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Compound Detail

CHEMBL170063

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N=C(N)c1ccc2c(ccn2CC(=O)N2CCC(Cc3cccc(F)c3)CC2)c1

Basic Information

ChEMBL ID CHEMBL170063
Phase Preclinical
Structure Type MOL
InChI Key CELLYTXIAPGBBG-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

392.5
MW (Da)
3.55
ALogP
3
HBA
2
HBD
75.1
PSA (Ų)
0.51
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25FN4O
MW 392.48
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.39

Activity Summary

Ki 2 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 7.62 7.62 24.0 1
Unchecked
CHEMBL612545
Ki 4.96 4.96 11000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 24.0 nM 7.62 Inhibition of Coagulation factor II 10230612
Unchecked Ki = 11000.0 nM 4.96 Inhibition of factor Xa 10230612

Literature References

PubMed DOI Target Context # Activities
10230612 10.1016/s0960-894x(99)00113-4 Prothrombin 1
10230612 10.1016/s0960-894x(99)00113-4 Serine protease 1 1
10230612 10.1016/s0960-894x(99)00113-4 Unchecked 1

Data from ChEMBL 36 via Core Engine