PF-3644022 [Ligand Id: 8045] activity data from GtoPdb and ChEMBL

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: CHEMBL1231206
There should be some charts here, you may need to enable JavaScript!
  • MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
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
ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342]
ChEMBL Inhibition of human BSEP expressed in recombinant baculovirus infected insect Sf9 cell membrane vesicles assessed as [3H]-taurocholate transport preincubated for 5 mins followed by ATP or AMP addition measured after 5 mins by scintillation counting method B 5.15 pIC50 7000 nM IC50 J Med Chem (2016) 59: 3609-3634 [PMID:26502061]
MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
ChEMBL Inhibition of recombinant MK2 (45 to 400 residues) (unknown origin) using fluorescein isothiocyanate-KKKALSRQLSVAA as substrate B 8.3 pKi 5 nM Ki Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
GtoPdb - - 8.52 pKi 3 nM Ki J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
ChEMBL Inhibition of MK2 in human U937 cells assessed as reduction in LPS-stimulated HSP27 phosphorylation at Ser82 preincubated for 1 hr followed by LPS addition measured after 30 mins by Western blot analysis B 6.7 pIC50 201 nM IC50 J Med Chem (2016) 59: 3609-3634 [PMID:26502061]
GtoPdb - - 8.28 pIC50 5.2 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
ChEMBL Binding affinity to recombinant MAPKAP-K2 using KKKALSRQLSVAA as substrate after 4 mins by surface plasmon resonance spectroscopic analysis B 8.3 pIC50 5 nM IC50 J Med Chem (2012) 55: 6700-6715 [PMID:22746295]

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]