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Compound Detail

CHEMBL472273

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N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccc(F)cc1)c1ccccn1

Basic Information

ChEMBL ID CHEMBL472273
Phase Preclinical
Structure Type MOL
InChI Key UTJRWVBWVPCMQL-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

394.4
MW (Da)
2.74
ALogP
4
HBA
4
HBD
106.5
PSA (Ų)
0.27
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 C21H23FN6O
MW 394.45
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.87

Activity Summary

EC50 1 meas. best 7.47
Kd 1 meas. best 5.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H2 receptor
CHEMBL2882
EC50 7.47 7.47 33.9 1
Histamine H1 receptor
CHEMBL3943
Kd 5.43 5.43 3715.3 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