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Compound Detail

CHEMBL172550

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CCOC(=O)C1=C(C)N=C(C)/C(=C(/O)OCC)C1c1c(-c2cc(Cl)ccc2OC)noc1C

Basic Information

ChEMBL ID CHEMBL172550
Phase Preclinical
Structure Type MOL
InChI Key QAHNETHDKINHBR-PTGBLXJZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

474.9
MW (Da)
5.51
ALogP
8
HBA
1
HBD
103.4
PSA (Ų)
0.42
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H27ClN2O6
MW 474.94
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.97

Activity Summary

IC50 1 meas. best 5.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 5.16 5.16 6860.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 6860.0 nM 5.16 Inhibition of L-type calcium channel subunits alpha1C, beta1b, and alpha2-delta ... 12502362

Literature References

PubMed DOI Target Context # Activities
12502362 10.1021/jm020354w Unchecked 3
23063517 10.1016/j.bmc.2012.09.022 ATP-dependent translocase ABCB1 1
23063517 10.1016/j.bmc.2012.09.022 Unchecked 1

Data from ChEMBL 36 via Core Engine