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Compound Detail

CHEMBL3344393

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COc1cc(/C=C/c2cccc3c2ccn3CCCn2ccnc2)cc(OC)c1

Basic Information

ChEMBL ID CHEMBL3344393
Phase Preclinical
Structure Type MOL
InChI Key JNCMZCZFSIAVQJ-BQYQJAHWSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

387.5
MW (Da)
5.12
ALogP
5
HBA
0
HBD
41.2
PSA (Ų)
0.39
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H25N3O2
MW 387.48
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.01

Activity Summary

IC50 2 meas. best 6.85
Ki 2 meas. best 7.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial
CHEMBL3329080
Ki 7.66 7.66 22.0 1
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial
CHEMBL4521
Ki 7.51 7.51 31.0 1
25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial
CHEMBL3329080
IC50 6.85 6.85 140.0 1
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial
CHEMBL4521
IC50 6.36 6.36 440.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25240094 10.1016/j.ejmech.2014.09.035 25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial 2
25240094 10.1016/j.ejmech.2014.09.035 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial 2
25240094 10.1016/j.ejmech.2014.09.035 Unchecked 1

Data from ChEMBL 36 via Core Engine