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: CHEMBL2386715 |
---|
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 |
---|---|---|---|---|---|---|---|---|
p21 (RAC1) activated kinase 1/Serine/threonine-protein kinase PAK 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4600] [GtoPdb: 2133] [UniProtKB: Q13153] | ||||||||
GtoPdb | - | - | 7.43 | pKi | 36.8 | nM | Ki | ACS Med Chem Lett (2013) 4: 431-2 [PMID:24900689] |
ChEMBL | Inhibition of human recombinant GST-tagged PAK1 kinase domain-mediated 5FAM-RRRLSFAEPG phosphorylation expressed in Sf9 cells preincubated for 10 mins prior to substrate addition measured after 30 mins by microfluidic mobility shift assay | B | 7.43 | pKi | 36.8 | nM | Ki | ACS Med Chem Lett (2013) 4: 431-432 [PMID:24900689] |
ChEMBL | Inhibition of PAK1-mediated MEK1 phosphorylation at Ser298 in human EBC1 cells after 2 hrs by HTRF assay | B | 7.19 | pIC50 | 64.1 | nM | IC50 | ACS Med Chem Lett (2013) 4: 431-432 [PMID:24900689] |
p21 (RAC1) activated kinase 2/Serine/threonine-protein kinase PAK 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177] | ||||||||
GtoPdb | - | - | 7.19 | pIC50 | 64.1 | nM | IC50 | ACS Med Chem Lett (2013) 4: 431-2 [PMID:24900689] |
ChEMBL | Inhibition of PAK2-mediated MEK1 phosphorylation at Ser298 in human EBC1 cells after 2 hrs by HTRF assay | B | 7.19 | pIC50 | 64.1 | nM | IC50 | ACS Med Chem Lett (2013) 4: 431-432 [PMID:24900689] |
p21 (RAC1) activated kinase 3/Serine/threonine-protein kinase PAK 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2999] [GtoPdb: 2135] [UniProtKB: O75914] | ||||||||
ChEMBL | Inhibition of PAK3-mediated MEK1 phosphorylation at Ser298 in human EBC1 cells after 2 hrs by HTRF assay | B | 7.19 | pIC50 | 64.1 | nM | IC50 | ACS Med Chem Lett (2013) 4: 431-432 [PMID:24900689] |
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]