Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5540233

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Toxicity
Inhibition of FLT3 (unknown origin)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Darovasertib (NVP-LXS196), a Pan-PKC Inhibitor for the Treatment of Metastatic Uveal Melanoma.
Visser M, Papillon JPN, Luzzio M, LaMarche MJ, Fan J, Michael W, Wang D, Zhang A, Straub C, Mathieu S, Kato M, Palermo M, Chen C, Ramsey T, Joud C, Barrett R, Vattay A, Guo R, Bric A, Chung F, Liang G, Romanowski MJ, Lam J, Thohan S, Atassi F, Wylie A, Cooke VG.
J Med Chem (2024) 67 : 1447 -1459
PubMed 38198520 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.43 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5566264 1 7.52
CHEMBL3957715 1 7.51
CHEMBL3982497 1 7.48
CHEMBL3943147 1 7.02
CHEMBL3957149 1 6.85
CHEMBL5573642 1 6.64
CHEMBL3966643 1 6.64
CHEMBL5571382 1 5.52
CHEMBL3924825 1 5.39
CHEMBL3915489 1 5.07
CHEMBL3890986 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5566264 IC50 = 30.0 nM 7.52
CHEMBL3957715 IC50 = 31.0 nM 7.51
CHEMBL3982497 IC50 = 33.0 nM 7.48
CHEMBL3943147 IC50 = 95.0 nM 7.02
CHEMBL3957149 IC50 = 140.0 nM 6.85
CHEMBL5573642 IC50 = 230.0 nM 6.64
CHEMBL3966643 IC50 = 230.0 nM 6.64
CHEMBL5571382 IC50 = 3000.0 nM 5.52
CHEMBL3924825 IC50 = 4100.0 nM 5.39
CHEMBL3915489 IC50 = 8460.0 nM 5.07
CHEMBL3890986 IC50 = 8700.0 nM 5.06