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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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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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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  • CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271]
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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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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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  • NTS1 receptor/Neurotensin receptor 1 in Human [ChEMBL: CHEMBL4123] [GtoPdb: 309] [UniProtKB: P30989]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • phosphodiesterase 2A/Phosphodiesterase 2A in Human [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
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  • phosphodiesterase 5A/Phosphodiesterase 5A in Human [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
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  • EP3 receptor/Prostanoid EP3 receptor in Human [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
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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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  • P2Y12 receptor/Purinergic receptor P2Y12 in Human [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
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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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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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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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  • SST4 receptor/Somatostatin receptor 4 in Human [ChEMBL: CHEMBL1853] [GtoPdb: 358] [UniProtKB: P31391]
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  • Vesicular monoamine transporter 2/Synaptic vesicular amine transporter in Human [ChEMBL: CHEMBL1893] [GtoPdb: 1012] [UniProtKB: Q05940]
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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
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Adrenergic alpha2A Eurofins-Panlabs radioligand binding assay B 5.82 pKi 1530 nM Ki Data for DCP probe PPTN
ChEMBL Adrenergic alpha2A Eurofins-Panlabs radioligand binding assay B 5.39 pIC50 4070 nM IC50 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
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Adrenergic alpha2C Eurofins-Panlabs radioligand binding assay B 6 pKi 1000 nM Ki Data for DCP probe PPTN
ChEMBL Adrenergic alpha2C Eurofins-Panlabs radioligand binding assay B 5.16 pIC50 6880 nM IC50 Data for DCP probe PPTN
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL Inhibition of Adrenergic beta3 at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_204200) B 5.14 pKi 7200 nM Ki Data for DCP probe PPTN
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
ChEMBL Inhibition of Adrenergic beta3 at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_204200) B 5.02 pIC50 9610 nM IC50 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]
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
ChEMBL Inhibition of Cyclooxygenase COX-2 at 10 µM in the Eurofins-Panlabs enzyme assay (Eurofins_assay_118010) B 5.06 pIC50 8710 nM IC50 Data for DCP probe PPTN
CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271]
ChEMBL Inhibition of Leukotriene, Cysteinyl CysLT1 at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_250460) B 6.64 pKi 230 nM Ki Data for DCP probe PPTN
ChEMBL Inhibition of Leukotriene, Cysteinyl CysLT1 at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_250460) B 6.25 pIC50 560 nM IC50 Data for DCP probe PPTN
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 Inhibition of Dopamine D3 at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_219800) B 5.57 pKi 2700 nM Ki Data for DCP probe PPTN
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
ChEMBL Inhibition of Dopamine D3 at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_219800) B 5.1 pIC50 7940 nM IC50 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
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL Inhibition of Transporter, Dopamine (DAT) at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_220320) B 5.74 pKi 1830 nM Ki Data for DCP probe PPTN
ChEMBL Inhibition of Transporter, Dopamine (DAT) at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_220320) B 5.64 pIC50 2310 nM IC50 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]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Inhibition of Opiate kappa (OP2, KOP) at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_260210) B 5.49 pKi 3210 nM Ki Data for DCP probe PPTN
ChEMBL Inhibition of Opiate kappa (OP2, KOP) at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_260210) B 5.1 pIC50 8030 nM IC50 Data for DCP probe PPTN
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL NanoBRET (SGC Frankfurt) (MAPK14) B 4.7 pIC50 >20000 nM IC50 Data for DCP probe PPTN
NTS1 receptor/Neurotensin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4123] [GtoPdb: 309] [UniProtKB: P30989]
