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Compound Detail

CHEMBL176157

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

Basic Information

ChEMBL ID CHEMBL176157
Phase Preclinical
Structure Type MOL
InChI Key XEHHJCXFVJSRRN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

510.4
MW (Da)
3.46
ALogP
9
HBA
3
HBD
159.9
PSA (Ų)
0.33
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H17F3N8O3
MW 510.44
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -1.88

Activity Summary

Ki 1 meas. best 8.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.11 8.11 7.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 7.7 nM 8.11 Binding affinity against human Coagulation factor Xa 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

Data from ChEMBL 36 via Core Engine