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Compound Detail

CHEMBL3398639

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COC(=O)Nc1ccc(-c2nc([C@H](Cc3ccccc3)NC(=O)NCc3cc(Cl)ccc3-n3cnnn3)[nH]c2Cl)cc1

Basic Information

ChEMBL ID CHEMBL3398639
Phase Preclinical
Structure Type MOL
InChI Key WGSFSUZPGGHIJB-QFIPXVFZSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
4
Publications
0
Known Names

Molecular Properties

606.5
MW (Da)
5.32
ALogP
8
HBA
4
HBD
151.7
PSA (Ų)
0.18
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H25Cl2N9O3
MW 606.47
Aromatic Rings 5
Heavy Atoms 42
NP-Likeness -1.87

Activity Summary

Ki 1 meas. best 8.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
Ki 8.47 8.47 3.4 1

Pharmacokinetic Data

Parameter Value Units Species
CL 34.5 mL.min-1.kg-1 Canis lupus familiaris
F - % Canis lupus familiaris
T1/2 2.8 hr Canis lupus familiaris
T1/2 0.01667 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XI Ki = 3.4 nM 8.47 Inhibition of human coagulation factor 11a at 25 degC 25728130

Literature References

PubMed DOI Target Context # Activities
25728130 10.1016/j.bmcl.2015.01.028 Canis familiaris 4
25728130 10.1016/j.bmcl.2015.01.028 Coagulation factor XI 1
25728130 10.1016/j.bmcl.2015.01.028 Plasma 1
25728130 10.1016/j.bmcl.2015.01.028 Liver microsome 1

Data from ChEMBL 36 via Core Engine