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Compound Detail

CHEMBL101563

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Cc1cnc(NCCc2ccccc2)c(=O)n1CC(=O)NCc1ccc2[nH]cnc2c1

Basic Information

ChEMBL ID CHEMBL101563
Phase Preclinical
Structure Type MOL
InChI Key BDCJAGQAAOPKLF-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
3
PK Parameters
5
Publications
0
Known Names

Molecular Properties

416.5
MW (Da)
2.40
ALogP
6
HBA
3
HBD
104.7
PSA (Ų)
0.41
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 C23H24N6O2
MW 416.49
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.57

Activity Summary

Ki 2 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 7.96 7.96 11.0 1
Serine protease 1
CHEMBL209
Ki 5.7 5.7 2000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1633.33 ng.hr.mL-1 Canis lupus familiaris
Cmax 936.4 nM Canis lupus familiaris
T1/2 1.767 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 11.0 nM 7.96 Inhibition of Thrombin 12617893
Serine protease 1 Ki = 2000.0 nM 5.7 Inhibition of Trypsin 12617893

Literature References

PubMed DOI Target Context # Activities
12270176 10.1016/s0960-894x(02)00585-1 Canis familiaris 3
12617893 10.1016/s0960-894x(03)00017-9 Prothrombin 1
12617893 10.1016/s0960-894x(03)00017-9 Serine protease 1 1
12270176 10.1016/s0960-894x(02)00585-1 Prothrombin 1
12270176 10.1016/s0960-894x(02)00585-1 No relevant target 1

Data from ChEMBL 36 via Core Engine