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Compound Detail

CHEMBL504260

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O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1

Basic Information

ChEMBL ID CHEMBL504260
Phase Preclinical
Structure Type MOL
InChI Key BPAUVSAWZVWRTJ-AREMUKBSSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

597.6
MW (Da)
5.71
ALogP
7
HBA
3
HBD
112.0
PSA (Ų)
0.21
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H26F3N3O5S
MW 597.62
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -1.06

Activity Summary

IC50 1 meas. best 6.65

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glucagon receptor
CHEMBL1985
IC50 6.65 6.65 225.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Glucagon receptor IC50 = 225.0 nM 6.65 Displacement of [125I]porcine glucagon from human recombinant glucagon receptor ... 19385613

Literature References

PubMed DOI Target Context # Activities
19385613 10.1021/jm8016249 Unchecked 2
19385613 10.1021/jm8016249 Glucagon receptor 1
19385613 10.1021/jm8016249 Gastric inhibitory polypeptide receptor 1

Data from ChEMBL 36 via Core Engine