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Compound Detail

CHEMBL43650

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CC(C)C[C@@H](/C=N/N1CCOCC1)NC(=O)[C@@H](NS(=O)(=O)c1ccc(F)cc1)C(C)C

Basic Information

ChEMBL ID CHEMBL43650
Phase Preclinical
Structure Type MOL
InChI Key NGFKOMHSHVCOKM-BWJMPLKHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

456.6
MW (Da)
1.98
ALogP
6
HBA
2
HBD
100.1
PSA (Ų)
0.52
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H33FN4O4S
MW 456.58
Aromatic Rings 1
Heavy Atoms 31
NP-Likeness -1.15

Activity Summary

IC50 1 meas. best 6.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Calpain-1 catalytic subunit
CHEMBL4062
IC50 6.1 6.1 790.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Calpain-1 catalytic subunit IC50 = 790.0 nM 6.1 Tested for inhibitory activity against porcine erythrocyte Mu-calpain 12039572

Literature References

PubMed DOI Target Context # Activities
12039572 10.1016/s0960-894x(02)00226-3 ADMET 4
12039572 10.1016/s0960-894x(02)00226-3 Calpain-1 catalytic subunit 1

Data from ChEMBL 36 via Core Engine