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Compound Detail

CHEMBL42900

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

Basic Information

ChEMBL ID CHEMBL42900
Phase Preclinical
Structure Type MOL
InChI Key BJUPAZWABXENNS-HNRBIFIRSA-N
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

686.9
MW (Da)
2.64
ALogP
8
HBA
6
HBD
211.7
PSA (Ų)
0.12
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H54N10O6
MW 686.86
Aromatic Rings 1
Heavy Atoms 49
NP-Likeness -0.52

Activity Summary

Ki 3 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase
CHEMBL2095193
Ki 9.3 9.3 0.5 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase Ki = 0.5 nM 9.3 Inhibition of Tryptase in human mast cells 11425524
Tryptase Ki = 0.5 nM 9.3 Evaluated for its inhibitory potency against tryptase 11055356

Literature References

Data from ChEMBL 36 via Core Engine