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Compound Detail

CHEMBL2158409

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COc1cc([C@H]2[C@](NC(=O)c3ccc(NC(=O)OC(C)(C)C)cc3)(C(=O)O)[C@@H](c3ccc(OC(=O)C(C)C)c(OC)c3)[C@]2(NC(=O)c2ccc(NC(=O)OC(C)(C)C)cc2)C(=O)O)ccc1OC(=O)C(C)C

Basic Information

ChEMBL ID CHEMBL2158409
Phase Preclinical
Structure Type MOL
InChI Key HQRAWJMCOYOPEO-SRLHGVHKSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

997.1
MW (Da)
7.91
ALogP
14
HBA
6
HBD
280.5
PSA (Ų)
0.05
QED
4
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C52H60N4O16
MW 997.06
Aromatic Rings 4
Heavy Atoms 72
NP-Likeness -0.16

Activity Summary

EC50 1 meas. best 5.86
IC50 1 meas. best 5.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glucagon-like peptide 1 receptor
CHEMBL5862
EC50 5.86 5.86 1380.0 1
Glucagon-like peptide 1 receptor
CHEMBL5862
IC50 5.12 5.12 7500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22103243 10.1021/jm201150j Glucagon-like peptide 1 receptor 5

Data from ChEMBL 36 via Core Engine