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Compound Detail

CHEMBL279187

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COc1ccc(-n2nc(C(N)=O)c3c2C(=O)N(c2ccc(-c4ccccc4CN)cc2)CC3)cc1

Basic Information

ChEMBL ID CHEMBL279187
Phase Preclinical
Structure Type MOL
InChI Key GNENBXDFTFJVCO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
5
Publications
0
Known Names

Molecular Properties

467.5
MW (Da)
3.31
ALogP
6
HBA
2
HBD
116.5
PSA (Ų)
0.45
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H25N5O3
MW 467.53
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.85

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 - - Canis lupus familiaris
F - % Canis lupus familiaris
t1/2 - - 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 Binding affinity to human F10a 17914785

Literature References

PubMed DOI Target Context # Activities
17914785 10.1021/jm070245n Canis familiaris 4
17914785 10.1021/jm070245n Plasma 1
17914785 10.1021/jm070245n Coagulation factor X 1
17914785 10.1021/jm070245n Oryctolagus cuniculus 1
17914785 10.1021/jm070245n Caco-2 1

Data from ChEMBL 36 via Core Engine