PPTN [Ligand Id: 5802] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1800685
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
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  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
  • CB1 receptor/Cannabinoid CB1 receptor in Rat [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
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  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
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  • 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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  • P2Y14 receptor/Purinergic receptor P2Y14 in Human [ChEMBL: CHEMBL4518] [GtoPdb: 330] [UniProtKB: Q15391]
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  • P2Y2 receptor/Purinergic receptor P2Y2 in Human [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231]
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  • P2Y4 receptor/Pyrimidinergic receptor P2Y4 in Human [ChEMBL: CHEMBL2123] [GtoPdb: 325] [UniProtKB: P51582]
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  • P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL GPCRScan assay: inhibition of Alpha1B B 5.49 pKi 3235.94 nM Ki Data for DCP probe PPTN
ChEMBL GPCRScan assay: inhibition of Alpha1B B 5.49 pKi 3230.73 nM Ki Data for DCP probe PPTN
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL GPCRScan assay: inhibition of Alpha2B B 5.59 pKi 2570.4 nM Ki Data for DCP probe PPTN
ChEMBL GPCRScan assay: inhibition of Alpha2B B 5.59 pKi 2561.53 nM Ki Data for DCP probe PPTN
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL GPCRScan assay: inhibition of Beta3 B 5.53 pKi 2951.21 nM Ki Data for DCP probe PPTN
ChEMBL GPCRScan assay: inhibition of Beta3 B 5.53 pKi 2918.77 nM Ki Data for DCP probe PPTN
CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL Agonist activity at CB1 receptor (unknown origin) B 5 pEC50 >10000 nM EC50 J Med Chem (2020) 63: 9563-9589 [PMID:32787142]
ChEMBL Antagonist activity at CB1 receptor (unknown origin) B 5 pEC50 >10000 nM EC50 J Med Chem (2020) 63: 9563-9589 [PMID:32787142]
CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
ChEMBL Antagonist activity at rat brain CB2 receptor expressed in HEK-Flp-In cells in presence of [3H]CP55940 measured after overnight incubation by Bright-Glo luminescence assay B 4.3 pIC50 >50000 nM IC50 ACS Med Chem Lett (2020) 11: 1281-1286 [PMID:32551012]
ChEMBL Antagonist activity at rat brain CB1 receptor expressed in HEK-Flp-In cells in presence of [3H]CP55940 measured after overnight incubation by Bright-Glo luminescence assay B 4.3 pIC50 >50000 nM IC50 ACS Med Chem Lett (2020) 11: 1281-1286 [PMID:32551012]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Agonist activity at CB2 receptor (unknown origin) B 5 pEC50 >10000 nM EC50 J Med Chem (2020) 63: 9563-9589 [PMID:32787142]
ChEMBL Antagonist activity at CB2 receptor (unknown origin) B 5 pEC50 >10000 nM EC50 J Med Chem (2020) 63: 9563-9589 [PMID:32787142]
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Binding affinity to human delta opioid receptor expressed in HEK cells by PDSP assay B 5.56 pKi 2750 nM Ki J Med Chem (2016) 59: 6149-6168 [PMID:27331270]
ChEMBL Binding affinity to DOR (unknown origin) B 5.56 pKi 2750 nM Ki J Med Chem (2020) 63: 9563-9589 [PMID:32787142]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL GPCRScan assay: inhibition of D1 B 5 pKi 10000 nM Ki Data for DCP probe PPTN
ChEMBL GPCRScan assay: inhibition of D1 B 5 pKi 10000 nM Ki Data for DCP probe PPTN
