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ChEMBL ligand: CHEMBL3754515 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]