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Compound Detail

CHEMBL5399120

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COc1ncc(C(=O)N2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cn1

Basic Information

ChEMBL ID CHEMBL5399120
Phase Preclinical
Structure Type MOL
InChI Key BXJIDYPPJRIREO-QPJJXVBHSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

431.3
MW (Da)
2.25
ALogP
5
HBA
0
HBD
75.6
PSA (Ų)
0.69
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H19BrN4O3
MW 431.29
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.95

Activity Summary

IC50 2 meas. best 7.53

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
G-protein coupled receptor 183
CHEMBL3259470
IC50 7.53 7.53 29.4 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.31 5.31 4900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38047891 10.1021/acs.jmedchem.3c01364 G-protein coupled receptor 183 1
38047891 10.1021/acs.jmedchem.3c01364 No relevant target 1
38047891 10.1021/acs.jmedchem.3c01364 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine