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Compound Detail

CHEMBL268695

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CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(CO)cnc32)CC1

Basic Information

ChEMBL ID CHEMBL268695
Phase Preclinical
Structure Type MOL
InChI Key MEWHFGOCTSSITK-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

382.9
MW (Da)
3.77
ALogP
3
HBA
1
HBD
53.4
PSA (Ų)
0.82
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23ClN2O2
MW 382.89
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.30

Activity Summary

IC50 2 meas. best 6.16
Ki 1 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL4701
Ki 7.7 7.7 20.0 1
Homo sapiens
CHEMBL372
IC50 6.16 6.16 690.0 1
Protein farnesyltransferase
CHEMBL2094108
IC50 4.39 4.39 41000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9406600 10.1021/jm970291v Protein farnesyltransferase 1
- 10.1016/S0960-894X(00)80290-5 Homo sapiens 1
- 10.1016/S0960-894X(00)80290-5 Histamine H1 receptor 1

Data from ChEMBL 36 via Core Engine