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Compound Detail

CHEMBL2385596

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CN1CCN(c2ccc(-c3cnc4c(-c5ccnc6ccccc56)cnn4c3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL2385596
Phase Preclinical
Structure Type MOL
InChI Key XBGWAKUQSRNWMA-UHFFFAOYSA-N
7
Targets
7
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

420.5
MW (Da)
4.36
ALogP
6
HBA
0
HBD
49.6
PSA (Ų)
0.43
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 C26H24N6
MW 420.52
Aromatic Rings 5
Heavy Atoms 32
NP-Likeness -1.29

Activity Summary

IC50 7 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
TGF-beta receptor type-2
CHEMBL4267
IC50 7.82 7.82 15.0 1
Bone morphogenetic protein 4
CHEMBL2384894
IC50 7.6 7.6 25.2 1
TGF-beta receptor type-1
CHEMBL4439
IC50 7.12 7.12 75.0 1
Activin receptor type-1B
CHEMBL5310
IC50 6.74 6.74 183.0 1
5'-AMP-activated protein kinase subunit beta-1
CHEMBL3847
IC50 6.02 6.02 960.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 5.82 5.82 1520.0 1
Bone morphogenetic protein receptor type-2
CHEMBL5467
IC50 5.63 5.63 2360.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23639540 10.1016/j.bmcl.2013.03.113 Bone morphogenetic protein receptor type-1B 1
23639540 10.1016/j.bmcl.2013.03.113 Bone morphogenetic protein receptor type-1A 1
23639540 10.1016/j.bmcl.2013.03.113 Activin receptor type-1 1
23639540 10.1016/j.bmcl.2013.03.113 Activin receptor type-1-like 1
23639540 10.1016/j.bmcl.2013.03.113 Bone morphogenetic protein receptor type-2 1
23639540 10.1016/j.bmcl.2013.03.113 Vascular endothelial growth factor receptor 2 1
23639540 10.1016/j.bmcl.2013.03.113 5'-AMP-activated protein kinase subunit beta-1 1
23639540 10.1016/j.bmcl.2013.03.113 Activin receptor type-1B 1
23639540 10.1016/j.bmcl.2013.03.113 TGF-beta receptor type-1 1
23639540 10.1016/j.bmcl.2013.03.113 Bone morphogenetic protein 4 1
23639540 10.1016/j.bmcl.2013.03.113 TGF-beta receptor type-2 1

Data from ChEMBL 36 via Core Engine