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Compound Detail

CHEMBL1775067

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Oc1ccc(NCn2nnc3ccccc32)cc1

Basic Information

ChEMBL ID CHEMBL1775067
Phase Preclinical
Structure Type MOL
InChI Key FGZLHPMNJNFFNE-UHFFFAOYSA-N
5
Targets
6
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

240.3
MW (Da)
2.21
ALogP
5
HBA
2
HBD
63.0
PSA (Ų)
0.69
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H12N4O
MW 240.27
Aromatic Rings 3
Heavy Atoms 18
NP-Likeness -1.68

Activity Summary

IC50 6 meas. best 6.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Ribosomal protein S6 kinase alpha-3
CHEMBL2345
IC50 6.32 6.32 480.0 1
MDA-MB-231
CHEMBL400
IC50 4.83 4.83 14880.0 1
MCF7
CHEMBL387
IC50 4.75 4.75 17980.0 1
GroEL/GroES
CHEMBL4106139
IC50 4.26 4.26 55000.0 1
HCT-116
CHEMBL394
IC50 4.25 4.25 56230.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21488662 10.1021/jm200139j HCT-116 2
21488662 10.1021/jm200139j MCF7 2
21488662 10.1021/jm200139j MDA-MB-231 2
24418775 10.1016/j.bmcl.2013.12.100 GroEL/GroES 2
21488662 10.1021/jm200139j Ribosomal protein S6 kinase alpha-3 2
21488662 10.1021/jm200139j Ephrin type-A receptor 2 1
21488662 10.1021/jm200139j Ribosomal protein S6 kinase beta-1 1
21488662 10.1021/jm200139j Mitogen-activated protein kinase 14 1
21488662 10.1021/jm200139j Mitogen-activated protein kinase 9 1
21488662 10.1021/jm200139j Glycogen synthase kinase-3 alpha 1
21488662 10.1021/jm200139j Mitogen-activated protein kinase 3 1
21488662 10.1021/jm200139j RAC-alpha serine/threonine-protein kinase 1
21488662 10.1021/jm200139j Fibroblast growth factor receptor 1 1
21488662 10.1021/jm200139j Proto-oncogene tyrosine-protein kinase Src 1
21488662 10.1021/jm200139j Epidermal growth factor receptor 1
24418775 10.1016/j.bmcl.2013.12.100 Unchecked 1
21488662 10.1021/jm200139j Platelet-derived growth factor receptor beta 1
21488662 10.1021/jm200139j Platelet-derived growth factor receptor alpha 1
21488662 10.1021/jm200139j Mast/stem cell growth factor receptor Kit 1
21488662 10.1021/jm200139j Vascular endothelial growth factor receptor 2 1

Data from ChEMBL 36 via Core Engine