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Compound Detail

CHEMBL172078

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CC(C)[C@H](NC(=O)OC(C)(C)C)C(=O)N1CCC[C@H]1C(=O)NC(Cc1ccccc1)C(=O)C(F)(F)C(=O)Nc1ccccc1C(=O)O

Basic Information

ChEMBL ID CHEMBL172078
Phase Preclinical
Structure Type MOL
InChI Key MOEROJCXGZXOPA-DJHGOXGWSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

658.7
MW (Da)
3.80
ALogP
7
HBA
4
HBD
171.2
PSA (Ų)
0.25
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H40F2N4O8
MW 658.70
Aromatic Rings 2
Heavy Atoms 47
NP-Likeness -0.62

Activity Summary

Ki 1 meas. best 5.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Chymase
CHEMBL4068
Ki 5.44 5.44 3620.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Chymase Ki = 3620.0 nM 5.44 Compound was evaluated for inhibitory activity against human heart chymase (HHC) 9871511

Literature References

PubMed DOI Target Context # Activities
9871511 10.1016/s0960-894x(98)00131-0 Chymase 1
9871511 10.1016/s0960-894x(98)00131-0 Chymotrypsinogen A 1
9871511 10.1016/s0960-894x(98)00131-0 Unchecked 1

Data from ChEMBL 36 via Core Engine