example 15 [WO2015079413] [Ligand Id: 12667] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL509624 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| SYNJ1/Synaptojanin-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523136] [GtoPdb: 1461] [UniProtKB: O43426] | ||||||||
| ChEMBL | Inhibition of C-Myc/DDK-tagged human recombinant SYNJ1 expressed in HEK293T cells assessed as reduction in 5'-phosphatase activity incubated for 8 mins using fluorescently-labeled PI(3,4)P2 probe and Tapp1 PH-domain as detector protein by fluorescence polarization competitive assay | B | 4.8 | pIC50 | <=15900 | nM | IC50 | US-20170042857-A1. Synaptojanin-2 inhibitors for use in the treatment of cancer (null) |
| ChEMBL | Inhibition of C-Myc/DDK-tagged human recombinant SYNJ1 expressed in HEK293T cells assessed as reduction in 5'-phosphatase activity incubated for 8 mins using fluorescently-labeled PI(3,4)P2 probe and Tapp1 PH-domain as detector protein by fluorescence polarization competitive assay | B | 4.8 | pIC50 | <=15900 | nM | IC50 | WO-2015079413-A2. Synaptojanin-2 inhibitors and uses thereof (null) |
| SYNJ2/Synaptojanin-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523129] [GtoPdb: 1462] [UniProtKB: O15056] | ||||||||
| ChEMBL | Inhibition of C-Myc/DDK-tagged human recombinant SYNJ2 expressed in HEK293T cells assessed as reduction in 5'-phosphatase activity incubated for 8 mins using fluorescently-labeled PI(3,4)P2 probe and Tapp1 PH-domain as detector protein by fluorescence polarization competitive assay | B | 6.06 | pIC50 | 874 | nM | IC50 | US-20170042857-A1. Synaptojanin-2 inhibitors for use in the treatment of cancer (null) |
| ChEMBL | Inhibition of C-Myc/DDK-tagged human recombinant SYNJ2 expressed in HEK293T cells assessed as reduction in 5'-phosphatase activity incubated for 8 mins using fluorescently-labeled PI(3,4)P2 probe and Tapp1 PH-domain as detector protein by fluorescence polarization competitive assay | B | 6.06 | pIC50 | 874 | nM | IC50 | WO-2015079413-A2. Synaptojanin-2 inhibitors and uses thereof (null) |
| ChEMBL | Inhibition of recombinant full length C-Myc/DDK-tagged human SYNJ2 expressed in HEK293T cells using PI(3,4,5)P3 as substrate incubated for 8 mins assessed as hydrolysis of PI(3,4,5)P3 to PI(3,4)P2 by fluorescence polarization assay | B | 6.06 | pIC50 | 874 | nM | IC50 | US-20170165285-A1. Methods of preventing tumor metastasis, treating and prognosing cancer and identifying agents which are putative metastasis inhibitors (null) |
| GtoPdb | Inhibition of 5'-phosphatase activity in HEK293T cells expressing hSYNJ2 by fluorescence polarization competitive assay. | - | 6.06 | pIC50 | 874 | nM | IC50 | WO2015079413A2. Synaptojanin-2 inhibitors and uses thereof (2015) |
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]
