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Compound Detail

CHEMBL430526

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CC1=CCN(C(=O)[C@H](Cc2ccc(C(=N)N)cc2)NS(=O)(=O)c2ccc3c(c2)CN(C)CC3)[C@@H](C(=O)O)C1

Basic Information

ChEMBL ID CHEMBL430526
Phase Preclinical
Structure Type MOL
InChI Key ZDHBBBQAVLNJBL-BJKOFHAPSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

539.7
MW (Da)
1.48
ALogP
6
HBA
4
HBD
156.9
PSA (Ų)
0.22
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H33N5O5S
MW 539.66
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -0.33

Activity Summary

Ki 1 meas. best 9.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL209
Ki 9.34 9.34 0.5 1

Pharmacokinetic Data

Parameter Value Units Species
F 45.0 % Canis lupus familiaris
T1/2 0.8 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine protease 1 Ki = 0.46 nM 9.34 Binding affinity against Trypsin 10669559

Literature References

PubMed DOI Target Context # Activities
10669559 10.1021/jm990412m Serine protease 1 1
10669559 10.1021/jm990412m ADMET 1
10669559 10.1021/jm990412m Homo sapiens 1

Data from ChEMBL 36 via Core Engine