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

CHEMBL4847070

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(NCC3CC3)c3ccccc3)ccc2F)c1

Basic Information

ChEMBL ID CHEMBL4847070
Phase Preclinical
Structure Type MOL
InChI Key MCLZOCFEIKBMBA-UHFFFAOYSA-N
1
Targets
30
Activities
2
Assay Types
5
PK Parameters
4
Publications
0
Known Names

Molecular Properties

537.6
MW (Da)
5.83
ALogP
5
HBA
3
HBD
85.0
PSA (Ų)
0.23
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 C29H27F4N5O
MW 537.56
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.56

Activity Summary

Ki 21 meas. best 7.6
IC50 9 meas. best 8.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasma kallikrein
CHEMBL2000
IC50 8.92 7.7878 1.2 9
Plasma kallikrein
CHEMBL2000
Ki 7.6 7.6 25.1 21

Pharmacokinetic Data

Parameter Value Units Species
AUC 493.0 ng.hr.mL-1 Rattus norvegicus
AUC 852.0 ng.hr.mL-1 Rattus norvegicus
AUC 1494.0 ng.hr.mL-1 Rattus norvegicus
Cmax 94.87 nM Rattus norvegicus
Cmax 247.41 nM Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasma kallikrein IC50 = 1.2 nM 8.92 Inhibition of purified human plasma kallikrein using H-D-Pro-Phe-Arg-pNA.2HCl as... 34436898
Plasma kallikrein IC50 = 8.51 nM 8.07 Inhibition of endogenous human plasma kallikrein using Z-Phe-Arg-AMC.HCl as subs... 34436898
Plasma kallikrein IC50 = 9.0 nM 8.05 Inhibition of purified human plasma kallikrein using H-D-Pro-Phe-Arg-pNA.2HCl as... 34436898
Plasma kallikrein IC50 = 9.0 nM 8.05 Inhibition of purified human plasma kallikrein using H-D-Pro-Phe-Arg-pNA.2HCl as... 36208543
Plasma kallikrein IC50 = 19.0 nM 7.72 Inhibition of endogenous human plasma kallikrein using Z-Phe-Arg-AMC.HCl as subs... 34436898
Plasma kallikrein IC50 = 19.1 nM 7.72 Inhibition of endogenous human plasma kallikrein using Z-Phe-Arg-AMC.HCl as subs... 36208543
Plasma kallikrein IC50 = 24.0 nM 7.62 Inhibition of purified human plasma kallikrein using H-D-Pro-Phe-Arg-pNA.2HCl as... 34436898
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: 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 hu... -
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: 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 hu... -
Plasma kallikrein Ki = 25.1 nM 7.6 Activity Assay: The effect of compounds of the invention on human plasma kallikr... -

Literature References

PubMed DOI Target Context # Activities
34436898 10.1021/acs.jmedchem.1c00511 ADMET 8
34436898 10.1021/acs.jmedchem.1c00511 Plasma kallikrein 6
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