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Compound Detail

CHEMBL597788

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O=C(CC(c1ccccc1)c1ccccc1)N1CCN(C(c2ccccc2)c2cccc(C(F)(F)F)c2)CC1

Basic Information

ChEMBL ID CHEMBL597788
Phase Preclinical
Structure Type MOL
InChI Key JDFLEUYRGZPZQD-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
8
PK Parameters
4
Publications
0
Known Names

Molecular Properties

528.6
MW (Da)
7.16
ALogP
2
HBA
0
HBD
23.6
PSA (Ų)
0.25
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H31F3N2O
MW 528.62
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.04

Activity Summary

IC50 5 meas. best 6.98

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Voltage-dependent N-type calcium channel subunit alpha-1B
CHEMBL5107
IC50 6.98 6.84 105.0 2
N-type calcium channel alpha-1b/alpha2delta-1/beta-1b
CHEMBL4106160
IC50 6.96 6.96 110.0 1
Voltage-dependent L-type calcium channel alpha1C/alpha2delta/beta1b
CHEMBL3988638
IC50 5.75 5.465 1800.0 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 762.27 ng.hr.mL-1 Rattus norvegicus
AUC 2468.66 ng.hr.mL-1 Rattus norvegicus
Cmax 518.0 nM Rattus norvegicus
Cmax 2540.0 nM Rattus norvegicus
F 65.0 % Rattus norvegicus
T1/2 5.0 hr Rattus norvegicus
T1/2 4.0 hr Rattus norvegicus
Tmax 5.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20117000 10.1016/j.bmcl.2010.01.008 Rattus norvegicus 10
20117000 10.1016/j.bmcl.2010.01.008 Voltage-dependent L-type calcium channel alpha1C/alpha2delta/beta1b 2
20117000 10.1016/j.bmcl.2010.01.008 No relevant target 1
20117000 10.1016/j.bmcl.2010.01.008 N-type calcium channel alpha-1b/alpha2delta-1/beta-1b 1

Data from ChEMBL 36 via Core Engine