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Compound Detail

CHEMBL322526

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CC(C)(C)OC(=O)N1CCN(C(=O)N2C(=O)[C@H](CCCN=C(N)N)[C@H]2C(N)=O)CC1

Basic Information

ChEMBL ID CHEMBL322526
Phase Preclinical
Structure Type MOL
InChI Key CBGNIBUPSHCBIU-NEPJUHHUSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

425.5
MW (Da)
-0.97
ALogP
6
HBA
3
HBD
177.7
PSA (Ų)
0.22
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H31N7O5
MW 425.49
Aromatic Rings 0
Heavy Atoms 30
NP-Likeness 0.01

Activity Summary

IC50 1 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase
CHEMBL2095193
IC50 9.4 9.4 0.4 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 42.0 hr -
T1/2 0.3 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase IC50 = 0.4 nM 9.4 In vitro inhibition of human tryptase. 12372540

Literature References

PubMed DOI Target Context # Activities
12372540 10.1016/s0960-894x(02)00688-1 Unchecked 5
12372540 10.1016/s0960-894x(02)00688-1 ADMET 2
12372540 10.1016/s0960-894x(02)00688-1 Tryptase 1

Data from ChEMBL 36 via Core Engine