UTP [Ligand Id: 1734] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL336296 (INS-316, INS316, Uridine 5'-triphosphate, Uridine-5'-triphosphate, Uridine triphosphate, UTP)
  • P2Y1 receptor/Purinergic receptor P2Y1 in Human [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900]
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  • P2Y11 receptor/Purinergic receptor P2Y11 in Human [ChEMBL: CHEMBL4867] [GtoPdb: 327] [UniProtKB: Q96G91]
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  • P2Y2 receptor/Purinergic receptor P2Y2 in Human [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231]
  • P2Y2 receptor/Purinergic receptor P2Y2 in Mouse [ChEMBL: CHEMBL1075298] [GtoPdb: 324] [UniProtKB: P35383]
  • P2Y2 receptor/Purinergic receptor P2Y2 in Rat [ChEMBL: CHEMBL4419] [GtoPdb: 324] [UniProtKB: P41232]
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  • P2Y4 receptor/Pyrimidinergic receptor P2Y4 in Human [ChEMBL: CHEMBL2123] [GtoPdb: 325] [UniProtKB: P51582]
  • P2Y4 receptor/Pyrimidinergic receptor P2Y4 in Rat [ChEMBL: CHEMBL2124] [GtoPdb: 325] [UniProtKB: O35811]
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  • P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
P2Y1 receptor/Purinergic receptor P2Y1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900]
ChEMBL Evaluated for agonist activity against phospholipase C coupled P2Y purinoceptor 1 (P2Y1) of human erythrocytes F 4 pEC50 >100000 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
ChEMBL Agonist activity at human cloned P2Y1 receptor expressed in human 1321N1 by FLIPR assay F 5.7 pEC50 >2000 nM EC50 Bioorg Med Chem Lett (2007) 17: 562-565 [PMID:17011188]
ChEMBL Agonist activity at human cloned P2Y1 receptor expressed in human 1321N1 by FLIPR assay F 5.7 pEC50 >2000 nM EC50 Bioorg Med Chem Lett (2007) 17: 558-561 [PMID:17079144]
P2Y11 receptor/Purinergic receptor P2Y11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4867] [GtoPdb: 327] [UniProtKB: Q96G91]
ChEMBL Agonist activity against phospholipase C coupled human P2Y purinoceptor 11 (P2Y11) F 4 pEC50 >100000 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
GtoPdb - - 5.2 pEC50 - - - Mol Pharmacol (2003) 63: 1356-63 [PMID:12761346]
P2Y2 receptor/Purinergic receptor P2Y2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231]
ChEMBL Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level F 4.69 pEC50 20600 nM EC50 J Med Chem (2009) 52: 2762-2775 [PMID:19419204]
ChEMBL Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level F 5.68 pEC50 2090 nM EC50 J Med Chem (2009) 52: 2762-2775 [PMID:19419204]
ChEMBL Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin) F 5.9 pEC50 1250 nM EC50 Bioorg Med Chem (2018) 26: 366-375 [PMID:29254895]
ChEMBL Agonist activity at P2Y2 receptor H184A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assay F 6 pEC50 996 nM EC50 J Med Chem (2017) 60: 8425-8440 [PMID:28938069]
ChEMBL Agonist activity at P2Y2 receptor Y288F mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assay F 6.04 pEC50 911 nM EC50 J Med Chem (2017) 60: 8425-8440 [PMID:28938069]
ChEMBL Agonist activity at N-terminal HA epitope-tagged wild type 1 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level F 6.11 pEC50 781 nM EC50 J Med Chem (2009) 52: 2762-2775 [PMID:19419204]
ChEMBL Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysis F 6.19 pEC50 640 nM EC50 Eur J Med Chem (2009) 44: 1525-1536 [PMID:18760862]
ChEMBL Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry F 6.19 pEC50 640 nM EC50 J Med Chem (2012) 55: 437-448 [PMID:22107038]
ChEMBL Activity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increase F 6.35 pEC50 450 nM EC50 J Med Chem (2006) 49: 1980-1990 [PMID:16539385]
ChEMBL Agonist activity at P2Y2 receptor in BEA cells (unknown origin) F 6.8 pEC50 160 nM EC50 Bioorg Med Chem (2018) 26: 366-375 [PMID:29254895]
ChEMBL Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level F 6.8 pEC50 157 nM EC50 J Med Chem (2009) 52: 2762-2775 [PMID:19419204]
ChEMBL Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2) F 6.85 pEC50 140 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
ChEMBL Agonist activity at human GFP-tagged P2Y2 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometry F 6.85 pEC50 140 nM EC50 Bioorg Med Chem (2012) 20: 5483-5495 [PMID:22901672]
ChEMBL Agonist activity at P2Y2 receptor (unknown origin) assessed as reduction in inositol phosphate accumulation F 6.85 pEC50 140 nM EC50 Bioorg Med Chem (2018) 26: 366-375 [PMID:29254895]
