Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL28324 (KN-62) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 |
---|---|---|---|---|---|---|---|---|
calcium/calmodulin-dependent protein kinase II alpha subunit/CaM kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7] | ||||||||
ChEMBL | Inhibition of human CaMKIIalpha using calmodulin and syntide-2 incubated for 15 mins by ELISA | B | 5.99 | pIC50 | 1030 | nM | IC50 | J Med Chem (2020) 63: 1313-1327 [PMID:31972088] |
calcium/calmodulin-dependent protein kinase II delta subunit/CaM kinase II delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557] | ||||||||
ChEMBL | Inhibition of human recombinant CAMK2delta using tetramethylbenzidine as substrate by spectrophotometry analysis | B | 6.42 | pIC50 | 380 | nM | IC50 | Bioorg Med Chem (2012) 20: 377-400 [PMID:22112539] |
P2X7 purinoceptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3600277] [UniProtKB: Q64F92] | ||||||||
ChEMBL | Inhibition of dog P2X7 receptor | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3164-3167 [PMID:26099538] |
P2X purinoceptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3600276] [UniProtKB: A9QW74] | ||||||||
ChEMBL | Inhibition of guinea pig P2X7 receptor | B | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3164-3167 [PMID:26099538] |
P2X4/P2X purinoceptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2104] [GtoPdb: 481] [UniProtKB: Q99571] | ||||||||
ChEMBL | Antagonist activity against recombinant human P2X purinoceptor 4 (P2X4) | F | 4 | pEC50 | 100000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
P2X7/P2X purinoceptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572] | ||||||||
ChEMBL | Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium bromide uptake after 2 hrs by fluorescence assay | B | 4.02 | pIC50 | 96000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 759-763 [PMID:28126517] |
ChEMBL | Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced fluorescent ethidium accumulation | F | 6.47 | pIC50 | 340 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 954-958 [PMID:19110420] |
ChEMBL | Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced pore formation | F | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem (2009) 17: 4861-4865 [PMID:19540765] |
ChEMBL | Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium bromide uptake after 2 hrs by fluorescence analysis | F | 6.55 | pIC50 | 280 | nM | IC50 | J Med Chem (2012) 55: 3687-3698 [PMID:22400713] |
ChEMBL | Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium ion uptake after 2 hrs | B | 6.6 | pIC50 | 250 | nM | IC50 | Eur J Med Chem (2015) 106: 180-193 [PMID:26547056] |
ChEMBL | Antagonist activity at recombinant human P2X7 receptor assessed as inhibition of BzATP-mediated Yo-Pro uptake measured for 1 hr by FLIPR assay | B | 6.68 | pIC50 | 210 | nM | IC50 | Eur J Med Chem (2013) 70: 811-830 [PMID:24246730] |
ChEMBL | Antagonist activity at human purinergic P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium bromide uptake | F | 6.76 | pIC50 | 175 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 571-575 [PMID:18078749] |
ChEMBL | Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake after 2 hrs by fluorescence assay relative to control | B | 6.8 | pIC50 | 158 | nM | IC50 | Eur J Med Chem (2018) 151: 462-481 [PMID:29649742] |
ChEMBL | Antagonist activity at human P2X7 receptor in expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake | B | 6.8 | pIC50 | 158 | nM | IC50 | Eur J Med Chem (2018) 151: 462-481 [PMID:29649742] |
ChEMBL | Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced accumulation of ethidium+ after 120 mins by fluorescence assay | B | 6.8 | pIC50 | 158 | nM | IC50 | Eur J Med Chem (2013) 70: 811-830 [PMID:24246730] |
