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Compound Detail

CHEMBL3646211

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COc1ccc(NC(=O)Nc2ccc(-c3csc4c(-c5cnn(C[C@H](O)CO)c5)cnc(N)c34)cc2)cc1

Basic Information

ChEMBL ID CHEMBL3646211
Phase Preclinical
Structure Type MOL
InChI Key BRTHUECZMVKNMQ-FQEVSTJZSA-N
7
Targets
10
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

530.6
MW (Da)
4.41
ALogP
9
HBA
5
HBD
147.6
PSA (Ų)
0.20
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H26N6O4S
MW 530.61
Aromatic Rings 5
Heavy Atoms 38
NP-Likeness -1.02

Activity Summary

IC50 10 meas. best 8.91

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 8.91 8.91 1.2 2
Macrophage colony-stimulating factor 1 receptor
CHEMBL1844
IC50 8.87 8.87 1.3 2
Vascular endothelial growth factor receptor 1
CHEMBL1868
IC50 8.84 8.84 1.4 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 8.74 8.74 1.8 1
Mast/stem cell growth factor receptor Kit
CHEMBL1936
IC50 7.9 7.9 12.6 2
Aurora kinase B
CHEMBL2185
IC50 7.54 7.54 28.9 1
Aurora kinase A
CHEMBL4722
IC50 6.24 6.24 570.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Receptor-type tyrosine-protein kinase FLT3 IC50 = 1.22 nM 8.91 Homogenous Time-Resolved Fluorescence Assay (HTRF): To determine the activity of... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 1.22 nM 8.91 Homogenous Time-Resolved Fluorescence Assay (HTRF): To determine the activity of... -
Macrophage colony-stimulating factor 1 receptor IC50 = 1.34 nM 8.87 Homogenous Time-Resolved Fluorescence Assay (HTRF): To determine the activity of... -
Macrophage colony-stimulating factor 1 receptor IC50 = 1.34 nM 8.87 Homogenous Time-Resolved Fluorescence Assay (HTRF): To determine the activity of... -
Vascular endothelial growth factor receptor 1 IC50 = 1.45 nM 8.84 Homogenous Time-Resolved Fluorescence Assay (HTRF): To determine the activity of... -
Vascular endothelial growth factor receptor 2 IC50 = 1.83 nM 8.74 Homogenous Time-Resolved Fluorescence Assay (HTRF): To determine the activity of... -
Mast/stem cell growth factor receptor Kit IC50 = 12.58 nM 7.9 Homogenous Time-Resolved Fluorescence Assay (HTRF): To determine the activity of... -
Mast/stem cell growth factor receptor Kit IC50 = 12.58 nM 7.9 Homogenous Time-Resolved Fluorescence Assay (HTRF): To determine the activity of... -
Aurora kinase B IC50 = 28.93 nM 7.54 Enzyme Inhibtion Assay: To determine Aurora B activity of representative compoun... -
Aurora kinase A IC50 = 570.14 nM 6.24 Enzyme Inhibtion Assay: To determine Aurora A and C activity of representative c... -

Data from ChEMBL 36 via Core Engine