Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL5219643

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
NCc1cccc(-n2nc(C(F)(F)F)cc2C(=O)Nc2cc(C(N)(CCC3CC3)c3ccccc3)ccc2F)c1

Basic Information

ChEMBL ID CHEMBL5219643
Phase Preclinical
Structure Type MOL
InChI Key NQFNNZJJOCPZCP-UHFFFAOYSA-N
1
Targets
17
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

551.6
MW (Da)
6.13
ALogP
5
HBA
3
HBD
99.0
PSA (Ų)
0.22
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H29F4N5O
MW 551.59
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -1.33

Activity Summary

Ki 13 meas. best 7.6
IC50 4 meas. best 8.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasma kallikrein
CHEMBL2000
IC50 8.66 7.505 2.2 4
Plasma kallikrein
CHEMBL2000
Ki 7.6 7.6 25.1 13

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasma kallikrein IC50 = 2.2 nM 8.66 Inhibition of purified human plasma kallikrein using H-D-Pro-Phe-Arg-pNA.2HCl as... 36208543
Plasma kallikrein IC50 = 24.0 nM 7.62 Inhibition of endogenous human plasma kallikrein using Z-Phe-Arg-AMC.HCl as subs... 36208543
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 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 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 IC50 = 40.0 nM 7.4 Inhibition of purified human plasma kallikrein using H-D-Pro-Phe-Arg-pNA.2HCl as... 36208543
Plasma kallikrein IC50 = 453.0 nM 6.34 Inhibition of endogenous human plasma kallikrein using Z-Phe-Arg-AMC.HCl as subs... 36208543

Literature References

PubMed DOI Target Context # Activities
36208543 10.1016/j.bmc.2022.117035 Plasma kallikrein 4

Data from ChEMBL 36 via Core Engine