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Compound Detail

CHEMBL1270158

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CN(C)Cc1nccn1-c1ccc(NC(=O)c2cc(C(F)(F)F)nn2-c2ccc3onc(N)c3c2)cc1

Basic Information

ChEMBL ID CHEMBL1270158
Phase Preclinical
Structure Type MOL
InChI Key HXYFTCBUYCZYRZ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

510.5
MW (Da)
4.11
ALogP
9
HBA
2
HBD
120.0
PSA (Ų)
0.35
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H21F3N8O2
MW 510.48
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -1.85

Activity Summary

Ki 1 meas. best 9.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.01 9.01 1.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 41.67 mL.min-1.kg-1 Canis lupus familiaris
F 16.0 % Canis lupus familiaris
T1/2 1.6 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.97 nM 9.01 Inhibition of factor 10a 20503967

Literature References

PubMed DOI Target Context # Activities
20503967 10.1021/jm100146h Canis familiaris 4
20503967 10.1021/jm100146h Coagulation factor X 1
20503967 10.1021/jm100146h NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine