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Compound Detail

CHEMBL211357

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NCCCC[C@H](NC(=O)c1cc(F)cc(F)c1)C(=O)c1noc(Cc2ccc(C(=O)NCCc3cccc(Cl)c3)cc2)n1

Basic Information

ChEMBL ID CHEMBL211357
Phase Preclinical
Structure Type MOL
InChI Key QIHKHBGQSKPTOB-SANMLTNESA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

610.1
MW (Da)
4.67
ALogP
7
HBA
3
HBD
140.2
PSA (Ų)
0.14
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H30ClF2N5O4
MW 610.06
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -1.03

Activity Summary

Ki 3 meas. best 8.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase beta-1
CHEMBL2617
Ki 8.82 8.82 1.5 1
Unchecked
CHEMBL612545
Ki 8.82 8.82 1.5 1
Trypsin
CHEMBL2095204
Ki 6.39 6.39 410.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase beta-1 Ki = 1.5 nM 8.82 Inhibition of human beta tryptase 16714109
Unchecked Ki = 1.5 nM 8.82 Inhibition of human beta-tryptase 18053726
Trypsin Ki = 410.0 nM 6.39 Inhibition of human trypsin 16714109

Literature References

PubMed DOI Target Context # Activities
18053726 10.1016/j.bmc.2007.11.015 Unchecked 2
16714109 10.1016/j.bmcl.2006.05.009 No relevant target 1
16714109 10.1016/j.bmcl.2006.05.009 Unchecked 1
16714109 10.1016/j.bmcl.2006.05.009 Trypsin 1
16714109 10.1016/j.bmcl.2006.05.009 Tryptase beta-1 1

Data from ChEMBL 36 via Core Engine