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Compound Detail

CHEMBL163771

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COc1ccc([C@@H]2Cc3c(cccc3C(F)(F)F)N(CCN(C)CCCCc3ccccc3)C(=O)[C@@H]2OC(C)=O)cc1

Basic Information

ChEMBL ID CHEMBL163771
Phase Preclinical
Structure Type MOL
InChI Key VXQKXTHFVVRBPP-JTSJOTPCSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

582.7
MW (Da)
6.27
ALogP
5
HBA
0
HBD
59.1
PSA (Ų)
0.20
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H37F3N2O4
MW 582.66
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness -0.16

Activity Summary

IC50 1 meas. best 7.14
Kd 1 meas. best 6.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.14 7.14 73.0 1
Voltage-dependent L-type calcium channel subunit alpha-1S
CHEMBL3805
Kd 6.66 6.66 220.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
1311765 10.1021/jm00082a020 Voltage-gated L-type calcium channel 3
1311765 10.1021/jm00082a020 Unchecked 1
1311765 10.1021/jm00082a020 Voltage-dependent L-type calcium channel subunit alpha-1S 1

Data from ChEMBL 36 via Core Engine