ChEMBL ligand: CHEMBL2338352
P2X7/P2X purinoceptor 7 in Human [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572] P2X7/P2X purinoceptor 7 in Mouse [ChEMBL: CHEMBL5183] [GtoPdb: 484] [UniProtKB: Q9Z1M0] P2X7/P2X purinoceptor 7 in Rat [ChEMBL: CHEMBL2496] [GtoPdb: 484] [UniProtKB: Q64663] There should be some charts here, you may need to enable JavaScript!
SERT/Serotonin transporter in Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] There should be some charts here, you may need to enable JavaScript!

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 THP-1 cells assessed as inhibition of ATP-induced IL-1beta secretion pretreated with LPS for 3 hrs followed by incubation with compound for 40 mins followed by treatment with ATP for 1 hr by ELISA	B	7.52	pIC50	<30	nM	IC50	J Med Chem (2023) 66: 11365-11389 [PMID:37582195]
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 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]
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]