Gene and Protein Information
Species	TM	AA	Chromosomal Location	Gene Symbol	Gene Name	Reference
Human	-	800	2q24.2	ZAK	ZAK sterile alpha motif and leucine zipper containing kinase AZK
Mouse	-	802	2 C3	Map3k20	mitogen-activated protein kinase kinase kinase 20
Rat	-	802	3q22	Map3k20	mitogen-activated protein kinase kinase kinase 20

Previous and Unofficial Names

Zak | HCCS-4 | mitogen-activated protein kinase kinase kinase MLT | mixed lineage kinase 7 | MLK7 | MLK-like mitogen-activated protein triple kinase | human cervical cancer suppressor gene 4 protein | MLK-related kinase | sterile alpha motif and leucine zipper containing kinase AZK

Database Links
BRENDA	2.7.11.25
ChEMBL Target	CHEMBL3886 (Hs)
Ensembl Gene	ENSG00000091436 (Hs), ENSMUSG00000004085 (Mm), ENSRNOG00000001515 (Rn)
Entrez Gene	51776 (Hs), 65964 (Mm), 311743 (Rn)
Human Protein Atlas	ENSG00000091436 (Hs)
KEGG Enzyme	2.7.11.25
KEGG Gene	hsa:51776 (Hs), mmu:65964 (Mm), rno:311743 (Rn)
OMIM	609479 (Hs)
RefSeq Nucleotide	NM_016653 (Hs), NM_023057 (Mm), XM_002729174 (Rn)
RefSeq Protein	NP_057737 (Hs), NP_075544 (Mm), XP_001059755 (Rn)
UniProtKB	Q9NYL2 (Hs), Q9ESL4 (Mm)
Wikipedia	ZAK (Hs)

Enzyme Reaction
EC Number: 2.7.11.25

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols	View all chemical structures	Click column headers to sort
Ligand Sp. Action Value Parameter Reference ZAK inhibitor 6p Hs Inhibition 8.1 pKd 5 ⤷ pKd 8.1 (Kd 8x10-9 M) [5] Description: Binding affinity determined using an active site-dependent competition binding assay. ZAK inhibitor 6p Hs Inhibition 8.4 pIC50 5 ⤷ pIC50 8.4 (IC50 4x10-9 M) [5] Description: Inhibition of enzymatic activity determined in a ADP-GloTM assay. compound 15b [PMID: 16539403] Hs Inhibition 6.2 pIC50 3 ⤷ pIC50 6.2 (IC50 7.08x10-7 M) [3]

DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform. http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan Reference: 2,4
Key to terms and symbols		Click column headers to sort
Target used in screen: ZAK
Ligand Sp. Type Action Value Parameter AST-487 Hs Inhibitor Inhibition 8.6 pKd sorafenib Hs Inhibitor Inhibition 8.2 pKd motesanib Hs Inhibitor Inhibition 8.1 pKd nilotinib Hs Inhibitor Inhibition 8.0 pKd PLX-4720 Hs Inhibitor Inhibition 7.4 pKd dasatinib Hs Inhibitor Inhibition 7.3 pKd foretinib Hs Inhibitor Inhibition 7.3 pKd CHIR-265 Hs Inhibitor Inhibition 7.2 pKd bosutinib Hs Inhibitor Inhibition 7.1 pKd PD-173955 Hs Inhibitor Inhibition 6.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service. A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform. http://www.millipore.com/techpublications/tech1/pf3036 http://www.reactionbiology.com/webapps/main/pages/kinase.aspx Reference: ...1
Key to terms and symbols		Click column headers to sort
Target used in screen: nd/ZAK(MLTK)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM dasatinib Hs Inhibitor Inhibition 8.6 dorsomorphin Hs Inhibitor Inhibition 11.7 TWS119 Hs Inhibitor Inhibition 13.9 sorafenib Hs Inhibitor Inhibition 16.7 nilotinib Hs Inhibitor Inhibition 17.8 Flt-3 inhibitor III Hs Inhibitor Inhibition 25.9 Flt-3 inhibitor II Hs Inhibitor Inhibition 34.3 PDGF receptor tyrosine kinase inhibitor IV Hs Inhibitor Inhibition 44.7 Cdk1/2 inhibitor III Hs Inhibitor Inhibition 49.1 PKR inhibitor Hs Inhibitor Inhibition 52.8
Displaying the top 10 most potent ligands  View all ligands in screen »