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Compound Detail

CHEMBL133623

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N=C(N)c1ccc(CNC(=O)Cn2c(-c3ccccc3)c(Cl)nc(NCc3ccccc3)c2=O)cc1

Basic Information

ChEMBL ID CHEMBL133623
Phase Preclinical
Structure Type MOL
InChI Key POBRKUJXLKRHCP-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

501.0
MW (Da)
3.78
ALogP
6
HBA
4
HBD
125.9
PSA (Ų)
0.21
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H25ClN6O2
MW 500.99
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.00

Activity Summary

IC50 4 meas. best 6.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor VII/tissue factor
CHEMBL2095194
IC50 6.11 6.11 770.0 2
Prothrombin
CHEMBL204
IC50 5.12 5.12 7630.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12954058 10.1021/jm030131l Coagulation factor VII/tissue factor 1
12954058 10.1021/jm030131l Prothrombin 1
12954058 10.1021/jm030131l Unchecked 1
29407959 10.1016/j.ejmech.2018.01.067 Prothrombin 1
29407959 10.1016/j.ejmech.2018.01.067 Coagulation factor VII/tissue factor 1

Data from ChEMBL 36 via Core Engine