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Compound Detail

CHEMBL3314454

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COc1ccc(-n2nc(C(N)=O)c3c2C(=O)N(c2ccc(C(C)(C)N4CCCC4)cc2)CC3)cc1

Basic Information

ChEMBL ID CHEMBL3314454
Phase Preclinical
Structure Type MOL
InChI Key DKVRJOBFFAOUJG-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

473.6
MW (Da)
3.51
ALogP
6
HBA
1
HBD
93.7
PSA (Ų)
0.59
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 C27H31N5O3
MW 473.58
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.94

Activity Summary

Ki 1 meas. best 10.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 10.15 10.15 0.1 1

Pharmacokinetic Data

Parameter Value Units Species
CL 126.67 mL.min-1.kg-1 Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.07 nM 10.15 Inhibition of purified human factor Xa 24951330

Literature References

PubMed DOI Target Context # Activities
24951330 10.1016/j.bmcl.2014.05.101 Canis familiaris 2
24951330 10.1016/j.bmcl.2014.05.101 Coagulation factor X 1
24951330 10.1016/j.bmcl.2014.05.101 ADMET 1
24951330 10.1016/j.bmcl.2014.05.101 Plasma 1

Data from ChEMBL 36 via Core Engine