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Compound Detail

CHEMBL308763

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N=C(N)Nc1ccc(CNC(=O)N2CCN(C(=O)O[C@H]3CCC[C@@H](OC(=O)N4CCN(C(=O)NC[C@H]5CC[C@H](N)CC5)CC4)CCC3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL308763
Phase Preclinical
Structure Type MOL
InChI Key OAIOSQMKFBSMMD-OGMPSCQESA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

712.9
MW (Da)
3.03
ALogP
8
HBA
6
HBD
211.7
PSA (Ų)
0.18
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H56N10O6
MW 712.90
Aromatic Rings 1
Heavy Atoms 51
NP-Likeness -0.59

Activity Summary

Ki 2 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase
CHEMBL2095193
Ki 9.0 9.0 1.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase Ki = 1.0 nM 9.0 Evaluated for its inhibitory potency against tryptase 11055356

Literature References

PubMed DOI Target Context # Activities
11055356 10.1016/s0960-894x(00)00485-6 Tryptase 1
11055356 10.1016/s0960-894x(00)00485-6 Serine protease 1 1
11055356 10.1016/s0960-894x(00)00485-6 Prothrombin 1
11055356 10.1016/s0960-894x(00)00485-6 Plasminogen 1

Data from ChEMBL 36 via Core Engine