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Compound Detail

CHEMBL3398615

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NCc1ccc(C(=O)N[C@@H](Cc2ccccc2)c2nc(-c3ccc4c(N)n[nH]c4c3)c(Cl)[nH]2)c(F)c1

Basic Information

ChEMBL ID CHEMBL3398615
Phase Preclinical
Structure Type MOL
InChI Key SXHMJNGJPFLPLF-NRFANRHFSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

504.0
MW (Da)
4.50
ALogP
5
HBA
5
HBD
138.5
PSA (Ų)
0.22
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H23ClFN7O
MW 503.97
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness -1.17

Activity Summary

Ki 2 meas. best 8.99

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
Ki 8.99 8.99 1.0 1
Trypsin
CHEMBL2095204
Ki 7.24 7.24 58.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XI Ki = 1.03 nM 8.99 Inhibition of human coagulation factor 11a at 25 degC 25728130
Trypsin Ki = 58.0 nM 7.24 Inhibition of human trypsin at 25 degC 25728130

Literature References

PubMed DOI Target Context # Activities
25728130 10.1016/j.bmcl.2015.01.028 Coagulation factor XI 1
25728130 10.1016/j.bmcl.2015.01.028 Trypsin 1

Data from ChEMBL 36 via Core Engine