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Compound Detail

CHEMBL472272

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N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccn1

Basic Information

ChEMBL ID CHEMBL472272
Phase Preclinical
Structure Type MOL
InChI Key XPEMILVWHHWGBE-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

376.5
MW (Da)
2.60
ALogP
4
HBA
4
HBD
106.5
PSA (Ų)
0.28
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H24N6O
MW 376.46
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.60

Activity Summary

EC50 1 meas. best 7.29
Kd 1 meas. best 4.95

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H2 receptor
CHEMBL2882
EC50 7.29 7.29 51.3 1
Histamine H1 receptor
CHEMBL3943
Kd 4.95 4.95 11220.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18950149 10.1021/jm800841w Histamine H2 receptor 3
18950149 10.1021/jm800841w Histamine H1 receptor 2

Data from ChEMBL 36 via Core Engine