ChEMBL Neurotensin NT1 Eurofins-Panlabs radioligand binding assay B 5.16 pKi 6970 nM Ki Data for DCP probe PPTN
ChEMBL Neurotensin NT1 Eurofins-Panlabs radioligand binding assay B 5.06 pIC50 8660 nM IC50 Data for DCP probe PPTN
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Inhibition of Transporter, Norepinephrine (NET) at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_204410) B 5.49 pKi 3270 nM Ki Data for DCP probe PPTN
ChEMBL Inhibition of Transporter, Norepinephrine (NET) at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_204410) B 5.48 pIC50 3300 nM IC50 Data for DCP probe PPTN
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]
phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
ChEMBL Phosphodiesterase PDE2 Eurofins-Panlabs enzyme assay B 4.06 pIC50 86900 nM IC50 Data for DCP probe PPTN
phosphodiesterase 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
ChEMBL Inhibition of Phosphodiesterase PDE5 at 10 µM in the Eurofins-Panlabs enzyme assay (Eurofins_assay_156000) B 4.42 pIC50 38200 nM IC50 Data for DCP probe PPTN
EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
ChEMBL Prostanoid EP3 Eurofins-Panlabs radioligand binding assay B 5.03 pIC50 9270 nM IC50 Data for DCP probe PPTN
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]
ChEMBL Antagonist activity at P2Y1R (unknown origin) expressed in human 1321N1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 15 mins in presence of IBMX by chromatography F 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 15967-15990 [PMID:36394994]
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]
ChEMBL Antagonist activity at P2Y11R (unknown origin) expressed in human 1321N1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 15 mins in presence of IBMX by chromatography F 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 15967-15990 [PMID:36394994]
P2Y12 receptor/Purinergic receptor P2Y12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
ChEMBL Antagonist activity at P2Y12R (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 15 mins in presence of IBMX by chromatography F 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 15967-15990 [PMID:36394994]
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]
ChEMBL Antagonist activity at human P2Y14R stably expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by measuring inhibition constant incubated for 15 mins in presence of IBMX by chromatography F 9.37 pKi 0.43 nM Ki J Med Chem (2023) 66: 9076-9094 [PMID:37382926]
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 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 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 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 P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay F 8.7 pIC50 1.98 nM IC50 J Med Chem (2022) 65: 15967-15990 [PMID:36394994]
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]
ChEMBL Antagonist activity at P2Y14R (unknown origin) expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 15 mins in presence of IBMX by chromatography F 9.4 pIC50 0.4 nM IC50 J Med Chem (2022) 65: 15967-15990 [PMID:36394994]
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]
ChEMBL Antagonist activity at P2Y2R (unknown origin) expressed in human 1321N1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 15 mins in presence of IBMX by chromatography F 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 15967-15990 [PMID:36394994]
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]
ChEMBL Antagonist activity at P2Y4R (unknown origin) expressed in human 1321N1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 15 mins in presence of IBMX by chromatography F 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 15967-15990 [PMID:36394994]
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]
ChEMBL Antagonist activity at P2Y6R (unknown origin) expressed in human 1321N1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 15 mins in presence of IBMX by chromatography F 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 15967-15990 [PMID:36394994]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Inhibition of Serotonin (5-Hydroxytryptamine) 5-HT1A at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_271110) B 5.4 pKi 4000 nM Ki Data for DCP probe PPTN
ChEMBL Inhibition of Serotonin (5-Hydroxytryptamine) 5-HT1A at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_271110) B 5.15 pIC50 7010 nM IC50 Data for DCP probe PPTN
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
SST4 receptor/Somatostatin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1853] [GtoPdb: 358] [UniProtKB: P31391]
ChEMBL Somatostatin sst4 Eurofins-Panlabs radioligand binding assay B 5.28 pIC50 5300 nM IC50 Data for DCP probe PPTN
Vesicular monoamine transporter 2/Synaptic vesicular amine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1893] [GtoPdb: 1012] [UniProtKB: Q05940]
ChEMBL Transporter, Monoamine Eurofins-Panlabs radioligand binding assay B 5.51 pKi 3090 nM Ki Data for DCP probe PPTN
ChEMBL Transporter, Monoamine Eurofins-Panlabs radioligand binding assay B 5.43 pIC50 3720 nM IC50 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 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]
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