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Compound Detail

CHEMBL77183

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NCCCCNC(=O)N1CCN(C(=O)O[C@H]2CCC[C@@H](OC(=O)N3CCN(C(=O)NCCCCN)CC3)CCC2)CC1

Basic Information

ChEMBL ID CHEMBL77183
Phase Preclinical
Structure Type MOL
InChI Key DSGUZTNQDJPJCQ-PSWAGMNNSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

596.8
MW (Da)
1.48
ALogP
8
HBA
4
HBD
175.8
PSA (Ų)
0.27
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H52N8O6
MW 596.77
Aromatic Rings 0
Heavy Atoms 42
NP-Likeness -0.35

Activity Summary

Ki 1 meas. best 6.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase
CHEMBL2095193
Ki 6.29 6.29 510.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase Ki = 510.0 nM 6.29 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