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Compound Detail

CHEMBL179410

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Cc1nccn1-c1ccc(NC(=O)c2cc(C(F)(F)F)nn2-c2ccc3onc(N)c3c2)c(C#N)c1

Basic Information

ChEMBL ID CHEMBL179410
Phase Preclinical
Structure Type MOL
InChI Key KEOSSYBRTAEQPD-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

492.4
MW (Da)
4.23
ALogP
9
HBA
2
HBD
140.6
PSA (Ų)
0.38
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H15F3N8O2
MW 492.42
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness -2.02

Activity Summary

Ki 2 meas. best 9.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.28 9.28 0.5 1
Prothrombin
CHEMBL204
Ki 6.05 6.05 900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.52 nM 9.28 Binding affinity against human Coagulation factor Xa 15771420
Prothrombin Ki = 900.0 nM 6.05 Binding affinity against human thrombin 15771420

Literature References

PubMed DOI Target Context # Activities
15771420 10.1021/jm0497949 Coagulation factor X 1
15771420 10.1021/jm0497949 Prothrombin 1
15771420 10.1021/jm0497949 Caco-2 1
21413808 10.1021/jm1013693 Caco-2 1
29400967 10.1021/acs.jmedchem.7b01788 ADMET 1

Data from ChEMBL 36 via Core Engine