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Compound Detail

CHEMBL141266

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Cc1nc(N)ccc1CNC(=O)Cn1c(C)cnc(NC(C)(C)Cc2ccccc2)c1=O

Basic Information

ChEMBL ID CHEMBL141266
Phase Preclinical
Structure Type MOL
InChI Key GFWVZRBBUJMRSI-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
4
PK Parameters
4
Publications
0
Known Names

Molecular Properties

434.5
MW (Da)
2.59
ALogP
7
HBA
3
HBD
114.9
PSA (Ų)
0.50
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 C24H30N6O2
MW 434.54
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.13

Activity Summary

Ki 2 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 7.62 7.62 24.0 1
Serine protease 1
CHEMBL209
Ki 5.58 5.58 2600.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 803.9 ng.hr.mL-1 -
Cmax 600.0 nM Canis lupus familiaris
T1/2 2.133 hr Canis lupus familiaris
Tmax 0.4167 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9804686 10.1021/jm980368v Canis familiaris 3
9804686 10.1021/jm980368v Prothrombin 1
9804686 10.1021/jm980368v Serine protease 1 1
9804686 10.1021/jm980368v ADMET 1

Data from ChEMBL 36 via Core Engine