PF06260933 [Ligand Id: 13265] 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: CHEMBL3754515
There should be some charts here, you may need to enable JavaScript!
  • misshapen like kinase 1/Misshapen-like kinase 1 in Human [ChEMBL: CHEMBL5518] [GtoPdb: 2103] [UniProtKB: Q8N4C8]
There should be some charts here, you may need to enable JavaScript!
  • mitogen-activated protein kinase kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase kinase 4 in Human [ChEMBL: CHEMBL6166] [GtoPdb: 2088] [UniProtKB: O95819]
There should be some charts here, you may need to enable JavaScript!
  • TRAF2 and NCK interacting kinase/TRAF2- and NCK-interacting kinase in Human [ChEMBL: CHEMBL4527] [GtoPdb: 2244] [UniProtKB: Q9UKE5]
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
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG transfected in HEK293 cells B 5.74 pIC50 1800 nM IC50 ACS Med Chem Lett (2015) 6: 1128-1133 [PMID:26617966]
ChEMBL Inhibition of human ERG expressed in HEK293 cells B 5.74 pIC50 1800 nM IC50 J Med Chem (2018) 61: 3114-3125 [PMID:29570292]
misshapen like kinase 1/Misshapen-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5518] [GtoPdb: 2103] [UniProtKB: Q8N4C8]
ChEMBL Inhibition of MINK (unknown origin) in presence of ATP (Km) B 8.1 pIC50 8 nM IC50 ACS Med Chem Lett (2015) 6: 1128-1133 [PMID:26617966]
GtoPdb - - 8.1 pIC50 8 nM IC50 ACS Med Chem Lett (2015) 6: 1128-33 [PMID:26617966]
mitogen-activated protein kinase kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6166] [GtoPdb: 2088] [UniProtKB: O95819]
ChEMBL Inhibition of human MAP4K4 transfected in 293 MSR cells assessed as inhibition of phosphorylation of traf2 at ser/thr residue by ELISA B 6.8 pIC50 160 nM IC50 ACS Med Chem Lett (2015) 6: 1128-1133 [PMID:26617966]
ChEMBL Inhibition of MAP4K4 in human GripTite 293 MSR cells assessed as reduction in TRAF2 Ser/Thr phosphorylation incubated for 1.5 hrs by ELISA B 6.8 pIC50 160 nM IC50 J Med Chem (2018) 61: 3114-3125 [PMID:29570292]
ChEMBL Inhibition of recombinant human GST-tagged MAP4K4 catalytic domain (1 to 328 residues) expressed in baculovirus expression system pre-incubated for 30 mins before Ser/Thr 07 peptide substrate and 1 mM ATP addition and further incubated for 90 mins by Z'-lyte assay B 6.87 pIC50 134 nM IC50 J Med Chem (2018) 61: 3114-3125 [PMID:29570292]
GtoPdb Inhibition of recombinant human MAP4K4 catalytic domain, determined in a FRET assay - 8.43 pIC50 3.7 nM IC50 ACS Med Chem Lett (2015) 6: 1128-33 [PMID:26617966];
J Med Chem (2018) 61: 3114-3125 [PMID:29570292]
ChEMBL Inhibition of recombinant human MAP4K4 catalytic domain in presence of 10 uM ATP (Km) by FRET assay B 8.43 pIC50 3.7 nM IC50 ACS Med Chem Lett (2015) 6: 1128-1133 [PMID:26617966]
ChEMBL Inhibition of recombinant human GST-tagged MAP4K4 catalytic domain (1 to 328 residues) expressed in baculovirus expression system pre-incubated for 30 mins before Ser/Thr 07 peptide substrate and 10 uM ATP addition and further incubated for 90 mins by Z'-lyte assay B 8.43 pIC50 3.7 nM IC50 J Med Chem (2018) 61: 3114-3125 [PMID:29570292]
TRAF2 and NCK interacting kinase/TRAF2- and NCK-interacting kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4527] [GtoPdb: 2244] [UniProtKB: Q9UKE5]
GtoPdb - - 7.82 pIC50 15 nM IC50 ACS Med Chem Lett (2015) 6: 1128-33 [PMID:26617966]
ChEMBL Inhibition of TNIK (unknown origin) in presence of ATP (Km) B 7.82 pIC50 15 nM IC50 ACS Med Chem Lett (2015) 6: 1128-1133 [PMID:26617966]

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]