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Compound Detail

CHEMBL379331

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COc1ccc(/C=C/C(=O)Nc2sc3c(c2C(N)=O)CCCC3)cc1

Basic Information

ChEMBL ID CHEMBL379331
Phase Preclinical
Structure Type MOL
InChI Key VLLBWVYPRXIQAU-DHZHZOJOSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

356.4
MW (Da)
3.39
ALogP
4
HBA
2
HBD
81.4
PSA (Ų)
0.81
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H20N2O3S
MW 356.45
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.38

Activity Summary

IC50 2 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 6.6 6.6 250.0 1
MV4-11
CHEMBL613835
IC50 5.75 5.75 1800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Receptor-type tyrosine-protein kinase FLT3 IC50 = 250.0 nM 6.6 Inhibition of FLT3 16580199
MV4-11 IC50 = 1800.0 nM 5.75 Antiproliferative activity against human MV4-11 cells 16580199

Literature References

PubMed DOI Target Context # Activities
16580199 10.1016/j.bmcl.2006.03.032 Receptor-type tyrosine-protein kinase FLT3 1
16580199 10.1016/j.bmcl.2006.03.032 MV4-11 1

Data from ChEMBL 36 via Core Engine