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Compound Detail

CHEMBL79655

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N=C(N)Nc1ccc(CNC(=O)N2CCN(C(=O)O[C@H]3CCC[C@@H](OC(=O)N4CCN(C(=O)NCc5ccccc5)CC4)CCC3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL79655
Phase Preclinical
Structure Type MOL
InChI Key IWHCIZMMRHJHFX-RNPORBBMSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

691.8
MW (Da)
3.71
ALogP
7
HBA
5
HBD
185.7
PSA (Ų)
0.21
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H49N9O6
MW 691.83
Aromatic Rings 2
Heavy Atoms 50
NP-Likeness -0.55

Activity Summary

Ki 4 meas. best 4.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase
CHEMBL2095193
Ki 4.82 4.82 15000.0 1
Tryptase beta-1
CHEMBL2617
Ki 4.82 4.82 15000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase beta-1 Ki = 15000.0 nM 4.82 Inhibitory potency against tryptase 11055355
Tryptase Ki = 15000.0 nM 4.82 Evaluated for its inhibitory potency against tryptase 11055356

Literature References

Data from ChEMBL 36 via Core Engine