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Compound Detail

CHEMBL221231

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CN(C)C(=N)c1ccc(C(=O)Nc2ccc(OCC(=O)O)cc2C(=O)Nc2ccc(Cl)cn2)cc1

Basic Information

ChEMBL ID CHEMBL221231
Phase Preclinical
Structure Type MOL
InChI Key VCQUPPLFOBCIHW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

495.9
MW (Da)
3.59
ALogP
6
HBA
4
HBD
144.7
PSA (Ų)
0.28
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H22ClN5O5
MW 495.92
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.41

Activity Summary

IC50 1 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 8.22 8.22 6.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 5.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 6.0 nM 8.22 Inhibition of Factor 10a 19297154

Literature References

PubMed DOI Target Context # Activities
16931010 10.1016/j.bmcl.2006.08.039 Voltage-gated inwardly rectifying potassium channel KCNH2 1
19297154 10.1016/j.bmcl.2009.02.111 Coagulation factor X 1
19297154 10.1016/j.bmcl.2009.02.111 Plasma 1
19297154 10.1016/j.bmcl.2009.02.111 Voltage-gated inwardly rectifying potassium channel KCNH2 1
19297154 10.1016/j.bmcl.2009.02.111 Rattus norvegicus 1
20503967 10.1021/jm100146h Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine