ChEMBL ligand: CHEMBL377219 (A-438079)
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!
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] There should be some charts here, you may need to enable JavaScript!
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762] 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]-A-804598 from human P2X7 receptor expressed in HEK293 cell membrane by in vitro binding assay	B	7.17	pKi	68	nM	Ki	J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
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	5.68	pIC50	2100	nM	IC50	J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
ChEMBL	Antagonist activity at human P2X7 receptor in expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake	B	6.52	pIC50	300	nM	IC50	Eur J Med Chem (2018) 151: 462-481 [PMID:29649742]
GtoPdb	-	-	6.9	pIC50	~125	nM	IC50	Br J Pharmacol (2007) 151: 571-9 [PMID:17471177]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of calcium flux by FLIPR	F	6.9	pIC50	125.89	nM	IC50	J Med Chem (2006) 49: 3659-3666 [PMID:16759108]
ChEMBL	Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake	F	6.9	pIC50	125.89	nM	IC50	J Med Chem (2009) 52: 3123-3141 [PMID:19191585]
ChEMBL	Antagonist activity at human recombinant P2X7 receptor assessed as inhibition of BzATP-induced calcium flux by FLIPR assay	F	6.91	pIC50	123.03	nM	IC50	Bioorg Med Chem Lett (2008) 18: 2089-2092 [PMID:18272366]
ChEMBL	Antagonist activity at human recombinant P2X7 receptor expressed in HEK293 cells assessed as inhibition of benzoylbenzoic ATP-induced calcium production by FLIPR assay	F	6.91	pIC50	123.03	nM	IC50	Bioorg Med Chem Lett (2011) 21: 3297-3300 [PMID:21536435]
P2X7/P2X purinoceptor 7 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5183] [GtoPdb: 484] [UniProtKB: Q9Z1M0]
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	5.54	pIC50	2900	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	6.7	pKi	200	nM	Ki	J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
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	6.04	pIC50	910	nM	IC50	J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
ChEMBL	Antagonist activity at rat P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of calcium flux by FLIPR	F	6.5	pIC50	316.23	nM	IC50	J Med Chem (2006) 49: 3659-3666 [PMID:16759108]
ChEMBL	Activity at rat P2X7 receptor expressed in HEK cells assessed as effect on BzATP-induced ethidium uptake	B	6.5	pIC50	316.23	nM	IC50	J Med Chem (2009) 52: 3123-3141 [PMID:19191585]
ChEMBL	Antagonist activity at rat recombinant P2X7 receptor assessed as inhibition of BzATP-induced calcium flux by FLIPR assay	F	6.51	pIC50	309.03	nM	IC50	Bioorg Med Chem Lett (2008) 18: 2089-2092 [PMID:18272366]
ChEMBL	Antagonist activity at rat recombinant P2X7 receptor expressed in HEK293 cells assessed as inhibition of benzoylbenzoic ATP-induced calcium production by FLIPR assay	F	6.51	pIC50	309.03	nM	IC50	Bioorg Med Chem Lett (2011) 21: 3297-3300 [PMID:21536435]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL	Selectivity interaction (GPCR panel (PDSP screen)) EUB0000308b SIGMAR1	B	6.3	pKi	505.48	nM	Ki	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762]
ChEMBL	Affinity Biochemical interaction (FLIPR-based Ca2+ assay (activated by 30 µM AITC)) EUB0000308b TRPA1	B	7.17	pIC50	67	nM	IC50	Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Affinity On-target Cellular interaction (Electrophysiological assay (inhibition of AITC (allylthiocyanate, 100 µmol/L)-evoked currents in HEK293F cells transiently overexpressing hTRPA1)) EUB0000308b TRPA1	B	7.29	pIC50	51	nM	IC50	Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3

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]