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Compound Detail

CHEMBL4636487

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Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCc1c[nH]cn1.O=C(O)C(F)(F)F.O=C([O-])C(F)(F)F

Basic Information

ChEMBL ID CHEMBL4636487
Phase Preclinical
Structure Type MOL
InChI Key AQJCVXSDQBVZED-UHFFFAOYSA-M
Parent Compound CHEMBL4651225
Active Moiety CHEMBL4651225
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

387.6
MW (Da)
4.74
ALogP
2
HBA
1
HBD
35.8
PSA (Ų)
0.45
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H32F6N4O4
MW 614.59
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.20

Activity Summary

Ki 2 meas. best 7.93

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 7.93 7.93 11.8 1
Histamine H4 receptor
CHEMBL3759
Ki 6.23 6.23 588.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32420741 10.1021/acs.jmedchem.0c00160 Histamine H4 receptor 1
32420741 10.1021/acs.jmedchem.0c00160 Histamine H3 receptor 1
32420741 10.1021/acs.jmedchem.0c00160 Histamine H2 receptor 1
32420741 10.1021/acs.jmedchem.0c00160 Histamine H1 receptor 1
32420741 10.1021/acs.jmedchem.0c00160 Unchecked 1

Data from ChEMBL 36 via Core Engine