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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 |
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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]