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Assay Detail

CHEMBL4620149

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Binding
Inhibition of LMTK3 (unknown origin)
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

Serine/threonine-protein kinase LMTK3 (CHEMBL4523432)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of cyclic guanidine-linked sulfonamides as inhibitors of LMTK3 kinase.
Ortiz MA, Michaels H, Molina B, Toenjes S, Davis J, Marconi GD, Hecht D, Gustafson JL, Piedrafita FJ, Nefzi A.
Bioorg Med Chem Lett (2020) 30 : 127108 -127108
PubMed 32192797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.14 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4637017 1 6.68
CHEMBL4647760 1 6.65
CHEMBL4635320 1 6.51
CHEMBL4649625 1 6.50
CHEMBL4638119 1 6.18
CHEMBL4649046 1 5.79
CHEMBL575448 BMS-754807 2.0 1 5.50
CHEMBL1983268 ENTRECTINIB 4.0 1 5.33
CHEMBL388978 STAUROSPORINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4637017 IC50 = 210.0 nM 6.68
CHEMBL4647760 IC50 = 226.0 nM 6.65
CHEMBL4635320 IC50 = 308.0 nM 6.51
CHEMBL4649625 IC50 = 318.0 nM 6.50
CHEMBL4638119 IC50 = 654.0 nM 6.18
CHEMBL4649046 IC50 = 1609.0 nM 5.79
CHEMBL575448 BMS-754807 IC50 = 3161.0 nM 5.50
CHEMBL1983268 ENTRECTINIB IC50 = 4653.0 nM 5.33
CHEMBL388978 STAUROSPORINE IC50 = 0.0024 nM -