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ChEMBL ligand: CHEMBL1615189 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527] | ||||||||
GtoPdb | - | - | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2011) 54: 1789-811 [PMID:21332118] |
ChEMBL | Inhibition of DNA-PK after 30 mins by TR-FRET assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2011) 54: 1789-1811 [PMID:21332118] |
phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9] | ||||||||
ChEMBL | Inhibition of human VPS34 after 30 mins by fluorescence-based immunoassay | B | 7.51 | pKi | 31 | nM | Ki | J Med Chem (2011) 54: 1789-1811 [PMID:21332118] |
GtoPdb | - | - | 7.51 | pKi | 31 | nM | Ki | J Med Chem (2011) 54: 1789-811 [PMID:21332118] |
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336] | ||||||||
GtoPdb | - | - | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2011) 54: 1789-811 [PMID:21332118] |
ChEMBL | Inhibition of human PI3Kalpha expressed in Sf9 cells | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2011) 54: 1789-1811 [PMID:21332118] |
ChEMBL | Inhibition of human PI3Kalpha using PI(4,5)P2 as substrate after 20 mins by alphascreen assay in presence of 20 uM ATP | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2011) 54: 5174-5184 [PMID:21714526] |
ChEMBL | Inhibition of N-terminus polyHis-tagged human recombinant PI3Kalpha expressed in baculovirus infected insect Sf9 cells using phosphoinositol-4,5-bisphosphate as substrate after 1.5 hrs by spectrophotometric analysis | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2011) 54: 4735-4751 [PMID:21612232] |
ChEMBL | Inhibition of PI3Kalpha-mediated Akt phosphorylation at Ser 473 in human U87MG cells | B | 8.2 | pIC50 | 6.3 | nM | IC50 | J Med Chem (2011) 54: 4735-4751 [PMID:21612232] |
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338] | ||||||||
ChEMBL | Inhibition of human PI3Kbeta expressed in Sf9 cells | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2011) 54: 1789-1811 [PMID:21332118] |
GtoPdb | - | - | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2011) 54: 1789-811 [PMID:21332118] |
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329] | ||||||||
GtoPdb | - | - | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2011) 54: 1789-811 [PMID:21332118] |
ChEMBL | Inhibition of human PI3Kdelta expressed in Sf9 cells | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2011) 54: 1789-1811 [PMID:21332118] |
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736] | ||||||||
ChEMBL | Inhibition of human PI3Kgamma expressed in Sf9 cells | B | 8.33 | pKi | 4.7 | nM | Ki | J Med Chem (2011) 54: 1789-1811 [PMID:21332118] |
GtoPdb | - | - | 8.33 | pIC50 | 4.7 | nM | IC50 | J Med Chem (2011) 54: 1789-811 [PMID:21332118] |
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
ChEMBL | Inhibition of AKT phosphorylation at S473 in human U-87MG cells at 5 mM after 2 hrs | B | 8.2 | pIC50 | 6.3 | nM | IC50 | J Med Chem (2011) 54: 1789-1811 [PMID:21332118] |
ChEMBL | Inhibition of PI3K-mediated Akt phosphorylation at Ser 473 in human U87MG cells after 2 hrs by alphascreen assay | B | 8.2 | pIC50 | 6.3 | nM | IC50 | J Med Chem (2011) 54: 5174-5184 [PMID:21714526] |
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] | ||||||||
GtoPdb | - | - | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2011) 54: 1789-811 [PMID:21332118] |
ChEMBL | Inhibition of mTOR assessed as inhibition of 4EBP1 phosphorylation by TR-FRET assay | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2011) 54: 1789-1811 [PMID:21332118] |
ChEMBL | Inhibition of recombinant N-terminal GST-tagged mTOR-mediated 4E-BP1 phosphorylation after 60 mins by TR-FRET assay | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2011) 54: 5174-5184 [PMID:21714526] |
SMO/Smoothened homolog in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6080] [GtoPdb: 239] [UniProtKB: P56726] | ||||||||
ChEMBL | Inhibition of SMO in mouse NIH/3T3 cells assessed as inhibition of SAG-induced hedgehog-mediated luminescence signaling by GRE-luciferase reporter gene assay | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3665-3670 [PMID:26119500] |
ChEMBL data shown on this page come from version 32:
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]