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Compound Detail

CHEMBL2376797

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CCc1ccc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1

Basic Information

ChEMBL ID CHEMBL2376797
Phase Preclinical
Structure Type MOL
InChI Key HUMDXPQUUMTPFD-LLVKDONJSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

271.4
MW (Da)
1.57
ALogP
5
HBA
2
HBD
67.1
PSA (Ų)
0.89
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H21N5
MW 271.37
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -1.15

Activity Summary

Ki 3 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H4 receptor
CHEMBL3759
Ki 7.77 7.77 17.0 1
Histamine H3 receptor
CHEMBL264
Ki 6.22 6.22 602.6 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
Ki 5.56 5.56 2754.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23558237 10.1016/j.bmcl.2013.02.091 Voltage-gated inwardly rectifying potassium channel KCNH2 1
23558237 10.1016/j.bmcl.2013.02.091 Unchecked 1
23558237 10.1016/j.bmcl.2013.02.091 Histamine H3 receptor 1
23558237 10.1016/j.bmcl.2013.02.091 Histamine H4 receptor 1

Data from ChEMBL 36 via Core Engine