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ChEMBL ligand: CHEMBL2386715 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]