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Compound Detail

CHEMBL3617788

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CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)O

Basic Information

ChEMBL ID CHEMBL3617788
Phase Preclinical
Structure Type BOTH
InChI Key AJRCWFAECDBHHJ-CYPNIFRBSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

987.1
MW (Da)
-2.22
ALogP
12
HBA
15
HBD
436.4
PSA (Ų)
0.02
QED
3
Ro5 Violations
31
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C44H66N12O14
MW 987.08
Aromatic Rings 2
Heavy Atoms 70
NP-Likeness 0.16

Activity Summary

EC50 1 meas. best 4.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Keap1/Nrf2
CHEMBL3038498
EC50 4.77 4.77 17100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Keap1/Nrf2 EC50 = 17100.0 nM 4.77 Inhibition of Keap1 (unknown origin) interaction to Nrf2 26348784

Literature References

PubMed DOI Target Context # Activities
26348784 10.1021/acs.jmedchem.5b00602 Keap1/Nrf2 1

Data from ChEMBL 36 via Core Engine