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Compound Detail

CHEMBL3398621

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C[C@H]1CC[C@H](C(=O)N[C@@H](Cc2ccccc2)c2nc(-c3ccc4c(N)n[nH]c4c3)c(Cl)[nH]2)CC1

Basic Information

ChEMBL ID CHEMBL3398621
Phase Preclinical
Structure Type MOL
InChI Key ZTZYRDIKEKUGBU-WJPUGNRLSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

477.0
MW (Da)
5.41
ALogP
4
HBA
4
HBD
112.5
PSA (Ų)
0.30
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H29ClN6O
MW 477.01
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.92

Activity Summary

Ki 1 meas. best 7.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
Ki 7.17 7.17 68.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 15.4 mL.min-1.kg-1 Canis lupus familiaris
F 1.0 % Canis lupus familiaris
T1/2 1.5 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XI Ki = 68.0 nM 7.17 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 Trypsin 1
25728130 10.1016/j.bmcl.2015.01.028 ADMET 1

Data from ChEMBL 36 via Core Engine