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Compound Detail

CHEMBL4868429

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NCc1cccc(-n2nc(C(F)(F)F)cc2C(=O)Nc2cc(C(OCC3CC3)c3ccccc3)ccc2F)c1

Basic Information

ChEMBL ID CHEMBL4868429
Phase Preclinical
Structure Type MOL
InChI Key HIMJVDQVZQMIPM-UHFFFAOYSA-N
1
Targets
25
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

538.5
MW (Da)
6.26
ALogP
5
HBA
2
HBD
82.2
PSA (Ų)
0.25
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H26F4N4O2
MW 538.55
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.45

Activity Summary

Ki 20 meas. best 7.6
IC50 5 meas. best 8.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasma kallikrein
CHEMBL2000
IC50 8.19 7.092 6.4 5
Plasma kallikrein
CHEMBL2000
Ki 7.6 7.6 25.1 20

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasma kallikrein IC50 = 6.4 nM 8.19 Inhibition of purified human plasma kallikrein using H-D-Pro-Phe-Arg-pNA.2HCl as... 34436898
Plasma kallikrein Ki = 25.1 nM 7.6 Activity Assay: The effect of compounds of the invention on human plasma kallikr... -
Plasma kallikrein Ki = 25.1 nM 7.6 Plasma Kallikrein Activity Assay: Plasma kallikrein activity assay. The effect o... -
Plasma kallikrein Ki = 25.1 nM 7.6 Plasma Kallikrein Activity Assay: Plasma kallikrein activity assay. The effect o... -
Plasma kallikrein Ki = 25.1 nM 7.6 Plasma Kallikrein Activity Assay: Plasma kallikrein activity assay. The effect o... -
Plasma kallikrein Ki = 25.1 nM 7.6 Plasma Kallikrein Activity Assay: Plasma kallikrein activity assay. The effect o... -
Plasma kallikrein Ki = 25.1 nM 7.6 Plasma Kallikrein Activity Assay: Plasma kallikrein activity assay. The effect o... -
Plasma kallikrein Ki = 25.1 nM 7.6 Plasma Kallikrein Activity Assay: Plasma kallikrein activity assay. The effect o... -
Plasma kallikrein Ki = 25.1 nM 7.6 Plasma Kallikrein Activity Assay.: The effect of compounds of the invention on h... -
Plasma kallikrein Ki = 25.1 nM 7.6 Plasma Kallikrein Activity Assay.: The effect of compounds of the invention on h... -
Plasma kallikrein Ki = 25.1 nM 7.6 Plasma Kallikrein Activity Assay.: The effect of compounds of the invention on h... -
Plasma kallikrein Ki = 25.1 nM 7.6 Plasma kallikrein Activity Assay: The effect of compounds of the invention on hu... -
Plasma kallikrein Ki = 25.1 nM 7.6 Plasma kallikrein Activity Assay: The effect of compounds of the invention on hu... -
Plasma kallikrein Ki = 25.1 nM 7.6 Activity Assay: The effect of compounds of the invention on human plasma kallikr... -
Plasma kallikrein Ki = 25.1 nM 7.6 Activity Assay: The effect of compounds of the invention on human plasma kallikr... -
Plasma kallikrein Ki = 25.1 nM 7.6 Activity Assay: The effect of compounds of the invention on human plasma kallikr... -
Plasma kallikrein Ki = 25.1 nM 7.6 Activity Assay: The effect of compounds of the invention on human plasma kallikr... -
Plasma kallikrein Ki = 25.1 nM 7.6 Activity Assay: The effect of compounds of the invention on human plasma kallikr... -
Plasma kallikrein Ki = 25.1 nM 7.6 Plasma Kallikrein Activity Assay: The effect of compounds of the invention on hu... -
Plasma kallikrein Ki = 25.1 nM 7.6 Plasma Kallikrein Activity Assay: The effect of compounds of the invention on hu... -

Literature References

PubMed DOI Target Context # Activities
34436898 10.1021/acs.jmedchem.1c00511 Plasma kallikrein 2
36208543 10.1016/j.bmc.2022.117035 Plasma kallikrein 2
32066009 10.1016/j.ejmech.2020.112137 Plasma kallikrein 1

Data from ChEMBL 36 via Core Engine