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Compound Detail

CHEMBL3398618

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Nc1n[nH]c2cc(C(=O)N[C@@H](Cc3ccccc3)c3nc(-c4ccc5c(N)n[nH]c5c4)c(Cl)[nH]3)ccc12

Basic Information

ChEMBL ID CHEMBL3398618
Phase Preclinical
Structure Type MOL
InChI Key QEDSKDDUNJZZHC-FQEVSTJZSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

512.0
MW (Da)
4.36
ALogP
6
HBA
6
HBD
167.2
PSA (Ų)
0.19
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H22ClN9O
MW 511.98
Aromatic Rings 6
Heavy Atoms 37
NP-Likeness -0.87

Activity Summary

Ki 2 meas. best 7.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
Ki 7.24 7.24 58.0 1
Trypsin
CHEMBL2095204
Ki 5.85 5.85 1400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XI Ki = 58.0 nM 7.24 Inhibition of human coagulation factor 11a at 25 degC 25728130
Trypsin Ki = 1400.0 nM 5.85 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