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Compound Detail

CHEMBL259339

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O=S(=O)(c1ccc2c(c1)OC(c1ccccc1)(c1ccccc1)O2)N1CC=C(c2ccc(F)cc2)CC1

Basic Information

ChEMBL ID CHEMBL259339
Phase Preclinical
Structure Type MOL
InChI Key HAQRKBMHJXTTRZ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

513.6
MW (Da)
5.98
ALogP
4
HBA
0
HBD
55.8
PSA (Ų)
0.33
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H24FNO4S
MW 513.59
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -0.82

Activity Summary

Ki 1 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cannabinoid receptor 1
CHEMBL218
Ki 7.89 7.89 13.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL - - Homo sapiens
CL - - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cannabinoid receptor 1 Ki = 13.0 nM 7.89 Displacement of [3H]CP-55940 from human CB1R expressed in HEK293 cells 18335976

Literature References

PubMed DOI Target Context # Activities
18335976 10.1021/jm701487t Cannabinoid receptor 1 2
18335976 10.1021/jm701487t Liver microsomes 2
18335976 10.1021/jm701487t Mus musculus 1
18335976 10.1021/jm701487t Cannabinoid receptor 2 1

Data from ChEMBL 36 via Core Engine