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Assay Detail

CHEMBL4018869

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Binding
Binding affinity to recombinant human N-terminal His6-tagged Myt1 kinase domain (75 to 361 residues) by isothermal titration calorimetry
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

Publication

Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors.
Zhu JY, Cuellar RA, Berndt N, Lee HE, Olesen SH, Martin MP, Jensen JT, Georg GI, Schönbrunn E.
J Med Chem (2017) 60 : 7863 -7875
PubMed 28792760 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 6.29 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5416410 DASATINIB 4.0 1 6.82
CHEMBL49120 PD-0166285 1.0 1 6.61
CHEMBL288441 BOSUTINIB 4.0 1 6.57
CHEMBL1976040 ADAVOSERTIB 2.0 1 6.49
CHEMBL4067978 1 6.35
CHEMBL564829 MILCICLIB 2.0 1 6.00
CHEMBL607707 PELITINIB 2.0 1 5.96
CHEMBL217092 SARACATINIB 3.0 1 5.55
CHEMBL4289017 PF-03814735 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5416410 DASATINIB Kd = 150.0 nM 6.82
CHEMBL49120 PD-0166285 Kd = 247.0 nM 6.61
CHEMBL288441 BOSUTINIB Kd = 270.0 nM 6.57
CHEMBL1976040 ADAVOSERTIB Kd = 324.0 nM 6.49
CHEMBL4067978 Kd = 444.0 nM 6.35
CHEMBL564829 MILCICLIB Kd = 990.0 nM 6.00
CHEMBL607707 PELITINIB Kd = 1105.0 nM 5.96
CHEMBL217092 SARACATINIB Kd = 2817.0 nM 5.55
CHEMBL4289017 PF-03814735 Kd - -