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Compound Detail

CHEMBL355314

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Cc1cnc(NCCc2ccccn2)c(=O)n1CC(=O)NCc1cc2cc[nH]c2cn1

Basic Information

ChEMBL ID CHEMBL355314
Phase Preclinical
Structure Type MOL
InChI Key YTKUDXQPZJABDC-UHFFFAOYSA-N
1
Targets
4
Activities
1
Assay Types
5
PK Parameters
7
Publications
0
Known Names

Molecular Properties

417.5
MW (Da)
1.79
ALogP
7
HBA
3
HBD
117.6
PSA (Ų)
0.40
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 C22H23N7O2
MW 417.47
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.63

Activity Summary

Ki 4 meas. best 8.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.92 8.92 1.2 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 70.97 ng.hr.mL-1 Canis lupus familiaris
AUC 70.97 ng.hr.mL-1 Canis lupus familiaris
Cmax 180.0 nM Canis lupus familiaris
Cmax 180.0 nM Canis lupus familiaris
T1/2 - hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12617893 10.1016/s0960-894x(03)00017-9 Canis familiaris 3
29407959 10.1016/j.ejmech.2018.01.067 Canis familiaris 2
12617893 10.1016/s0960-894x(03)00017-9 Prothrombin 1
12617893 10.1016/s0960-894x(03)00017-9 Serine protease 1 1
12617893 10.1016/s0960-894x(03)00017-9 NON-PROTEIN TARGET 1
29407959 10.1016/j.ejmech.2018.01.067 Trypsin 1
29407959 10.1016/j.ejmech.2018.01.067 Prothrombin 1

Data from ChEMBL 36 via Core Engine