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Compound Detail

CHEMBL1761581

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Cn1cc(-c2ccc3cnc(Nc4ccc(-n5cnc(N6CCOCC6)n5)cc4)nc3c2C2CC2)cn1

Basic Information

ChEMBL ID CHEMBL1761581
Phase Preclinical
Structure Type MOL
InChI Key SVIZILSXAQTEQC-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

493.6
MW (Da)
4.07
ALogP
10
HBA
1
HBD
98.8
PSA (Ų)
0.38
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H27N9O
MW 493.58
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -1.57

Activity Summary

IC50 2 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 10
CHEMBL2637
IC50 7.7 7.7 20.0 1
Transcription factor Jun
CHEMBL4977
IC50 6.89 6.89 130.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 10 IC50 = 20.0 nM 7.7 Inhibition of JNK3 by HRTF 21316221
Transcription factor Jun IC50 = 130.0 nM 6.89 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