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

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ChEMBL ligand: CHEMBL336296 (Uridine 5'-triphosphate, UTP, Uridine triphosphate, Uridine-5'-triphosphate, INS-316, INS316)
  • 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 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 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 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 human P2Y2 F 7.22 pEC50 60 nM EC50 J. Med. Chem. (2011) 54: 4018-4033 [PMID:21528910]
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 B 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 26:

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]