PF06260933 [Ligand Id: 13265] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3754515
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  • misshapen like kinase 1/Misshapen-like kinase 1 in Human [ChEMBL: CHEMBL5518] [GtoPdb: 2103] [UniProtKB: Q8N4C8]
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  • mitogen-activated protein kinase kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase kinase 4 in Human [ChEMBL: CHEMBL6166] [GtoPdb: 2088] [UniProtKB: O95819]
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  • TRAF2 and NCK interacting kinase/TRAF2- and NCK-interacting kinase in Human [ChEMBL: CHEMBL4527] [GtoPdb: 2244] [UniProtKB: Q9UKE5]
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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 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]