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Compound Detail

CHEMBL1761583

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Cn1cc(-c2ccc3cnc(Nc4ccc(-n5cnc(N6CCOCC6)n5)cc4)nc3c2-c2ccccc2)cn1

Basic Information

ChEMBL ID CHEMBL1761583
Phase Preclinical
Structure Type MOL
InChI Key CEANXNAMUUCBQK-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

529.6
MW (Da)
4.86
ALogP
10
HBA
1
HBD
98.8
PSA (Ų)
0.33
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 C30H27N9O
MW 529.61
Aromatic Rings 6
Heavy Atoms 40
NP-Likeness -1.56

Activity Summary

IC50 2 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 10
CHEMBL2637
IC50 8.0 8.0 10.0 1
Transcription factor Jun
CHEMBL4977
IC50 7.4 7.4 40.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 10 IC50 = 10.0 nM 8.0 Inhibition of JNK3 by HRTF 21316221
Transcription factor Jun IC50 = 40.0 nM 7.4 Inhibition of c-Jun 21316221

Literature References

PubMed DOI Target Context # Activities
21316221 10.1016/j.bmcl.2011.01.079 Mitogen-activated protein kinase 10 1
21316221 10.1016/j.bmcl.2011.01.079 Transcription factor Jun 1
21316221 10.1016/j.bmcl.2011.01.079 Plasma 1
21316221 10.1016/j.bmcl.2011.01.079 Brain 1

Data from ChEMBL 36 via Core Engine