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Compound Detail

CHEMBL4576507

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[2H][C@]1(c2c(F)ccc(Cl)c2F)CCN([C@H]2C/C=C/CCC(=O)Nc3cc(NC(=O)OC)ccc3-c3nc2[nH]c3Cl)C(=O)O1

Basic Information

ChEMBL ID CHEMBL4576507
Phase Preclinical
Structure Type MOL
InChI Key AYXFLKXWZHHQPA-VJCXLJATSA-N
Parent Compound CHEMBL4467360
Active Moiety CHEMBL4467360
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

620.4
MW (Da)
7.14
ALogP
6
HBA
3
HBD
125.7
PSA (Ų)
0.21
QED
2
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H25Cl2F2N5O5
MW 621.45
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness -0.68

Activity Summary

Ki 1 meas. best 9.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
Ki 9.57 9.57 0.3 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.2667 hr Homo sapiens
T1/2 0.5167 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31445854 10.1016/j.bmcl.2019.08.008 ADMET 2
31445854 10.1016/j.bmcl.2019.08.008 Coagulation factor XI 1
31445854 10.1016/j.bmcl.2019.08.008 Plasma 1

Data from ChEMBL 36 via Core Engine