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Compound Detail

CHEMBL1078212

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N#C/N=C(\NCCCCc1ccccc1)NCCCc1c[nH]cn1

Basic Information

ChEMBL ID CHEMBL1078212
Phase Preclinical
Structure Type MOL
InChI Key ZKWGAWHXRZTQPB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

324.4
MW (Da)
2.38
ALogP
3
HBA
3
HBD
88.9
PSA (Ų)
0.29
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H24N6
MW 324.43
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -0.65

Activity Summary

EC50 1 meas. best 5.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H2 receptor
CHEMBL1941
EC50 5.05 5.05 8912.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H2 receptor EC50 = 8912.51 nM 5.05 Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpress... 19791743

Literature References

PubMed DOI Target Context # Activities
19791743 10.1021/jm900526h Histamine H2 receptor 2
19791743 10.1021/jm900526h Histamine H3 receptor 2
19791743 10.1021/jm900526h Histamine H4 receptor 1

Data from ChEMBL 36 via Core Engine