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ChEMBL ligand: CHEMBL336296 (INS-316, INS316, Uridine 5'-triphosphate, Uridine-5'-triphosphate, Uridine triphosphate, UTP) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 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 | 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 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 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 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 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 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 | F | 7.22 | pEC50 | 60 | nM | EC50 | J Med Chem (2011) 54: 4018-4033 [PMID:21528910] |
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: 562-565 [PMID:17011188] |
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 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] |
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 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 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 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 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 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 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 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]