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Compound Detail

CHEMBL1807722

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CN1CCN(c2ccc3[nH]c(-c4n[nH]c5ncc(-c6cncc(CN7CCCC7)c6)cc45)nc3c2)CC1

Basic Information

ChEMBL ID CHEMBL1807722
Phase Preclinical
Structure Type MOL
InChI Key ZWWIKQPGGNSGJY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

493.6
MW (Da)
3.91
ALogP
7
HBA
2
HBD
92.9
PSA (Ų)
0.38
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H31N9
MW 493.62
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -1.44

Activity Summary

IC50 1 meas. best 6.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
IC50 6.32 6.32 475.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Proto-oncogene tyrosine-protein kinase receptor Ret IC50 = 475.0 nM 6.32 Inhibition of RET kinase 21724393

Literature References

PubMed DOI Target Context # Activities
21724393 10.1016/j.bmcl.2011.06.003 Proto-oncogene tyrosine-protein kinase receptor Ret 1

Data from ChEMBL 36 via Core Engine