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Binding affinity to DRD3 (unknown origin) B 5.17 pKi 6790 nM Ki J Med Chem (2020) 63: 9563-9589 [PMID:32787142]
ChEMBL GPCRScan assay: inhibition of D3 B 6.05 pKi 891.25 nM Ki Data for DCP probe PPTN
ChEMBL GPCRScan assay: inhibition of D3 B 6.05 pKi 884.3 nM Ki Data for DCP probe PPTN
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL Binding affinity to rat D3 dopamine receptor expressed in HEK293T cells by PDSP assay B 5.17 pKi 6790 nM Ki J Med Chem (2016) 59: 6149-6168 [PMID:27331270]
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
ChEMBL GPCRScan assay: inhibition of D5 B 5.55 pKi 2819.68 nM Ki Data for DCP probe PPTN
ChEMBL GPCRScan assay: inhibition of D5 B 5.55 pKi 2818.38 nM Ki Data for DCP probe PPTN
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of full length human ERG expressed in CHO cells by patch-clamp method B 4.52 pEC50 >30000 nM EC50 J Med Chem (2021) 64: 5099-5122 [PMID:33787273]
P2Y14 receptor in Human [GtoPdb: 330] [UniProtKB: Q15391]
GtoPdb - - 10.1 pKi 0.43 nM KB Mol Pharmacol (2013) 84: 41-9 [PMID:23592514]
P2Y14 receptor/P2Y purinoceptor 14 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770046] [GtoPdb: 330] [UniProtKB: Q9ESG6]
ChEMBL Inhibition of mouse P2Y14 receptor in presence of 2% HSA B 7.46 pKi 35 nM Ki Eur J Med Chem (2019) 175: 34-39 [PMID:31071548]
ChEMBL Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis B 7.67 pIC50 21.6 nM IC50 ACS Med Chem Lett (2020) 11: 1281-1286 [PMID:32551012]
ChEMBL Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay B 7.67 pIC50 21.6 nM IC50 J Med Chem (2020) 63: 9563-9589 [PMID:32787142]
P2Y14 receptor/P2Y purinoceptor 14 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295660] [GtoPdb: 330] [UniProtKB: O35881]
ChEMBL Antagonist activity at P2Y14R in rat C6 cells assessed as suppression of UDP-glucose-mediated inhibition of forskolin-stimulated [3H]cyclic-AMP accumulation after 15 mins in presence of [3H]-adenine B 9.4 pKi 0.4 nM Ki J Med Chem (2018) 61: 4860-4882 [PMID:29767967]
P2Y1 receptor/Purinergic receptor P2Y1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900]
ChEMBL Antagonist activity human P2Y1R expressed in human 1321N1 cells assessed as inhibition of 2MeSADP-induced [3H]inositol phosphate accumulation after 30 mins by liquid scintillation counting method F 5 pIC50 >10000 nM IC50 J Med Chem (2016) 59: 6149-6168 [PMID:27331270]
P2Y11 receptor/Purinergic receptor P2Y11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4867] [GtoPdb: 327] [UniProtKB: Q96G91]
ChEMBL Antagonist activity human P2Y11R expressed in human 1321N1 cells assessed as inhibition of ATP-induced [3H]inositol phosphate accumulation after 30 mins by liquid scintillation counting method F 5 pIC50 >10000 nM IC50 J Med Chem (2016) 59: 6149-6168 [PMID:27331270]
P2Y14 receptor/Purinergic receptor P2Y14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4518] [GtoPdb: 330] [UniProtKB: Q15391]
ChEMBL Binding assay with 2% HSA B 7.46 pKi 35 nM Ki Data for DCP probe PPTN
ChEMBL Binding assay (no HSA) B 8.64 pKi 2.3 nM Ki Data for DCP probe PPTN
ChEMBL Antagonist activity at human P2Y14 expressed in CHO cells assessed as inhibition of forskolin-induced increase of cAMP accumulation incubated for 15 mins in presence of IBMX F 9.37 pKi 0.43 nM Ki J Med Chem (2022) 65: 3434-3459 [PMID:35113556]
GtoPdb - - 10.1 pKi 0.43 nM KB Mol Pharmacol (2013) 84: 41-9 [PMID:23592514]
ChEMBL Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assay B 7.72 pIC50 19 nM IC50 J Med Chem (2020) 63: 9563-9589 [PMID:32787142]
