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Compound Detail

CHEMBL438010

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COC(=O)N[C@H](C(=O)NN(Cc1ccc(Br)cc1)C(=O)CC[C@@](O)(Cc1ccccc1)C(=O)N[C@H]1c2ccccc2C[C@H]1O)C(C)(C)C

Basic Information

ChEMBL ID CHEMBL438010
Phase Preclinical
Structure Type MOL
InChI Key FPXYCCHKLAQWFU-AYZRFRAKSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

723.7
MW (Da)
4.11
ALogP
7
HBA
5
HBD
157.3
PSA (Ų)
0.19
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H43BrN4O7
MW 723.67
Aromatic Rings 3
Heavy Atoms 48
NP-Likeness 0.06

Activity Summary

Ki 1 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protease
CHEMBL2366517
Ki 6.92 6.92 120.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protease Ki = 120.0 nM 6.92 Inhibition of HIV1 protease expressed in Escherichia coli 18215014

Literature References

PubMed DOI Target Context # Activities
18215014 10.1021/jm070680h Protease 1
18215014 10.1021/jm070680h Human immunodeficiency virus 1 1
18215014 10.1021/jm070680h MT4 1

Data from ChEMBL 36 via Core Engine