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Compound Detail

CHEMBL1801185

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Cc1nnc(N2CCCC2)c2nn(-c3ccc(Cl)cc3OC(F)(F)F)c(C)c12

Basic Information

ChEMBL ID CHEMBL1801185
Phase Preclinical
Structure Type MOL
InChI Key JWUFFURPSKRHTA-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

411.8
MW (Da)
4.58
ALogP
6
HBA
0
HBD
56.1
PSA (Ų)
0.63
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H17ClF3N5O
MW 411.82
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.87

Activity Summary

IC50 2 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Voltage-dependent calcium channel subunit alpha-2/delta-1
CHEMBL1919
IC50 8.52 8.52 3.0 1
Voltage-dependent calcium channel subunit alpha-2/delta-2
CHEMBL3896
IC50 6.1 6.1 794.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 0.6 mL.min-1.g-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 Liver microsomes 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 Voltage-dependent calcium channel subunit alpha-2/delta-2 1

Data from ChEMBL 36 via Core Engine