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Compound Detail

CHEMBL234290

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O=C(O)c1cc(C2=C(c3cc(C(F)(F)F)ccc3OCc3ccccc3)CCC2)ccn1

Basic Information

ChEMBL ID CHEMBL234290
Phase Preclinical
Structure Type MOL
InChI Key NRHSPKLTENMHSI-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
5
Publications
0
Known Names

Molecular Properties

439.4
MW (Da)
6.47
ALogP
3
HBA
1
HBD
59.4
PSA (Ų)
0.48
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H20F3NO3
MW 439.43
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.49

Activity Summary

IC50 1 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prostaglandin E2 receptor EP1 subtype
CHEMBL1811
IC50 7.4 7.4 39.8 1

Pharmacokinetic Data

Parameter Value Units Species
CL - - Rattus norvegicus
CL - - Rattus norvegicus
t1/2 - - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prostaglandin E2 receptor EP1 subtype IC50 = 39.81 nM 7.4 Inhibition of human EP1 receptor 17084082

Literature References

PubMed DOI Target Context # Activities
17084082 10.1016/j.bmcl.2006.10.041 Rattus norvegicus 3
17084082 10.1016/j.bmcl.2006.10.041 Prostaglandin E2 receptor EP1 subtype 1
17084082 10.1016/j.bmcl.2006.10.041 No relevant target 1
17084082 10.1016/j.bmcl.2006.10.041 Liver microsomes 1
17084082 10.1016/j.bmcl.2006.10.041 Cytochrome P450 2C9 1

Data from ChEMBL 36 via Core Engine