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Compound Detail

CHEMBL17436

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COc1cc(C(C)=O)ccc1OCCCN1CCC(C(O)(c2ccc(F)cc2)c2ccc(F)cc2)CC1

Basic Information

ChEMBL ID CHEMBL17436
Phase Preclinical
Structure Type MOL
InChI Key QFUKWQQHSSRPQM-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

509.6
MW (Da)
5.59
ALogP
5
HBA
1
HBD
59.0
PSA (Ų)
0.29
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H33F2NO4
MW 509.59
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.77

Activity Summary

IC50 1 meas. best 8.1
Kd 1 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL3943
IC50 8.1 8.1 8.0 1
Oryctolagus cuniculus
CHEMBL374
Kd 8.0 8.0 10.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2562852 10.1021/jm00121a022 Rattus norvegicus 3
2562852 10.1021/jm00121a022 Cavia porcellus 3
1920352 10.1021/jm00114a009 Rattus norvegicus 2
1920352 10.1021/jm00114a009 Oryctolagus cuniculus 1
2562852 10.1021/jm00121a022 Histamine H1 receptor 1

Data from ChEMBL 36 via Core Engine