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Compound Detail

CHEMBL571976

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CC1=C(c2nc3cc(F)ccc3n2C)C(c2ccc(Cl)c(Cl)c2)n2nccc2N1

Basic Information

ChEMBL ID CHEMBL571976
Phase Preclinical
Structure Type MOL
InChI Key GSXVIOPVSCTVSK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

428.3
MW (Da)
5.66
ALogP
5
HBA
1
HBD
47.7
PSA (Ų)
0.45
QED
1
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H16Cl2FN5
MW 428.30
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.63

Activity Summary

IC50 1 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Potassium voltage-gated channel subfamily A member 5
CHEMBL4306
IC50 7.82 7.82 15.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 35.0 mL.min-1.kg-1 Rattus norvegicus
F 51.0 % Rattus norvegicus
T1/2 0.57 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19665893 10.1016/j.bmcl.2009.07.083 Unchecked 4
19665893 10.1016/j.bmcl.2009.07.083 Rattus norvegicus 4
19665893 10.1016/j.bmcl.2009.07.083 Potassium voltage-gated channel subfamily A member 5 1
19665893 10.1016/j.bmcl.2009.07.083 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine