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Compound Detail

CHEMBL434001

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OCCN1CCN(c2ncnc3c2oc2ccccc23)CC1

Basic Information

ChEMBL ID CHEMBL434001
Phase Preclinical
Structure Type MOL
InChI Key DSKGOKHOBPYUEE-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

298.4
MW (Da)
1.49
ALogP
6
HBA
1
HBD
65.6
PSA (Ų)
0.79
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 C16H18N4O2
MW 298.35
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -1.19

Activity Summary

IC50 1 meas.
Ki 1 meas. best 5.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL231
Ki 5.27 5.27 5370.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H1 receptor Ki = 5370.32 nM 5.27 Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK... 22007643

Literature References

PubMed DOI Target Context # Activities
17350255 10.1016/j.bmcl.2007.02.056 Unchecked 1
17350255 10.1016/j.bmcl.2007.02.056 Escherichia coli 1
22007643 10.1021/jm2011589 Histamine H1 receptor 1

Data from ChEMBL 36 via Core Engine