ChEMBL Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assay B 7.84 pIC50 14.5 nM IC50 J Med Chem (2020) 63: 9563-9589 [PMID:32787142]
ChEMBL Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assay B 8.01 pIC50 9.75 nM IC50 J Med Chem (2020) 63: 9563-9589 [PMID:32787142]
ChEMBL Inhibition of fluorescent antagonist binding to human P2Y14 expressed in CHO cells incubated for 30 mins B 8.1 pIC50 8 nM IC50 J Med Chem (2022) 65: 3434-3459 [PMID:35113556]
ChEMBL Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method B 8.1 pIC50 7.96 nM IC50 J Med Chem (2018) 61: 4860-4882 [PMID:29767967]
ChEMBL Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis B 8.22 pIC50 6 nM IC50 ACS Med Chem Lett (2020) 11: 1281-1286 [PMID:32551012]
ChEMBL Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis B 8.22 pIC50 6 nM IC50 J Med Chem (2016) 59: 6149-6168 [PMID:27331270]
ChEMBL Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay F 8.7 pIC50 1.98 nM IC50 Eur J Med Chem (2019) 181: 111564-111564 [PMID:31376563]
ChEMBL Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay F 8.7 pIC50 1.98 nM IC50 Eur J Med Chem (2021) 216: 113313-113313 [PMID:33667846]
ChEMBL FLIPR assay B 9.3 pIC50 0.5 nM IC50 Data for DCP probe PPTN
ChEMBL Antagonist activity human P2Y14R expressed in African green monkey COS7 cells assessed as inhibition of UDPG-induced [3H]inositol phosphate accumulation after 30 mins by liquid scintillation counting method F 9.4 pIC50 0.4 nM IC50 J Med Chem (2016) 59: 6149-6168 [PMID:27331270]
P2Y2 receptor/Purinergic receptor P2Y2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231]
ChEMBL Antagonist activity human P2Y2R expressed in human 1321N1 cells assessed as inhibition of UTP-induced [3H]inositol phosphate accumulation after 30 mins by liquid scintillation counting method F 5 pIC50 >10000 nM IC50 J Med Chem (2016) 59: 6149-6168 [PMID:27331270]
P2Y4 receptor/Pyrimidinergic receptor P2Y4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2123] [GtoPdb: 325] [UniProtKB: P51582]
ChEMBL Antagonist activity human P2Y4R expressed in human 1321N1 cells assessed as inhibition of UTP-induced [3H]inositol phosphate accumulation after 30 mins by liquid scintillation counting method F 5 pIC50 >10000 nM IC50 J Med Chem (2016) 59: 6149-6168 [PMID:27331270]
P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077]
ChEMBL Antagonist activity human P2Y6R expressed in human 1321N1 cells assessed as inhibition of UDP-induced [3H]inositol phosphate accumulation after 30 mins by liquid scintillation counting method F 5 pIC50 >10000 nM IC50 J Med Chem (2016) 59: 6149-6168 [PMID:27331270]
σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2]
ChEMBL GPCRScan assay: inhibition of Sigma 2 B 5.95 pKi 1122.02 nM Ki Data for DCP probe PPTN
ChEMBL GPCRScan assay: inhibition of Sigma 2 B 5.95 pKi 1120.99 nM Ki Data for DCP probe PPTN
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL GPCRScan assay: inhibition of Sigma 1 B 5.93 pKi 1180.59 nM Ki Data for DCP probe PPTN
ChEMBL GPCRScan assay: inhibition of Sigma 1 B 5.93 pKi 1174.9 nM Ki Data for DCP probe PPTN
Uncharacterized protein in Pan troglodytes (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3831325] [UniProtKB: A0A2J8P2M1]
ChEMBL Antagonist activity against chimpanzee GPR105 expressed in stable HEK cells co-expressing chimeric G-protein Gqi5 assessed as inhibition of UDP-glucose-induced Ca2+ signaling response incubated for 20 mins by FLIPR assay F 8.66 pIC50 2.2 nM IC50 US-20100298347-A1. Substituted 2-naphthoic acids as antagonists of gpr105 activity (2010)

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]