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Compound Detail

CHEMBL499301

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N=C(NCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL499301
Phase Preclinical
Structure Type MOL
InChI Key BCIVIRNJAROBHW-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

361.4
MW (Da)
2.81
ALogP
3
HBA
4
HBD
93.7
PSA (Ų)
0.38
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23N5O
MW 361.45
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.34

Activity Summary

EC50 1 meas. best 6.19
Kd 1 meas. best 5.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H2 receptor
CHEMBL2882
EC50 6.19 6.19 645.6 1
Histamine H1 receptor
CHEMBL3943
Kd 5.01 5.01 9772.4 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

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

Data from ChEMBL 36 via Core Engine