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Compound Detail

CHEMBL79545

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N=C(N)Nc1ccc(CNC(=O)CCCC(=O)NCc2ccc(CNC(=O)CCCC(=O)NCc3ccc(NC(=N)N)cc3)cc2)cc1

Basic Information

ChEMBL ID CHEMBL79545
Phase Preclinical
Structure Type MOL
InChI Key MQFPKMGNYBQKII-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

656.8
MW (Da)
2.50
ALogP
6
HBA
10
HBD
240.2
PSA (Ų)
0.07
QED
2
Ro5 Violations
18
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H44N10O4
MW 656.79
Aromatic Rings 3
Heavy Atoms 48
NP-Likeness -0.35

Activity Summary

Ki 3 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase beta-1
CHEMBL2617
Ki 7.0 7.0 100.0 1
Serine protease 1
CHEMBL209
Ki 4.16 4.16 70000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase beta-1 Ki = 100.0 nM 7.0 Inhibitory potency against tryptase 11055355
Serine protease 1 Ki = 70000.0 nM 4.16 Inhibitory potency against trypsin 11055355

Literature References

PubMed DOI Target Context # Activities
11055355 10.1016/s0960-894x(00)00484-4 Tryptase beta-1 1
11055355 10.1016/s0960-894x(00)00484-4 Serine protease 1 1
11055355 10.1016/s0960-894x(00)00484-4 Prothrombin 1
11055355 10.1016/s0960-894x(00)00484-4 Plasminogen 1

Data from ChEMBL 36 via Core Engine