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Compound Detail

CHEMBL3099498

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O=C(CC[C@H](NC(=O)CNC(=O)OCc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)OCc1ccccc1)NCC(=O)Nc1cccc2c(NCCCCCCCCNc3c4c(nc5ccccc35)CCCC4)c3c(nc12)CCCC3

Basic Information

ChEMBL ID CHEMBL3099498
Phase Preclinical
Structure Type MOL
InChI Key GMKNIGFXBQZAKP-YQOHNZFASA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

1136.4
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C67H77N9O8
MW 1136.41

Activity Summary

Ki 2 meas. best 8.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
Ki 8.72 8.72 1.9 1
Cholinesterase
CHEMBL1914
Ki 7.39 7.39 40.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase Ki = 1.92 nM 8.72 Inhibition of human acetylcholine esterase 24900626
Cholinesterase Ki = 40.9 nM 7.39 Inhibition of human butyrylcholine esterase 24900626

Literature References

PubMed DOI Target Context # Activities
24900626 10.1021/ml4002908 Amyloid-beta precursor protein 12
24900626 10.1021/ml4002908 Acetylcholinesterase 2
24900626 10.1021/ml4002908 Unchecked 1
24900626 10.1021/ml4002908 Cholinesterase 1

Data from ChEMBL 36 via Core Engine