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Compound Detail

CHEMBL3286829

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C[C@H]1Oc2cc(cnc2N)-c2c(C3CC3)nn(C)c2CN(C)C(=O)c2ccc(F)cc21

Basic Information

ChEMBL ID CHEMBL3286829
Phase Preclinical
Structure Type MOL
InChI Key SBEYSILWLYDNSN-GFCCVEGCSA-N
2
Targets
2
Activities
2
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

421.5
MW (Da)
3.81
ALogP
6
HBA
1
HBD
86.3
PSA (Ų)
0.65
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H24FN5O2
MW 421.48
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.48

Activity Summary

IC50 1 meas. best 8.24
Ki 1 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
BDNF/NT-3 growth factors receptor
CHEMBL4898
Ki 9.4 9.4 0.4 1
ALK tyrosine kinase receptor
CHEMBL4247
IC50 8.24 8.24 5.8 1

Pharmacokinetic Data

Parameter Value Units Species
CL 14.6 mL.min-1.kg-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24819116 10.1021/jm500261q ALK tyrosine kinase receptor 2
24819116 10.1021/jm500261q No relevant target 1
24819116 10.1021/jm500261q Liver microsome 1
24819116 10.1021/jm500261q MDCK 1
24819116 10.1021/jm500261q BDNF/NT-3 growth factors receptor 1
24819116 10.1021/jm500261q Unchecked 1

Data from ChEMBL 36 via Core Engine