69 pKi 20.6 nM Ki J. Med. Chem. (2008) 51: 6614-6618 [PMID:18811139]
ChEMBL Displacement of [3H]AMPA from rat recombinant GluR3 expressed in Sf9 cells B 10.68 pKi 0.02 nM Ki J. Med. Chem. (2007) 50: 2408-2414 [PMID:17455929]
ChEMBL Agonist activity at rat recombinant GluA3 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay F 4.43 pEC50 37000 nM EC50 Bioorg. Med. Chem. (2010) 18: 1381-1387 [PMID:20096591]
ChEMBL Effective concentration of compound was determined for electrophysiological properties on Ionotropic glutamate receptor AMPA 3 (GluR3) using rat cortical slice model in Xenopus laevis oocytes F 5.85 pEC50 1400 nM EC50 J. Med. Chem. (2003) 46: 2246-2249 [PMID:12747796]
ChEMBL Agonist activity at rat recombinant GluA3 receptor flop isoform expressed in Xenopus oocytes F 5.85 pEC50 1400 nM EC50 Bioorg. Med. Chem. (2010) 18: 1381-1387 [PMID:20096591]
GluA4/Glutamate receptor ionotropic, AMPA 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058]
ChEMBL Binding affinity of compound was determined towards cloned Ionotropic glutamate receptor AMPA 4 (GluR4) expressed in Sf 9 insect cells B 7.4 pKi 40 nM Ki J. Med. Chem. (2003) 46: 2246-2249 [PMID:12747796]
GluA4/Glutamate receptor ionotropic, AMPA 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3505] [GtoPdb: 447] [UniProtKB: P19493]
ChEMBL Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR4 expressed in Sf9 cells B 7.4 pKi 40 nM Ki J. Med. Chem. (2008) 51: 6614-6618 [PMID:18811139]
ChEMBL Displacement of [3H]AMPA from rat recombinant GluR4 expressed in Sf9 cells B 10.4 pKi 0.04 nM Ki J. Med. Chem. (2007) 50: 2408-2414 [PMID:17455929]
ChEMBL Agonist activity at rat recombinant GluA4 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay F 4.8 pEC50 16000 nM EC50 Bioorg. Med. Chem. (2010) 18: 1381-1387 [PMID:20096591]
GluK1/GluK2/GluK3/GluK4/GluK5/Glutamate receptor ionotropic kainate in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2109241] [GtoPdb: 450451452453454] [UniProtKB: P39086Q13002Q13003Q16099Q16478]
ChEMBL In vitro binding affinity against Ionotropic glutamate receptor kainate (kainic acid) using [3H]KAIN as radioligand B 4.17 pIC50 68000 nM IC50 J. Med. Chem. (1997) 40: 2831-2842 [PMID:9288165]
GluK1/GluK2/GluK3/GluK4/GluK5/Glutamate receptor ionotropic, kainate in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094119] [GtoPdb: 450451452453454] [UniProtKB: P22756P42260P42264Q01812Q63273]
ChEMBL Binding affinity for Ionotropic glutamate receptor using [3H]- kainic acid B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2002) 45: 19-31 [PMID:11754576]
ChEMBL Compound was evaluated for the inhibition of binding of [3H]-Kainic acid to kianic acid receptor B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1994) 37: 878-884 [PMID:7512140]
ChEMBL Binding affinity by measuring displacement of [3H]KAIN from Ionotropic glutamate receptor kainate in rat cortical slice preparation B 4 pIC50 >100000 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 1649-1654
ChEMBL Concentration required for 50% inhibition of [3H]-kainic acid binding to ionotropic glutamate receptor ionotropic kainate in rat cortical slice preparation B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1992) 35: 3512-3519 [PMID:1383544]
ChEMBL Binding affinity was measured by [3H]- Ionotropic glutamate receptor ionotropic kainate binding assay. B 4.3 pIC50 50100 nM IC50 J. Med. Chem. (1992) 35: 107-111 [PMID:1370693]
ChEMBL Inhibition of [3H]- Kainate binding to Ionotropic glutamate receptor kainate in brain homogenates. B 7.92 pIC50 12 nM IC50 J. Med. Chem. (1996) 39: 4430-4438 [PMID:8893837]
GluK1/Glutamate receptor ionotropic kainate 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1918] [GtoPdb: 450] [UniProtKB: P39086]
ChEMBL Binding affinity of compound was determined towards cloned Ionotropic glutamate receptor ionotropic kainate 1 (GluR5) expressed in Sf 9 insect cells B 6.13 pKi 740 nM Ki J. Med. Chem. (2003) 46: 2246-2249 [PMID:12747796]
GluK1/Glutamate receptor ionotropic kainate 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756]
ChEMBL Displacement of [3H]SYM2081 from rat recombinant iGluR5(Q)1b expressed in Sf9 cells B 5.94 pKi 1150 nM Ki J. Med. Chem. (2008) 51: 6614-6618 [PMID:18811139]
ChEMBL Displacement of [3H]SYM 2081 from rat recombinant GluR5 expressed in Sf9 cells B 8.92 pKi 1.2 nM Ki J. Med. Chem. (2007) 50: 2408-2414 [PMID:17455929]
GluK2/Glutamate receptor ionotropic kainate 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3683] [GtoPdb: 451] [UniProtKB: Q13002]
ChEMBL Binding affinity of compound was determined towards cloned Ionotropic glutamate receptor ionotropic kainate 6 (GluR6) expressed in Sf 9 insect cells B 4 pKi >100000 nM Ki J. Med. Chem. (2003) 46: 2246-2249 [PMID:12747796]
GluK2/Glutamate receptor ionotropic kainate 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3607] [GtoPdb: 451] [UniProtKB: P42260]
ChEMBL Displacement of [3H]KA from rat recombinant GluR6 expressed in Sf9 cells B 6 pKi >1000 nM Ki J. Med. Chem. (2007) 50: 2408-2414 [PMID:17455929]
GluK3/Glutamate receptor ionotropic kainate 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3744] [GtoPdb: 452] [UniProtKB: P42264]
ChEMBL Binding affinity of compound was determined against Ionotropic glutamate receptor ionotropic kainate, using radioligand [3H]- KA B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2003) 46: 2246-2249 [PMID:12747796]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]