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Compound Detail

CHEMBL598603

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COc1ccc(C(c2ccc(OC)cc2)N2CCN(C(=O)CC(c3ccccc3)c3ccccc3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL598603
Phase Preclinical
Structure Type MOL
InChI Key CBDZLOJIUYHCHO-UHFFFAOYSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

520.7
MW (Da)
6.16
ALogP
4
HBA
0
HBD
42.0
PSA (Ų)
0.27
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H36N2O3
MW 520.67
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -0.72

Activity Summary

IC50 5 meas. best 6.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
N-type calcium channel alpha-1b/alpha2delta-1/beta-1b
CHEMBL4106160
IC50 6.62 6.62 240.0 1
Voltage-dependent N-type calcium channel subunit alpha-1B
CHEMBL5107
IC50 6.6 6.52 249.0 2
Voltage-dependent T-type calcium channel subunit alpha-1G
CHEMBL4641
IC50 6.13 6.13 745.0 1
Voltage-dependent L-type calcium channel alpha1C/alpha2delta/beta1b
CHEMBL3988638
IC50 5.54 5.54 2900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20117000 10.1016/j.bmcl.2010.01.008 Voltage-dependent L-type calcium channel alpha1C/alpha2delta/beta1b 1
20117000 10.1016/j.bmcl.2010.01.008 N-type calcium channel alpha-1b/alpha2delta-1/beta-1b 1

Data from ChEMBL 36 via Core Engine