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Compound Detail

CHEMBL110061

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CNC(=O)[C@@H]1[C@@H](CCCN=C(N)N)C(=O)N1C(=O)N1CCN(C(=O)OC(C)(C)C)CC1

Basic Information

ChEMBL ID CHEMBL110061
Phase Preclinical
Structure Type MOL
InChI Key HXHUFCTVAIQYDR-OLZOCXBDSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

439.5
MW (Da)
-0.71
ALogP
6
HBA
3
HBD
163.7
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 C19H33N7O5
MW 439.52
Aromatic Rings 0
Heavy Atoms 31
NP-Likeness -0.06

Activity Summary

IC50 1 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase
CHEMBL2095193
IC50 9.15 9.15 0.7 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 31.8 hr -
T1/2 0.3 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase IC50 = 0.7 nM 9.15 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