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Compound Detail

CHEMBL60342

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Fc1ccc(C(OCCCc2c[nH]cn2)c2ccc(F)cc2)cc1.O=C(O)/C=C\C(=O)O

Basic Information

ChEMBL ID CHEMBL60342
Phase Preclinical
Structure Type MOL
InChI Key FUZFRHWMRFPIQH-BTJKTKAUSA-N
Parent Compound CHEMBL1179104
Active Moiety CHEMBL1179104
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

328.4
MW (Da)
4.43
ALogP
2
HBA
1
HBD
37.9
PSA (Ų)
0.65
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H22F2N2O5
MW 444.43
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -0.59

Activity Summary

Ki 1 meas. best 7.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL4124
Ki 7.6 7.6 25.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H3 receptor Ki = 25.12 nM 7.6 In vitro antagonistic activity against histamine H3-receptor in an assay with K+... -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(96)00361-7 Histamine H3 receptor 2
- 10.1016/0960-894X(96)00361-7 Histamine H1 receptor 1
- 10.1016/0960-894X(96)00361-7 Histamine H2 receptor 1

Data from ChEMBL 36 via Core Engine