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Compound Detail

CHEMBL513330

GW781673X
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Clc1ccc(CNc2nccc(-c3cnn4ncccc34)n2)cc1

Basic Information

ChEMBL ID CHEMBL513330
Name GW781673X
Phase Preclinical
Structure Type MOL
InChI Key NEWXQDRWGLAOAY-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

336.8
MW (Da)
3.45
ALogP
6
HBA
1
HBD
68.0
PSA (Ų)
0.62
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H13ClN6
MW 336.79
Aromatic Rings 4
Heavy Atoms 24
NP-Likeness -1.55

Activity Summary

IC50 3 meas. best 6.0
EC50 1 meas. best 5.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2
CHEMBL301
IC50 6.0 6.0 1000.0 1
Cyclin-dependent kinase 4
CHEMBL331
IC50 6.0 6.0 1000.0 1
Trypanosoma brucei brucei
CHEMBL612851
EC50 5.2 5.2 6309.6 1
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL1961873 Tyrosine-protein kinase ABL1 14
- 10.6019/CHEMBL1961873 Epidermal growth factor receptor 10
- 10.6019/CHEMBL1961873 Mast/stem cell growth factor receptor Kit 8
- 10.6019/CHEMBL1961873 Platelet-derived growth factor receptor alpha 8
- 10.6019/CHEMBL1961873 Proto-oncogene tyrosine-protein kinase receptor Ret 6
- 10.6019/CHEMBL1961873 Cyclin-dependent kinase 2 4
- 10.6019/CHEMBL1961873 Serine/threonine-protein kinase B-raf 4
- 10.6019/CHEMBL1961873 Leucine-rich repeat serine/threonine-protein kinase 2 4
- 10.6019/CHEMBL1961873 Tyrosine-protein kinase Lyn 4
- 10.6019/CHEMBL1961873 Protein kinase C beta type 4
- 10.6019/CHEMBL1961873 Receptor-type tyrosine-protein kinase FLT3 4
31846577 10.1021/acs.jmedchem.9b01741 ADMET 3
- 10.6019/CHEMBL1961873 Ribosomal protein S6 kinase alpha-4 2
- 10.6019/CHEMBL1961873 Ribosomal protein S6 kinase beta-1 2
- 10.6019/CHEMBL1961873 Serine/threonine-protein kinase MRCK beta 2
- 10.6019/CHEMBL1961873 cAMP-dependent protein kinase catalytic subunit alpha 2
- 10.6019/CHEMBL1961873 G protein-coupled receptor kinase 6 2
- 10.6019/CHEMBL1961873 RAC-gamma serine/threonine-protein kinase 2
- 10.6019/CHEMBL1961873 Serine/threonine-protein kinase D3 2
- 10.6019/CHEMBL1961873 Serine/threonine-protein kinase D2 2

Data from ChEMBL 36 via Core Engine