ChEMBL Agonist activity at human P2Y2 transfected in human 1321N1 cells B 6.85 pEC50 140 nM EC50 J Med Chem (2016) 59: 9981-10005 [PMID:27413802]
ChEMBL Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level F 6.86 pEC50 138 nM EC50 J Med Chem (2009) 52: 2762-2775 [PMID:19419204]
ChEMBL Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level F 6.91 pEC50 124 nM EC50 J Med Chem (2009) 52: 2762-2775 [PMID:19419204]
ChEMBL Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level F 6.92 pEC50 121 nM EC50 J Med Chem (2009) 52: 2762-2775 [PMID:19419204]
ChEMBL Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method F 6.92 pEC50 120 nM EC50 Bioorg Med Chem (2018) 26: 366-375 [PMID:29254895]
ChEMBL Agonist activity at P2Y2 receptor expressed in 1321N1 cells assessed as cytosolic calcium level F 6.96 pEC50 109.65 nM EC50 J Med Chem (2007) 50: 5600-5607 [PMID:17941622]
ChEMBL Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level F 6.97 pEC50 108 nM EC50 J Med Chem (2009) 52: 2762-2775 [PMID:19419204]
ChEMBL Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay F 7 pEC50 100 nM EC50 J Med Chem (2010) 53: 1673-1685 [PMID:20095577]
ChEMBL Agonist activity at P2Y2 receptor in human CF/T43 cells F 7 pEC50 100 nM EC50 Bioorg Med Chem (2018) 26: 366-375 [PMID:29254895]
ChEMBL Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level F 7.09 pEC50 80.4 nM EC50 J Med Chem (2009) 52: 2762-2775 [PMID:19419204]
ChEMBL Agonist activity at P2Y2 receptor S193A mutant (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assay F 7.15 pEC50 70.6 nM EC50 J Med Chem (2017) 60: 8425-8440 [PMID:28938069]
ChEMBL Agonist activity at human P2Y2 F 7.22 pEC50 60 nM EC50 J Med Chem (2011) 54: 4018-4033 [PMID:21528910]
ChEMBL Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay F 7.22 pEC50 60 nM EC50 J Med Chem (2010) 53: 4488-4501 [PMID:20446735]
ChEMBL Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay F 7.22 pEC50 60 nM EC50 Bioorg Med Chem (2008) 16: 6319-6332 [PMID:18514530]
ChEMBL Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level F 7.23 pEC50 59 nM EC50 J Med Chem (2009) 52: 2762-2775 [PMID:19419204]
ChEMBL Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay F 7.26 pEC50 55 nM EC50 J Med Chem (2011) 54: 4018-4033 [PMID:21528910]
ChEMBL Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level F 7.3 pEC50 50.1 nM EC50 J Med Chem (2009) 52: 2762-2775 [PMID:19419204]
ChEMBL Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C F 7.31 pEC50 49 nM EC50 J Med Chem (2007) 50: 1166-1176 [PMID:17302398]
ChEMBL Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA F 7.37 pEC50 43 nM EC50 J Med Chem (2006) 49: 7076-7087 [PMID:17125260]
ChEMBL Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level F 7.43 pEC50 37.2 nM EC50 J Med Chem (2009) 52: 2762-2775 [PMID:19419204]
ChEMBL Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y2 receptor F 7.52 pEC50 30 nM EC50 Bioorg Med Chem Lett (2001) 11: 157-160 [PMID:11206448]
ChEMBL Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting F 7.7 pEC50 20 nM EC50 Bioorg Med Chem (2012) 20: 2304-2315 [PMID:22386981]
ChEMBL Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay F 7.75 pEC50 17.9 nM EC50 J Med Chem (2011) 54: 2878-2890 [PMID:21417463]
GtoPdb - - 8.1 pEC50 - - - Br J Pharmacol (1995) 116: 1619-27 [PMID:8564228];
J Med Chem (2002) 45: 208-18 [PMID:11754592]
ChEMBL Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay F 8.15 pEC50 7 nM EC50 Bioorg Med Chem Lett (2007) 17: 558-561 [PMID:17079144]
ChEMBL Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay F 8.15 pEC50 7 nM EC50 Bioorg Med Chem Lett (2007) 17: 562-565 [PMID:17011188]
ChEMBL Agonist activity at wild type P2Y2 receptor (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assay F 8.25 pEC50 5.61 nM EC50 J Med Chem (2017) 60: 8425-8440 [PMID:28938069]
P2Y2 receptor/Purinergic receptor P2Y2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075298] [GtoPdb: 324] [UniProtKB: P35383]
ChEMBL Antagonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as inhibition of 1 uM UTP-induced intracellular calcium release preincubated 30 mins before UTP challenge by fluorescence assay F 5.82 pIC50 1510 nM IC50 Bioorg Med Chem (2009) 17: 5071-5079 [PMID:19523835]
ChEMBL Agonist activity at mouse P2Y2 receptor expressed in NG108-15 hybrid cells assessed as increase in intracellular calcium release by fluorescence assay F 5.9 pEC50 1260 nM EC50 Bioorg Med Chem (2009) 17: 5071-5079 [PMID:19523835]
P2Y2 receptor/Purinergic receptor P2Y2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4419] [GtoPdb: 324] [UniProtKB: P41232]
