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Compound Detail

CHEMBL569185

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COc1ccc(CCN2C(=O)N(NS(C)(=O)=O)C[C@H]2c2ccc(OC)cc2)cc1

Basic Information

ChEMBL ID CHEMBL569185
Phase Preclinical
Structure Type MOL
InChI Key GFFIHDXPUGXVGG-IBGZPJMESA-N
8
Targets
9
Activities
1
Assay Types
11
PK Parameters
19
Publications
0
Known Names

Molecular Properties

419.5
MW (Da)
2.19
ALogP
5
HBA
1
HBD
88.2
PSA (Ų)
0.71
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H25N3O5S
MW 419.50
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.64

Activity Summary

IC50 9 meas. best 6.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Potassium voltage-gated channel subfamily A member 5
CHEMBL4306
IC50 6.32 6.32 480.0 1
Potassium voltage-gated channel subfamily A member 3
CHEMBL4633
IC50 5.85 5.85 1410.0 1
Potassium voltage-gated channel subfamily A member 1
CHEMBL2309
IC50 5.58 5.58 2660.0 1
A-type voltage-gated potassium channel KCND3
CHEMBL1964
IC50 5.41 5.41 3870.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.82 4.82 15100.0 1
Voltage-dependent L-type calcium channel subunit alpha-1D
CHEMBL4138
IC50 4.63 4.63 23400.0 1
Cytochrome P450 3A4
CHEMBL340
IC50 4.43 4.43 37000.0 1
Cytochrome P450 2C9
CHEMBL3397
IC50 4.33 4.33 47000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 2412.0 ng.hr.mL-1 Canis lupus familiaris
AUC 1989.0 ng.hr.mL-1 Canis lupus familiaris
CL 23.0 mL.min-1.kg-1 Canis lupus familiaris
CL 21.88 uL.min-1.(10^6cells)-1 Homo sapiens
Cmax 1118.0 nM Canis lupus familiaris
F 82.0 % Canis lupus familiaris
T1/2 0.5 hr Homo sapiens
T1/2 0.1833 hr Canis lupus familiaris
T1/2 1.2 hr Canis lupus familiaris
T1/2 1.7 hr Canis lupus familiaris
Tmax 1.0 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19888755 10.1021/jm901042m Canis familiaris 20
- 10.6019/CHEMBL3301361 ADMET 4
19888755 10.1021/jm901042m Plasma 2
19888755 10.1021/jm901042m Caco-2 2
19888755 10.1021/jm901042m Cytochrome P450 3A4 2
19888755 10.1021/jm901042m Potassium voltage-gated channel subfamily A member 3 1
19888755 10.1021/jm901042m Unchecked 1
19888755 10.1021/jm901042m Cytochrome P450 2C9 1
19888755 10.1021/jm901042m Cytochrome P450 2D6 1
19888755 10.1021/jm901042m ADMET 1
19888755 10.1021/jm901042m A-type voltage-gated potassium channel KCND3 1
19888755 10.1021/jm901042m Potassium voltage-gated channel subfamily A member 1 1
19888755 10.1021/jm901042m Voltage-dependent L-type calcium channel subunit alpha-1C 1
19888755 10.1021/jm901042m Voltage-dependent L-type calcium channel subunit alpha-1D 1
19888755 10.1021/jm901042m Sodium channel protein type 5 subunit alpha 1
19888755 10.1021/jm901042m Voltage-gated inwardly rectifying potassium channel KCNH2 1
19888755 10.1021/jm901042m Potassium voltage-gated channel subfamily A member 5 1
19888755 10.1021/jm901042m Liver microsomes 1
19888755 10.1021/jm901042m No relevant target 1

Data from ChEMBL 36 via Core Engine