JNJ-47965567 [Ligand Id: 7538] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2338352
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
P2X7/P2X purinoceptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572]
ChEMBL Displacement of [3H]-A804598 from human recombinant P2X7 receptor expressed in human 1321N1 cell membranes after 1 hr by fluorescence assay B 7.9 pKi 12.59 nM Ki ACS Med Chem Lett (2013) 4: 419-422 [PMID:24900687]
GtoPdb - - 7.9 pKi 12.6 nM Ki Br J Pharmacol (2013) 170: 624-40 [PMID:23889535]
ChEMBL Antagonist activity at P2X7 receptor in human whole blood assessed as inhibition of BzATP-induced IL1beta release incubated 30 mins prior to BzATP-challenge measured after 1.5 hrs by ELISA B 6.7 pIC50 199.53 nM IC50 ACS Med Chem Lett (2013) 4: 419-422 [PMID:24900687]
ChEMBL Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis B 7.46 pIC50 35 nM IC50 J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
ChEMBL Antagonist activity at P2X7 receptor in human PBMC assessed as inhibition of BzATP-induced IL1beta release incubated 30 mins prior to BzATP-challenge measured after 1.5 hrs by ELISA B 7.6 pIC50 25.12 nM IC50 ACS Med Chem Lett (2013) 4: 419-422 [PMID:24900687]
ChEMBL Antagonist activity at human P2X7R expressed in HEK293 cells assessed as reduction in YO-PRO-1 iodide dye uptake preincubated for 30 mins followed by YO-PRO-1 iodide addition and measured after 2 hrs by fluorescence plate reader analysis B 7.8 pIC50 15.85 nM IC50 Eur J Med Chem (2021) 226: 113838-113838 [PMID:34571173]
ChEMBL Antagonist activity at human recombinant P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of BzATP-induced Ca2+ flux after 30 mins by FLIPR assay B 8.3 pIC50 5.01 nM IC50 ACS Med Chem Lett (2013) 4: 419-422 [PMID:24900687]
GtoPdb Measuring antagonism of BzATP induced calcium flux. - 8.3 pIC50 5 nM IC50 Br J Pharmacol (2013) 170: 624-40 [PMID:23889535]
P2X7/P2X purinoceptor 7 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5183] [GtoPdb: 484] [UniProtKB: Q9Z1M0]
ChEMBL Antagonist activity at mouse P2X7 receptor assessed as inhibition of ATP-induced Ca2+ flux by FLIPR assay B 7.5 pIC50 31.62 nM IC50 ACS Med Chem Lett (2013) 4: 419-422 [PMID:24900687]
ChEMBL Antagonist activity at mouse P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis B 9.19 pIC50 0.65 nM IC50 J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
P2X7/P2X purinoceptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2496] [GtoPdb: 484] [UniProtKB: Q64663]
ChEMBL Displacement of [3H]-A-804598 from rat P2X7 receptor expressed in HEK293 cell membrane by in vitro binding assay B 7.01 pKi 98 nM Ki J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
ChEMBL Antagonist activity at rat P2X7 receptor by radioligand binding assay B 8.7 pKi 2 nM Ki ACS Med Chem Lett (2013) 4: 419-422 [PMID:24900687]
ChEMBL Antagonist activity at rat P2X7 receptor assessed as inhibition of ATP-induced Ca2+ flux by FLIPR assay B 7.2 pIC50 63.1 nM IC50 ACS Med Chem Lett (2013) 4: 419-422 [PMID:24900687]
ChEMBL Antagonist activity at rat P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis B 8.33 pIC50 4.7 nM IC50 J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Displacement of [3H]-Citalopram from SERT in rat brain after 60 mins by scintillation counting analysis B 5.5 pKi 3162.28 nM Ki ACS Med Chem Lett (2013) 4: 419-422 [PMID:24900687]

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]