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Compound Detail

CHEMBL536972

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Cl.NCCCC[C@H](NC(=O)c1ccc(F)c(F)c1)C(=O)c1noc(Cc2ccc(OCCc3ccc(Cl)c(Cl)c3)cc2)n1

Basic Information

ChEMBL ID CHEMBL536972
Phase Preclinical
Structure Type MOL
InChI Key OQXHDVFOGPLGCK-SNYZSRNZSA-N
Parent Compound CHEMBL1188643
Active Moiety CHEMBL1188643
5
Targets
6
Activities
1
Assay Types
0
PK Parameters
17
Publications
0
Known Names

Molecular Properties

617.5
MW (Da)
5.98
ALogP
7
HBA
2
HBD
120.3
PSA (Ų)
0.13
QED
2
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H29Cl3F2N4O4
MW 653.94
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -1.08

Activity Summary

Ki 6 meas. best 8.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase beta-1
CHEMBL2617
Ki 8.12 7.26 7.6 2
Tryptase
CHEMBL4749
Ki 6.44 6.44 365.0 1
Plasminogen
CHEMBL1801
Ki 6.04 6.04 910.0 1
Trypsin
CHEMBL2095204
Ki 5.48 5.48 3300.0 1
Plasma kallikrein
CHEMBL2000
Ki 4.08 4.08 83000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase beta-1 Ki = 7.6 nM 8.12 Inhibition of human B tryptase 16644215
Tryptase Ki = 365.0 nM 6.44 Inhibition of mouse tryptase 16644215
Tryptase beta-1 Ki = 400.0 nM 6.4 Inhibition of monkey tryptase 16644215
Plasminogen Ki = 910.0 nM 6.04 Inhibition of plasmin 16644215
Trypsin Ki = 3300.0 nM 5.48 Inhibition of trypsin 16644215
Plasma kallikrein Ki = 83000.0 nM 4.08 Inhibition of kallikrein 16644215

Literature References

PubMed DOI Target Context # Activities
16644215 10.1016/j.bmcl.2006.04.013 Tryptase beta-1 2
16644215 10.1016/j.bmcl.2006.04.013 Unchecked 2
16644215 10.1016/j.bmcl.2006.04.013 Urokinase-type plasminogen activator 1
16644215 10.1016/j.bmcl.2006.04.013 Trypsin 1
16644215 10.1016/j.bmcl.2006.04.013 Prothrombin 1
16644215 10.1016/j.bmcl.2006.04.013 Plasminogen 1
16644215 10.1016/j.bmcl.2006.04.013 Plasma kallikrein 1
16644215 10.1016/j.bmcl.2006.04.013 Vitamin K-dependent protein C 1
16644215 10.1016/j.bmcl.2006.04.013 Chymotrypsinogen B 1
16644215 10.1016/j.bmcl.2006.04.013 Chymase 1
16644215 10.1016/j.bmcl.2006.04.013 Coagulation factor XI 1
16644215 10.1016/j.bmcl.2006.04.013 Granzyme K 1
16644215 10.1016/j.bmcl.2006.04.013 Tryptase 1
16644215 10.1016/j.bmcl.2006.04.013 Cathepsin G 1
16644215 10.1016/j.bmcl.2006.04.013 Coagulation factor VII 1
16644215 10.1016/j.bmcl.2006.04.013 Coagulation factor X 1
16644215 10.1016/j.bmcl.2006.04.013 Coagulation factor IX 1

Data from ChEMBL 36 via Core Engine