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

CHEMBL3646210

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
Cc1cccc(NC(=O)Nc2ccc(-c3csc4c(-c5cnn(C[C@H](C)O)c5)cnc(N)c34)cc2)c1

Basic Information

ChEMBL ID CHEMBL3646210
Phase Preclinical
Structure Type MOL
InChI Key VKBFHTIUXUCYRQ-KRWDZBQOSA-N
8
Targets
11
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

498.6
MW (Da)
5.74
ALogP
7
HBA
4
HBD
118.1
PSA (Ų)
0.24
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H26N6O2S
MW 498.61
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness -1.44

Activity Summary

IC50 11 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 8.8 8.8 1.6 1
Vascular endothelial growth factor receptor 1
CHEMBL1868
IC50 8.69 8.69 2.0 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 8.66 8.66 2.2 2
Macrophage colony-stimulating factor 1 receptor
CHEMBL1844
IC50 8.25 8.25 5.6 2
Aurora kinase B
CHEMBL2185
IC50 7.95 7.95 11.2 1
Mast/stem cell growth factor receptor Kit
CHEMBL1936
IC50 7.57 7.57 27.1 2
Serine/threonine-protein kinase Nek2
CHEMBL3835
IC50 7.3 7.3 50.0 1
Aurora kinase A
CHEMBL4722
IC50 6.61 6.61 248.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Vascular endothelial growth factor receptor 2 IC50 = 1.6 nM 8.8 Homogenous Time-Resolved Fluorescence Assay (HTRF): To determine the activity of... -
Vascular endothelial growth factor receptor 1 IC50 = 2.04 nM 8.69 Homogenous Time-Resolved Fluorescence Assay (HTRF): To determine the activity of... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 2.18 nM 8.66 Homogenous Time-Resolved Fluorescence Assay (HTRF): To determine the activity of... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 2.18 nM 8.66 Homogenous Time-Resolved Fluorescence Assay (HTRF): To determine the activity of... -
Macrophage colony-stimulating factor 1 receptor IC50 = 5.62 nM 8.25 Homogenous Time-Resolved Fluorescence Assay (HTRF): To determine the activity of... -
Macrophage colony-stimulating factor 1 receptor IC50 = 5.62 nM 8.25 Homogenous Time-Resolved Fluorescence Assay (HTRF): To determine the activity of... -
Aurora kinase B IC50 = 11.21 nM 7.95 Enzyme Inhibtion Assay: To determine Aurora B activity of representative compoun... -
Mast/stem cell growth factor receptor Kit IC50 = 27.11 nM 7.57 Homogenous Time-Resolved Fluorescence Assay (HTRF): To determine the activity of... -
Mast/stem cell growth factor receptor Kit IC50 = 27.11 nM 7.57 Homogenous Time-Resolved Fluorescence Assay (HTRF): To determine the activity of... -
Serine/threonine-protein kinase Nek2 IC50 = 50.0 nM 7.3 Inhibition of NEK2 (unknown origin) 30108900
Aurora kinase A IC50 = 248.31 nM 6.61 Enzyme Inhibtion Assay: To determine Aurora A and C activity of representative c... -

Literature References

PubMed DOI Target Context # Activities
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek4 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek2 1

Data from ChEMBL 36 via Core Engine