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Compound Detail

CHEMBL3398637

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Nc1n[nH]c2cc(-c3nc([C@H](Cc4ccccc4)NC(=O)NCc4cc(Cl)ccc4-n4cccn4)[nH]c3Cl)ccc12

Basic Information

ChEMBL ID CHEMBL3398637
Phase Preclinical
Structure Type MOL
InChI Key ZTWCMSKJJMBCDA-QHCPKHFHSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
4
Publications
0
Known Names

Molecular Properties

586.5
MW (Da)
5.81
ALogP
6
HBA
5
HBD
142.3
PSA (Ų)
0.15
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H25Cl2N9O
MW 586.49
Aromatic Rings 6
Heavy Atoms 41
NP-Likeness -1.65

Activity Summary

Ki 1 meas. best 6.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
Ki 6.35 6.35 450.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL - - Canis lupus familiaris
F - % Canis lupus familiaris
t1/2 - - 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 = 450.0 nM 6.35 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