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Assay Detail

CHEMBL4006633

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Binding
Inhibition of MELK (unknown origin) containing kinase domain and UBA domain using STK S1 as substrate after 20 mins by HTRF assay
9
Total Activities
9
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

"Addition" and "Subtraction": Selectivity Design for Type II Maternal Embryonic Leucine Zipper Kinase Inhibitors.
Chen X, Giraldes J, Sprague ER, Shakya S, Chen Z, Wang Y, Joud C, Mathieu S, Chen CH, Straub C, Duca J, Hurov K, Yuan Y, Shao W, Touré BB.
J Med Chem (2017) 60 : 2155 -2161
PubMed 28186750 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.17 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4077934 1 9.82
CHEMBL4088246 1 8.96
CHEMBL4071823 1 8.82
CHEMBL4092605 1 8.82
CHEMBL4085799 1 8.06
CHEMBL4066968 1 8.04
CHEMBL4095977 1 7.92
CHEMBL4065944 1 6.92
CHEMBL4093545 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4077934 IC50 = 0.15 nM 9.82
CHEMBL4088246 IC50 = 1.1 nM 8.96
CHEMBL4071823 IC50 = 1.5 nM 8.82
CHEMBL4092605 IC50 = 1.5 nM 8.82
CHEMBL4085799 IC50 = 8.8 nM 8.06
CHEMBL4066968 IC50 = 9.2 nM 8.04
CHEMBL4095977 IC50 = 12.0 nM 7.92
CHEMBL4065944 IC50 = 120.0 nM 6.92
CHEMBL4093545 IC50 = 740.0 nM 6.13