Il-94 [Ligand Id: 8132] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2386715
  • p21 (RAC1) activated kinase 1/Serine/threonine-protein kinase PAK 1 in Human [ChEMBL: CHEMBL4600] [GtoPdb: 2133] [UniProtKB: Q13153]
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  • p21 (RAC1) activated kinase 2/Serine/threonine-protein kinase PAK 2 in Human [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177]
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  • p21 (RAC1) activated kinase 3/Serine/threonine-protein kinase PAK 3 in Human [ChEMBL: CHEMBL2999] [GtoPdb: 2135] [UniProtKB: O75914]
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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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]