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Assay Detail

CHEMBL4838728

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Binding
Inhibition of N-terminal GST-tagged MELK (1 to 493 residues) (unknown origin) expressed in Escherichia coli
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Maternal embryonic leucine zipper kinase (CHEMBL4578)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

UNC5293, a potent, orally available and highly MERTK-selective inhibitor.
Zheng H, Zhao J, Li B, Zhang W, Stashko MA, Minson KA, Huey MG, Zhou Y, Earp HS, Kireev D, Graham DK, DeRyckere D, Frye SV, Wang X.
Eur J Med Chem (2021) 220 : 113534 -113534
PubMed 34038857 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.83 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4283353 1 8.64
CHEMBL4877347 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4283353 IC50 = 2.3 nM 8.64
CHEMBL4877347 IC50 = 95.7 nM 7.02