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Compound Detail

CHEMBL3344396

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C(=C/c1ccc2c(ccn2CCCn2ccnc2)c1)\c1ccccc1

Basic Information

ChEMBL ID CHEMBL3344396
Phase Preclinical
Structure Type MOL
InChI Key QLAVBERHXIFWTE-BQYQJAHWSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

327.4
MW (Da)
5.10
ALogP
3
HBA
0
HBD
22.8
PSA (Ų)
0.45
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H21N3
MW 327.43
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -1.10

Activity Summary

IC50 2 meas. best 6.55
Ki 2 meas. best 7.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial
CHEMBL4521
Ki 7.43 7.43 37.0 1
25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial
CHEMBL3329080
Ki 7.34 7.34 46.0 1
25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial
CHEMBL3329080
IC50 6.55 6.55 280.0 1
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial
CHEMBL4521
IC50 6.28 6.28 520.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

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

Data from ChEMBL 36 via Core Engine