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Compound Detail

CHEMBL497096

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Cc1cccc(C)c1CNc1cc(-n2ccccc2=O)cn2c(CO)c(C)nc12

Basic Information

ChEMBL ID CHEMBL497096
Phase Preclinical
Structure Type MOL
InChI Key TWPYUBYLSOSBJQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
3
Publications
0
Known Names

Molecular Properties

388.5
MW (Da)
3.51
ALogP
6
HBA
2
HBD
71.6
PSA (Ų)
0.55
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 C23H24N4O2
MW 388.47
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.15

Activity Summary

IC50 1 meas. best 6.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.9 6.9 125.9 1

Pharmacokinetic Data

Parameter Value Units Species
CL 37.0 mL.min-1.kg-1 Rattus norvegicus
CL 10.0 mL.min-1.kg-1 Canis lupus familiaris
F 28.0 % Rattus norvegicus
F 36.0 % Canis lupus familiaris
T1/2 5.3 hr Rattus norvegicus
T1/2 1.6 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 125.89 nM 6.9 Inhibition of H+/K+ ATPase 19467868

Literature References

PubMed DOI Target Context # Activities
19467868 10.1016/j.bmcl.2009.04.127 Rattus norvegicus 6
19467868 10.1016/j.bmcl.2009.04.127 Canis familiaris 4
19467868 10.1016/j.bmcl.2009.04.127 Unchecked 1

Data from ChEMBL 36 via Core Engine