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Compound Detail

CHEMBL77043

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N=C(N)N1CCC(CCNC(=O)N2CCN(C(=O)O[C@H]3CCC[C@@H](OC(=O)N4CCN(C(=O)NCCC5CCN(C(=N)N)CC5)CC4)CCC3)CC2)CC1

Basic Information

ChEMBL ID CHEMBL77043
Phase Preclinical
Structure Type MOL
InChI Key OPSSBUHWCXHUBD-RNPORBBMSA-N
1
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

761.0
MW (Da)
2.00
ALogP
8
HBA
6
HBD
230.0
PSA (Ų)
0.16
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H64N12O6
MW 760.99
Aromatic Rings 0
Heavy Atoms 54
NP-Likeness -0.38

Activity Summary

Ki 4 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase
CHEMBL2095193
Ki 7.52 7.52 30.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase Ki = 30.0 nM 7.52 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