ChEMBL | Antagonist activity at P2X7 receptor in human lymphocytes assessed as inhibition of ATP-induced ethidium ion uptake preincubated for 5 mins followed by ATP addition and incubated further 2 mins prior to ethidium addition measured up to 5 mins by flow cytometric analysis | B | 6.8 | pIC50 | 158 | nM | IC50 | Eur J Med Chem (2015) 106: 180-193 [PMID:26547056] |
ChEMBL | Antagonist activity at recombinant human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced intracellular ethidium bromide uptake after 2 hrs by fluorescence assay | B | 6.8 | pIC50 | 158 | nM | IC50 | J Med Chem (2015) 58: 2114-2134 [PMID:25597334] |
ChEMBL | Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preincubated for 30 mins followed by BzATP induction measured after 30 mins by ELISA | B | 6.84 | pIC50 | 143 | nM | IC50 | J Med Chem (2015) 58: 2114-2134 [PMID:25597334] |
ChEMBL | Antagonist activity at P2X7 in LPS/IFN gamma differentiated human THP-1 cells assessed as inhibition of BzATP-induced IL-1beta release preincubated for 30 mins followed by BzATP stimulation for 30 mins by ELISA | B | 6.89 | pIC50 | 130 | nM | IC50 | Eur J Med Chem (2018) 151: 462-481 [PMID:29649742] |
ChEMBL | Antagonist activity at P2X7 receptor expressed in LPS/IFNgamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta production after 4 hrs by ELISA | B | 6.89 | pIC50 | 129 | nM | IC50 | Eur J Med Chem (2015) 106: 180-193 [PMID:26547056] |
ChEMBL | Antagonist activity at human P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced IL8 release pretreated for 30 mins before bzATP challenge measured after 30 mins by ELISA | F | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2012) 55: 3687-3698 [PMID:22400713] |
ChEMBL | Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced fluorescent ethidium accumulation at 10 uM | F | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 6053-6058 [PMID:19800793] |
ChEMBL | Inhibition of human P2X7 receptor | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3164-3167 [PMID:26099538] |
ChEMBL | Antagonist activity at P2X7 receptor (unknown origin) | B | 7.03 | pIC50 | 94.4 | nM | IC50 | Bioorg Med Chem (2014) 22: 54-88 [PMID:24314880] |
ChEMBL | Antagonistic activity against P2X7 receptor measured as the ATP dependent calcium influx in human monocytes | F | 7.29 | pIC50 | 51.1 | nM | IC50 | J Med Chem (2003) 46: 1318-1329 [PMID:12672232] |
ChEMBL | Antagonist activity at human P2X7 receptor | B | 7.29 | pIC50 | 51 | nM | IC50 | J Med Chem (2015) 58: 2114-2134 [PMID:25597334] |
ChEMBL | Antagonistic activity against P2X7 receptor | F | 7.29 | pIC50 | 51 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4047-4050 [PMID:14592505] |
ChEMBL | Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium influx | F | 7.3 | pIC50 | 50.12 | nM | IC50 | J Med Chem (2009) 52: 3123-3141 [PMID:19191585] |
ChEMBL | Inhibitory concentration was evaluated against P2X purinoceptor 7 | B | 7.87 | pIC50 | 13.4 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 681-684 [PMID:10762053] |
ChEMBL | Antagonist activity at P2X7 receptor in human lymphocytes assessed as inhibition of ATP-induced Ba2+ influx | F | 7.9 | pIC50 | 12.59 | nM | IC50 | J Med Chem (2009) 52: 3123-3141 [PMID:19191585] |
ChEMBL | Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preincubated for 30 mins followed by BzATP induction measured after 30 mins by ELISA | B | 7.9 | pIC50 | 12.59 | nM | IC50 | J Med Chem (2015) 58: 2114-2134 [PMID:25597334] |
ChEMBL | Antagonist activity against recombinant human P2X purinoceptor 7 (P2X7) | F | 7.47 | pEC50 | 34 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
P2X7/P2X purinoceptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2496] [GtoPdb: 484] [UniProtKB: Q64663] | ||||||||
ChEMBL | Inhibition of rat P2X7 receptor | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3164-3167 [PMID:26099538] |
Calmodulin-dependent kinase II in Human [GtoPdb: 1554] | ||||||||
GtoPdb | - | - | 6.05 | pIC50 | 900 | nM | IC50 | J Biol Chem (1990) 265: 4315-20 [PMID:2155222] |
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]