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Compound Detail

CHEMBL2028906

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CC[C@H](C)[C@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)OCc1ccccc1)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC)C(C)C

Basic Information

ChEMBL ID CHEMBL2028906
Phase Preclinical
Structure Type MOL
InChI Key LIQDTPYQUQZTGR-GCFINZEGSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

991.2
MW (Da)
2.27
ALogP
11
HBA
11
HBD
331.4
PSA (Ų)
0.02
QED
3
Ro5 Violations
26
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C49H74N12O10
MW 991.20
Aromatic Rings 3
Heavy Atoms 71
NP-Likeness -0.11

Activity Summary

Ki 3 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin B
CHEMBL4072
Ki 7.89 7.89 13.0 1
Papain
CHEMBL4779
Ki 7.77 7.77 17.0 1
Cathepsin K
CHEMBL268
Ki 7.14 7.14 72.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin B Ki = 13.0 nM 7.89 Inhibition of Human Cathepsin B 12213061
Papain Ki = 17.0 nM 7.77 In vitro inhibition of papain. 12213061
Cathepsin K Ki = 72.0 nM 7.14 Inhibition of Human Cathepsin K 12213061

Literature References

PubMed DOI Target Context # Activities
12213061 10.1021/jm020850k Papain 1
12213061 10.1021/jm020850k Cathepsin B 1
12213061 10.1021/jm020850k Cathepsin K 1

Data from ChEMBL 36 via Core Engine