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Compound Detail

CHEMBL281762

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COc1ccc(C2Sc3ccccc3-n3c(CN4CCOCC4)ccc32)c(OC)c1

Basic Information

ChEMBL ID CHEMBL281762
Phase Preclinical
Structure Type MOL
InChI Key UAZHCBHXTWVCAF-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

422.6
MW (Da)
4.52
ALogP
6
HBA
0
HBD
35.9
PSA (Ų)
0.60
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H26N2O3S
MW 422.55
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.94

Activity Summary

IC50 2 meas. best 5.91
Ki 1 meas. best 6.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Voltage-gated L-type calcium channel
CHEMBL2095177
Ki 6.34 6.34 461.0 1
Voltage-gated L-type calcium channel
CHEMBL2095177
IC50 5.91 5.91 1230.0 1
Voltage-dependent L-type calcium channel subunit alpha-1D
CHEMBL4132
IC50 5.91 5.91 1230.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7473567 10.1021/jm00022a005 Voltage-gated L-type calcium channel 2
9016337 10.1021/jm9605647 Voltage-dependent L-type calcium channel subunit alpha-1D 1

Data from ChEMBL 36 via Core Engine