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Compound Detail

CHEMBL1801179

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CCOc1ccc(-n2nc3c(N4CC[C@@H](OC)C4)nnc(C)c3c2C)cc1

Basic Information

ChEMBL ID CHEMBL1801179
Phase Preclinical
Structure Type MOL
InChI Key CMKXTNFXBYWXGN-QGZVFWFLSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

367.4
MW (Da)
3.06
ALogP
7
HBA
0
HBD
65.3
PSA (Ų)
0.69
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 C20H25N5O2
MW 367.45
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.72

Activity Summary

IC50 2 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Voltage-dependent calcium channel subunit alpha-2/delta-1
CHEMBL1919
IC50 8.22 8.22 6.0 1
Voltage-dependent calcium channel subunit alpha-2/delta-2
CHEMBL3896
IC50 7.1 7.1 79.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 51.0 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20566291 10.1016/j.bmcl.2010.05.026 Rattus norvegicus 1
20566291 10.1016/j.bmcl.2010.05.026 ADMET 1
20566291 10.1016/j.bmcl.2010.05.026 Voltage-dependent calcium channel subunit alpha-2/delta-1 1
20566291 10.1016/j.bmcl.2010.05.026 Unchecked 1
20566291 10.1016/j.bmcl.2010.05.026 Voltage-dependent calcium channel subunit alpha-2/delta-2 1

Data from ChEMBL 36 via Core Engine