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Compound Detail

CHEMBL2392182

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COc1ccc(C(=O)Nc2cc(Br)cc3c(=O)cc(C(=O)O)oc23)nc1

Basic Information

ChEMBL ID CHEMBL2392182
Phase Preclinical
Structure Type MOL
InChI Key HUCLWZDRJIRCBM-UHFFFAOYSA-N
3
Targets
4
Activities
3
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

419.2
MW (Da)
2.91
ALogP
6
HBA
2
HBD
118.7
PSA (Ų)
0.67
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H11BrN2O6
MW 419.19
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -0.65

Activity Summary

EC50 2 meas. best 6.84
IC50 1 meas. best 5.05
Ki 1 meas. best 7.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
G-protein coupled receptor 35
CHEMBL1293267
Ki 7.25 7.25 56.8 1
G-protein coupled receptor 35
CHEMBL1293267
EC50 6.84 6.84 144.0 1
G protein-coupled receptor GPR35
CHEMBL2390812
EC50 5.81 5.81 1540.0 1
G-protein coupled receptor 55
CHEMBL1075322
IC50 5.05 5.05 8920.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23713606 10.1021/jm400587g G-protein coupled receptor 35 3
23713606 10.1021/jm400587g G-protein coupled receptor 55 2
23713606 10.1021/jm400587g G protein-coupled receptor GPR35 2
23888932 10.1021/jm4009373 G-protein coupled receptor 35 1

Data from ChEMBL 36 via Core Engine