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Compound Detail

CHEMBL109602

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N=C(N)NCCC[C@H]1C(=O)N(C(=O)N2CCN(S(=O)(=O)c3ccccc3)CC2)[C@@H]1C(=O)O

Basic Information

ChEMBL ID CHEMBL109602
Phase Preclinical
Structure Type MOL
InChI Key ZCBOGFQZYMUMCO-CABCVRRESA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

466.5
MW (Da)
-0.71
ALogP
6
HBA
4
HBD
177.2
PSA (Ų)
0.18
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H26N6O6S
MW 466.52
Aromatic Rings 1
Heavy Atoms 32
NP-Likeness -0.59

Activity Summary

IC50 1 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase
CHEMBL2095193
IC50 7.89 7.89 13.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 48.0 hr -
T1/2 1.7 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase IC50 = 13.0 nM 7.89 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