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Compound Detail

CHEMBL1160803

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CC(C)(C)[C@@H](NC(=O)N1CCOCC1)C(=O)NCC(=O)NC(Cc1ccc(NC(=N)N)cc1)C(=O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL1160803
Phase Preclinical
Structure Type MOL
InChI Key CHUNZFVEPFJQIA-DAFXYXGESA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

557.6
MW (Da)
0.72
ALogP
6
HBA
6
HBD
178.7
PSA (Ų)
0.19
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H34F3N7O5
MW 557.57
Aromatic Rings 1
Heavy Atoms 39
NP-Likeness -0.77

Activity Summary

Ki 2 meas. best 4.81

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasma kallikrein
CHEMBL2000
Ki 4.81 4.81 15500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasma kallikrein Ki = 15500.0 nM 4.81 Inhibitory activity of compound against human plasma Kallikrein (PK) 10091673

Literature References

PubMed DOI Target Context # Activities
10091673 10.1016/s0960-894x(98)00562-9 Plasma kallikrein 1
10091673 10.1016/s0960-894x(98)00562-9 Kallikrein-1 1
10091673 10.1016/s0960-894x(98)00562-9 Plasminogen 1

Data from ChEMBL 36 via Core Engine