ChEMBL Activity against rat P2Y2-GFP transfected in HEK293 cells by intracellular calcium increase F 6.89 pEC50 130 nM EC50 J Med Chem (2006) 49: 1980-1990 [PMID:16539385]
P2Y4 receptor/Pyrimidinergic receptor P2Y4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2123] [GtoPdb: 325] [UniProtKB: P51582]
ChEMBL The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4) F 5.6 pEC50 2500 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
ChEMBL Agonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometry F 6.05 pEC50 900 nM EC50 Bioorg Med Chem (2012) 20: 5483-5495 [PMID:22901672]
ChEMBL Agonist activity at human P2Y4 transfected in human 1321N1 cells B 6.26 pEC50 550 nM EC50 J Med Chem (2016) 59: 9981-10005 [PMID:27413802]
GtoPdb - - 6.3 pEC50 - - - Mol Pharmacol (2000) 57: 926-31 [PMID:10779375]
ChEMBL Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay F 6.3 pEC50 500 nM EC50 J Med Chem (2010) 53: 1673-1685 [PMID:20095577]
ChEMBL Agonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry F 6.32 pEC50 480 nM EC50 J Med Chem (2012) 55: 437-448 [PMID:22107038]
ChEMBL Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysis F 6.32 pEC50 480 nM EC50 Eur J Med Chem (2009) 44: 1525-1536 [PMID:18760862]
ChEMBL Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor F 7 pEC50 100 nM EC50 Bioorg Med Chem Lett (2001) 11: 157-160 [PMID:11206448]
ChEMBL Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay F 7.05 pEC50 90 nM EC50 J Med Chem (2010) 53: 4488-4501 [PMID:20446735]
ChEMBL Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay F 7.05 pEC50 90 nM EC50 Bioorg Med Chem (2008) 16: 6319-6332 [PMID:18514530]
ChEMBL Agonist activity at human P2Y4 F 7.05 pEC50 90 nM EC50 J Med Chem (2011) 54: 4018-4033 [PMID:21528910]
ChEMBL Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay F 7.05 pEC50 88.4 nM EC50 J Med Chem (2011) 54: 2878-2890 [PMID:21417463]
ChEMBL Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA F 7.06 pEC50 87 nM EC50 J Med Chem (2006) 49: 7076-7087 [PMID:17125260]
ChEMBL Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay F 7.1 pEC50 80 nM EC50 J Med Chem (2011) 54: 4018-4033 [PMID:21528910]
ChEMBL Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C F 7.14 pEC50 73 nM EC50 J Med Chem (2007) 50: 1166-1176 [PMID:17302398]
ChEMBL Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay F 7.41 pEC50 39 nM EC50 Bioorg Med Chem Lett (2007) 17: 562-565 [PMID:17011188]
ChEMBL Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay F 7.41 pEC50 39 nM EC50 Bioorg Med Chem Lett (2007) 17: 558-561 [PMID:17079144]
P2Y4 receptor/Pyrimidinergic receptor P2Y4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2124] [GtoPdb: 325] [UniProtKB: O35811]
ChEMBL The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4) F 5.59 pEC50 2600 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
GtoPdb - - 5.6 pEC50 - - - Br J Pharmacol (1998) 124: 428-30 [PMID:9647463]
P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077]
ChEMBL Agonist activity at human recombinant P2Y6 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay F 5 pEC50 >10000 nM EC50 J Med Chem (2011) 54: 4018-4033 [PMID:21528910]
ChEMBL Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y6 receptor F 5 pEC50 >10000 nM EC50 Bioorg Med Chem Lett (2001) 11: 157-160 [PMID:11206448]
ChEMBL Agonist activity at human recombinant P2Y6 receptor expressed in 1321N1 cells assessed as intracellular calcium mobilization F 5 pEC50 >10000 nM EC50 J Med Chem (2007) 50: 1166-1176 [PMID:17302398]
ChEMBL Agonist activity at human P2Y6 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay F 5 pEC50 >10000 nM EC50 Bioorg Med Chem (2008) 16: 6319-6332 [PMID:18514530]
ChEMBL Agonist activity at human recombinant P2Y6 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay F 5 pEC50 >10000 nM EC50 J Med Chem (2010) 53: 4488-4501 [PMID:20446735]
GtoPdb - - 5.2 pEC50 - - - Biochem Biophys Res Commun (1996) 222: 303-8 [PMID:8670200]
ChEMBL The compound was evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 6 (P2Y6) F 5.22 pEC50 6000 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
ChEMBL Agonist activity at human recombinant P2Y6 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay F 5.22 pEC50 6000 nM EC50 J Med Chem (2011) 54: 2878-2890 [PMID:21417463]
ChEMBL Agonist activity at human cloned P2Y6 receptor expressed in human 1321N1 by FLIPR assay F 6.37 pEC50 424 nM EC50 Bioorg Med Chem Lett (2007) 17: 562-565 [PMID:17011188]

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]