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Compound Detail

CHEMBL91729

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Cc1ncccc1CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1

Basic Information

ChEMBL ID CHEMBL91729
Phase Preclinical
Structure Type MOL
InChI Key TWYWYAQDLCIHEK-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

416.0
MW (Da)
5.63
ALogP
3
HBA
0
HBD
29.0
PSA (Ų)
0.54
QED
1
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H26ClN3
MW 415.97
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.57

Activity Summary

IC50 2 meas. best 6.57
Ki 1 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL231
Ki 8.05 8.05 8.9 1
Cavia porcellus
CHEMBL369
IC50 6.57 6.57 270.0 1
Oryctolagus cuniculus
CHEMBL374
IC50 4.89 4.89 13000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7914928 10.1021/jm00043a009 Mus musculus 2
31274307 10.1021/acs.jmedchem.9b00447 Histamine H1 receptor 2
7914928 10.1021/jm00043a009 Oryctolagus cuniculus 1
7914928 10.1021/jm00043a009 Rattus norvegicus 1
7914928 10.1021/jm00043a009 Cavia porcellus 1

Data from ChEMBL 36 via Core Engine