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Compound Detail

CHEMBL2179508

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Cc1noc(-c2ccc3c(c2)c2c(n3CCCOc3cc(F)cc(F)c3)CCCC2)n1

Basic Information

ChEMBL ID CHEMBL2179508
Phase Preclinical
Structure Type MOL
InChI Key GFRRDXNITYHDER-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
7
PK Parameters
3
Publications
0
Known Names

Molecular Properties

423.5
MW (Da)
5.63
ALogP
5
HBA
0
HBD
53.1
PSA (Ų)
0.38
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 C24H23F2N3O2
MW 423.46
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.57

Activity Summary

IC50 1 meas. best 8.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Scavenger receptor class B member 1
CHEMBL1914272
IC50 8.82 8.82 1.5 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 404.0 ng.hr.mL-1 Rattus norvegicus
CL 60.67 mL.min-1.kg-1 Rattus norvegicus
Cmax 1938.79 nM Rattus norvegicus
T1/2 0.8833 hr Rattus norvegicus
T1/2 0.9167 hr Homo sapiens
T1/2 3.76 hr Rattus norvegicus
Vd 22.09 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22784640 10.1016/j.bmcl.2012.06.038 Rattus norvegicus 5
22784640 10.1016/j.bmcl.2012.06.038 Liver microsomes 2
22784640 10.1016/j.bmcl.2012.06.038 Scavenger receptor class B member 1 1

Data from ChEMBL 36 via Core Engine